Journal articles: 'Drug receptors'

1

Shaw, P., and L. S. Pilowsky. "Probing Cortical Sites of Antipsychotic Drug Action within vivoReceptor Imaging." Behavioural Neurology 12, no. 1-2 (2000): 3–9. http://dx.doi.org/10.1155/2000/184707.

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Imaging receptors using radioactive ligands has allowed direct determination of the sites of action of antipsychotic drugs. Initial studies relating antipsychotic drug efficacy to action at striatal dopamine D2-like receptors have recently been undermined. Developments in imaging extrastriatal dopamine D2-like receptors suggest rather that antagonism of these receptors in the temporal cortex is the common site of action for antipsychotic drugs, with occupancy at striatal receptors relating more closely to extrapyramidal side effects. Further work into dopamine receptor subtypes and other receptor groups such as serotonin and GABA neurotransmitters awaits the development of suitable probes, but there are some initial finding. Again a main site of antipsychotic drug action is at cortical levels with high degrees of cortical D1 and 5HT2areceptor occupancy attained particularly by atypical antipsychotic drugs.

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Hartig, Paul R. "Can cloned receptors aid drug research?" Proceedings of the Royal Society of Edinburgh. Section B. Biological Sciences 99, no. 1-2 (1992): 19–25. http://dx.doi.org/10.1017/s0269727000013014.

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Synopsis:Over 50 different neurotransmitter and hormone receptors have been cloned, transfected and characterised. Within the pharmaceutical industry, the thrust of this research is now moving from receptor cloning to focussed application of these new tools to the task of drug development. With human receptor clones now available, it is possible to target drug design to single human proteins from the inception of a drug-design project. A critical question is whether human genes will express a human pharmacology when expressed in non-human, non-neuronal cell lines. Relevant results from studies with the human serotonin 5-HT2 and 5-HT1D receptors are presented, including the cloning of a rat 5-HT1B receptor which is homologous to a human 5-HT1D receptor gene. Another issue is the relationship between agonist and antagonist binding sites. The ability to study individual human receptors in selected cell lines which are free from interfering receptors has helped to advance our understanding of this relationship. Studies comparing agonist and antagonist binding sites of the human 5-HT2 receptor are described. Finally, the fact that so many neurotransmitter receptors belong to the same gene superfamily, the G-protein-coupled or 7TM (7 transmembrane domain) receptor superfamily, allows us to form new insights about receptor structure and function. Examples where comparative studies of gene sequences are helping to predict pharmacological properties of drugs are described.

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Takayanagl, Issei. "Drug receptors and drug design." Japanese Journal of Pharmacology 67 (1995): 45. http://dx.doi.org/10.1016/s0021-5198(19)46150-7.

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Sunahara, Roger K., Philip Seeman, Hubert H. M. Van Tol, and Hyman B. Niznik. "Dopamine Receptors and Antipsychotic Drug Response." British Journal of Psychiatry 163, S22 (December 1993): 31–38. http://dx.doi.org/10.1192/s000712500029257x.

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Dopamine receptors have been divided into two major types – D1 and D2 – based primarily on pharmacological and biochemical criteria. Recent advances in the molecular biology of the dopamine receptor system have allowed the identification and characterisation of at least five distinct neuronal dopamine receptor genes (D1 to D5). These genes encode dopamine receptors belonging to the D1 receptor family, termed D1 and D5, and three D2-like receptors, termed D2, D3 and D4. These receptors are distinguished on the basis of their primary structure, chromosomal location, mRNA size and tissue distribution, and biochemical and pharmacological differences. Although individually these receptor subtypes may not be directly and exclusively involved in the maintenance or expression of schizophrenia, alterations of any of the receptors may contribute to the perturbation or instability of dopaminergic homeostasis in the brain. What was once thought to be a simple two-receptor system seems to have emerged as an intricate and interactive entity. This review summarises what is currently understood about dopamine receptors, their role in antipsychotic drug action, and their association with psychosis.

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García-Nafría, Javier, and Christopher G. Tate. "Cryo-Electron Microscopy: Moving Beyond X-Ray Crystal Structures for Drug Receptors and Drug Development." Annual Review of Pharmacology and Toxicology 60, no. 1 (January 6, 2020): 51–71. http://dx.doi.org/10.1146/annurev-pharmtox-010919-023545.

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Electron cryo-microscopy (cryo-EM) has revolutionized structure determination of membrane proteins and holds great potential for structure-based drug discovery. Here we discuss the potential of cryo-EM in the rational design of therapeutics for membrane proteins compared to X-ray crystallography. We also detail recent progress in the field of drug receptors, focusing on cryo-EM of two protein families with established therapeutic value, the γ-aminobutyric acid A receptors (GABAARs) and G protein–coupled receptors (GPCRs). GABAARs are pentameric ion channels, and cryo-EM structures of physiological heteromeric receptors in a lipid environment have uncovered the molecular basis of receptor modulation by drugs such as diazepam. The structures of ten GPCR–G protein complexes from three different classes of GPCRs have now been determined by cryo-EM. These structures give detailed insights into molecular interactions with drugs, GPCR–G protein selectivity, how accessory membrane proteins alter receptor–ligand pharmacology, and the mechanism by which HIV uses GPCRs to enter host cells.

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Suvarna, B. S. "Drug - Receptor Interactions." Kathmandu University Medical Journal 9, no. 3 (June 13, 2012): 203–7. http://dx.doi.org/10.3126/kumj.v9i3.6306.

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In present-day pharmacology and medicine, it is usually taken for granted that cells contain a host of highly specific receptors. Drugs act on the cell membrane by physical and/or chemical interactions. This is usually through specific drug receptor sites known to be located on the membrane. These are defined as proteins on or within the cell that bind with specificity to particular drugs, chemical messenger substances or hormones and mediate their effects on the body. Today, the concept of specific receptors for drugs and transmitters lies at the very heart of pharmacology. However, it is only relatively recently that the notion of drug-specific receptors has become widely accepted, with considerable doubts being expressed about their existence as late as the 1960s.DOI: http://dx.doi.org/10.3126/kumj.v9i3.6306 Kathmandu Univ Med J 2011;9(3):203-7

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Kondej, Magda, Piotr Stępnicki, and Agnieszka A. Kaczor. "Multi-Target Approach for Drug Discovery against Schizophrenia." International Journal of Molecular Sciences 19, no. 10 (October 10, 2018): 3105. http://dx.doi.org/10.3390/ijms19103105.

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Polypharmacology is nowadays considered an increasingly crucial aspect in discovering new drugs as a number of original single-target drugs have been performing far behind expectations during the last ten years. In this scenario, multi-target drugs are a promising approach against polygenic diseases with complex pathomechanisms such as schizophrenia. Indeed, second generation or atypical antipsychotics target a number of aminergic G protein-coupled receptors (GPCRs) simultaneously. Novel strategies in drug design and discovery against schizophrenia focus on targets beyond the dopaminergic hypothesis of the disease and even beyond the monoamine GPCRs. In particular these approaches concern proteins involved in glutamatergic and cholinergic neurotransmission, challenging the concept of antipsychotic activity without dopamine D2 receptor involvement. Potentially interesting compounds include ligands interacting with glycine modulatory binding pocket on N-methyl-d-aspartate (NMDA) receptors, positive allosteric modulators of α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors, positive allosteric modulators of metabotropic glutamatergic receptors, agonists and positive allosteric modulators of α7 nicotinic receptors, as well as muscarinic receptor agonists. In this review we discuss classical and novel drug targets for schizophrenia, cover benefits and limitations of current strategies to design multi-target drugs and show examples of multi-target ligands as antipsychotics, including marketed drugs, substances in clinical trials, and other investigational compounds.

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Sonoda, J., and R. M. Evans. "Biological function and mode of action of nuclear xenobiotic receptors." Pure and Applied Chemistry 75, no. 11-12 (January 1, 2003): 1733–42. http://dx.doi.org/10.1351/pac200375111733.

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Two related nuclear receptors, the pregnane X receptor (PXR) and the constitutive androstane receptor (CAR), act as xenobiotic sensors that protect the body from a multitude of foreign chemicals (xenobiotics) and play a central role in the metabolism and clearance of steroids and toxic endogenous lipids (endobiotics). A structurally diverse array of chemicals including pharmaceutical drugs, steroids, herbal extracts, and pesticides activate PXR or CAR. This activation results in induction of overlapping, but yet distinct drug clearance pathways consisting of cytochrome P450 enzymes, conjugating enzymes, drug transporters, and other related proteins. Similar pathways are also utilized to protect the body from toxic compounds of endogenous origin. Thus, the xenobiotic regulatory circuit contributes both to drug-drug and food-drug interactions as well as endocrine disruption. Consistent with the notion that xenobiotic receptors regulate drug clearance, single nucleotide polymorphisms (SNPs) in either the receptors themselves or receptor-binding sites in the regulatory region of genes encoding metabolic enzymes appear to contribute to the polymorphic expression of components of drug clearance pathways. Together, the xenobiotic receptors PXR and CAR confer metabolic immunity via the ability to control an integrated array of target genes.

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9

Parker, E. M., and D. W. Smith. "G Protein-Coupled Serotonin Receptors-Multiple Subtypes, Multiple Opportunities." Current Pharmaceutical Design 1, no. 3 (October 1995): 363–72. http://dx.doi.org/10.2174/1381612801666220918170118.

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Serotonin receptors have been fertile targets for drug development for decades. The attractiveness of serotonin receptors as drug targets is due to the wide range of physiological processes in which serotonin plays a role and to diversity of receptor subtypes that mediate the physiological effects of serotonin. The powerful combination of molecular cloning and pharmacology has thus far led to the identification of fifteen different serotonin receptor subtypes. Fourteen of these serotonin receptors are G protein coupled receptors and one is a ligand-gated ion channel. Because many of these serotonin receptor subtypes have been identified very recently, the current opportunities for development of d gs that act via these receptors are manifold. This chapter focuses on recent molecular insights into the structure and function of serotonin receptors, discusses the relevance of these insights to the design and discovery of receptor selective drugs and reviews recently discovered selective antagonists for serotonin receptors.

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10

Reynolds, Gavin P., and Olga O. McGowan. "Mechanisms underlying metabolic disturbances associated with psychosis and antipsychotic drug treatment." Journal of Psychopharmacology 31, no. 11 (September 11, 2017): 1430–36. http://dx.doi.org/10.1177/0269881117722987.

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The increase in cardiovascular disease and reduced life expectancy in schizophrenia likely relate to an increased prevalence of metabolic disturbances. Such metabolic risk factors in schizophrenia may result from both symptom-related effects and aetiological factors. However, a major contributory factor is that of treatment with antipsychotic drugs. These drugs differ in effects on body weight; the underlying mechanisms are not fully understood and may vary between drugs, but may include actions at receptors associated with the hypothalamic control of food intake. Evidence supports 5-hydroxytryptamine receptor 2C and dopamine D2 receptor antagonism as well as antagonism at histamine H1 and muscarinic M3 receptors. These M3 receptors may also mediate the effects of some drugs on glucose regulation. Several antipsychotics showing little propensity for weight gain, such as aripiprazole, have protective pharmacological mechanisms, rather than just the absence of a hyperphagic effect. In addition to drug differences, there is large individual variation in antipsychotic drug-induced weight gain. This pharmacogenetic association reflects genetic variation in several drug targets, including the 5-hydroxytryptamine receptor 2C, as well as genes involved in obesity and metabolic disturbances. Thus predictive genetic testing for drug-induced weight gain would represents a first step towards personalised medicine addressing this severe and problematic iatrogenic disease.

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11

Gado, Francesca, Serena Meini, Simone Bertini, Maria Digiacomo, Marco Macchia, and Clementina Manera. "Allosteric modulators targeting cannabinoid cb1 and cb2 receptors: implications for drug discovery." Future Medicinal Chemistry 11, no. 15 (August 2019): 2019–37. http://dx.doi.org/10.4155/fmc-2019-0005.

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Allosteric modulators of cannabinoid receptors hold great therapeutic potential, as they do not possess intrinsic efficacy, but instead enhance or diminish the receptor's response of orthosteric ligands allowing for the tempering of cannabinoid receptor signaling without the desensitization, tolerance and dependence. Allosteric modulators of cannabinoid receptors have numerous advantages over the orthosteric ligands such as higher receptor type selectivity, probe dependence and biased signaling, so they have a great potential to separate the therapeutic benefits from side effects own of orthosteric ligands. This review aims to give an overview of the CB1 and CB2 receptor allosteric modulators highlighting the structure–activity relationship and pharmacological profile of each classes, and their future promise.

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12

Snyder, Solomon H. "Drug and Neurotransmitter Receptors." JAMA 261, no. 21 (June 2, 1989): 3126. http://dx.doi.org/10.1001/jama.1989.03420210074019.

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13

Williams, Michael. "Receptors as Drug Targets." Current Protocols in Pharmacology 00, no. 1 (March 1998): 1.1.1–1.1.17. http://dx.doi.org/10.1002/0471141755.ph0101s00.

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14

Hanada, Takahisa. "Ionotropic Glutamate Receptors in Epilepsy: A Review Focusing on AMPA and NMDA Receptors." Biomolecules 10, no. 3 (March 18, 2020): 464. http://dx.doi.org/10.3390/biom10030464.

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It is widely accepted that glutamate-mediated neuronal hyperexcitation plays a causative role in eliciting seizures. Among glutamate receptors, the roles of N-methyl-D-aspartate (NMDA) and α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptors in physiological and pathological conditions represent major clinical research targets. It is well known that agonists of NMDA or AMPA receptors can elicit seizures in animal or human subjects, while antagonists have been shown to inhibit seizures in animal models, suggesting a potential role for NMDA and AMPA receptor antagonists in anti-seizure drug development. Several such drugs have been evaluated in clinical studies; however, the majority, mainly NMDA-receptor antagonists, failed to demonstrate adequate efficacy and safety for therapeutic use, and only an AMPA-receptor antagonist, perampanel, has been approved for the treatment of some forms of epilepsy. These results suggest that a misunderstanding of the role of each glutamate receptor in the ictogenic process may underlie the failure of these drugs to demonstrate clinical efficacy and safety. Accumulating knowledge of both NMDA and AMPA receptors, including pathological gene mutations, roles in autoimmune epilepsy, and evidence from drug-discovery research and pharmacological studies, may provide valuable information enabling the roles of both receptors in ictogenesis to be reconsidered. This review aimed to integrate information from several studies in order to further elucidate the specific roles of NMDA and AMPA receptors in epilepsy.

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Balabolkin, M. I., and L. B. Nedosugova. "The use of second generation sulfonylurea agents and the role of glurenorm in the therapy of non-insulin-dependent diabetes mellitus." Problems of Endocrinology 41, no. 2 (April 15, 1995): 11–14. http://dx.doi.org/10.14341/probl11362.

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Sulfonylurea drugs stimulate the 1st phase of insulin secretion, activate adenylate cyclase, inhibit phosphodiesterase or cause prolonged depolarization of the beta cell membrane. The peripheral effect of the hypoglycemic action of sulfonylurea drugs is mediated through the effect on insulin receptors. It is clearly shown that sulfonylureas lead to an increase in the number of receptors on target cells (hepatocytes, muscle and adipose tissue, lymphocytes and other cells). It is known that patients with type II diabetes mellitus have a decrease in both the number of receptors and their affinity. The increase in the number of receptors on the membrane of target cells is not due to their de novo synthesis, but by improving the return of the receptor to the membrane from the cytosol, where they are translocated as an insulin-receptor complex after the interaction of insulin with the corresponding receptor. One of the sulfonylurea drugs of the second generation is Gliquidone (glurenorm). This drug has one advantage, distinguishing it from other sulfonylurea drugs. About 95% of the drug is excreted from the body through the gastrointestinal tract, and only 5% is extracted by the kidneys. Therefore, it is the drug of choice in the treatment of diabetic patients with nephropathy, given the fact that the drug is metabolized in the liver and eliminated through the bile ducts into the intestine. Naturally, the question arises of the possibility of its influence on the liver function of patients who have been receiving long-term treatment with glurenorm.

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16

LaBella, Frank S. "Cytochrome P450 enzymes: ubiquitous "receptors" for drugs." Canadian Journal of Physiology and Pharmacology 69, no. 8 (August 1, 1991): 1129–32. http://dx.doi.org/10.1139/y91-165.

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Most foreign compounds bind to one or more cytochrome P450 drug-metabolizing isozymes. These heme monooxygenases are most concentrated in the endoplasmic reticulum of liver cells but are present in virtually all biological membranes and in all cells. Some radioligands for known hormone receptors have been found to label, with comparable affinities, specific P450 enzymes. A characteristic feature of P450 enzymes is their broad and overlapping drug specificities, with affinity constants ranging over several orders of magnitude. Because fatty acid derivatives and steroids are endogenous substrates for the P450 enzymes, drugs may interfere with the generation of functional cellular lipids. The functional significance of high-affinity binding of drugs to the oxygenases may, on the one hand, be minimal and reflect extraneous or trivial drug–protein interactions. On the other hand, the drug–P450 union may in other cases mediate the major pharmacological response.Key words: cytochrome P450, radioligand binding, microsomes, sigma receptor, antiestrogen receptor.

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Lešnik, Samo, Éva Bertalan, Urban Bren, and Ana-Nicoleta Bondar. "Opioid Receptors and Protonation-Coupled Binding of Opioid Drugs." International Journal of Molecular Sciences 22, no. 24 (December 12, 2021): 13353. http://dx.doi.org/10.3390/ijms222413353.

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Opioid receptors are G-protein-coupled receptors (GPCRs) part of cell signaling paths of direct interest to treat pain. Pain may associate with inflamed tissue characterized by acidic pH. The potentially low pH at tissue targeted by opioid drugs in pain management could impact drug binding to the opioid receptor, because opioid drugs typically have a protonated amino group that contributes to receptor binding, and the functioning of GPCRs may involve protonation change. In this review, we discuss the relationship between structure, function, and dynamics of opioid receptors from the perspective of the usefulness of computational studies to evaluate protonation-coupled opioid-receptor interactions.

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Wu, Yan-ran, Jia-qin Tang, Wan-nian Zhang, Chun-lin Zhuang, and Ying Shi. "Rational drug design of CB2 receptor ligands: from 2012 to 2021." RSC Advances 12, no. 54 (2022): 35242–59. http://dx.doi.org/10.1039/d2ra05661e.

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Siembida, Jakub, and Kaja Karakuła. "GHB receptors - a new trend in psychopharmacology?" Current Problems of Psychiatry 19, no. 4 (December 1, 2018): 285–98. http://dx.doi.org/10.2478/cpp-2018-0023.

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Abstract Introduction: Gamma-hydroxybutyric acid (GHB) is commonly known as a recreation drug or the so-called “date rape drug”. It is also used in medicine to treat narcolepsy and alcohol addiction. GHB has an affinity for two types of receptors: GABAB and the relatively recently discovered GHB receptors. GHB receptors were first cloned in 2003 in mice and then in 2007 in humans. So far, evidence has been presented for their impact on dopaminergic transmission, which may imply that they play a role in the pathogenesis of diseases such as schizophrenia. At the same time, it has been demonstrated that benzamide antipsychotic drugs have an affinity for GHB receptors, which is why it is postulated that some of the effects of these drugs may result precisely from this affinity. Aim: The study presents the current state of knowledge about GHB receptors and their potential role in the pathogenesis of schizophrenia, and discusses drugs which show an affinity for this receptor. Material and method: The literature review was based on a search of articles indexed between 1965 and 2018 in Medline, Google Scholar, ScienceDirect and Research Gate databases. The following search terms were used: GHB receptor, GHB, sulpiride, and amisulpride. Result and discussion: 1. It is possible that GHB receptors are involved in the pathogenesis of schizophrenia, although more research is needed in this area. 2. Part of the effects of some benzamide antipsychotic drugs (such as amisulpride) may be due to their affinity for GHB receptors.

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Saxena, Pramod R., and Michel D. Ferrari. "From Serotonin Receptor Classification to the Antimigraine Drug Sumatriptan." Cephalalgia 12, no. 4 (August 1992): 187–96. http://dx.doi.org/10.1046/j.1468-2982.1992.1204187.x.

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After the synthetic serotonin 5-hydroxytryptamine (5-HT) became available in the early 1950s, attempts were soon under way to study the nature of 5-HT receptors. Using the guinea-pig isolated ileum, Gaddum and Picarelli (1957) suggested that 5-HT-induced contractions were mediated by a morphine-sensitive “M” receptor located on the parasympathetic ganglion and a dibenzyline-sensitive “D” receptor located on the smooth muscle. Though this classification was used during the next three decades, it was realized that some effects of serotonin, for example vasoconstriction within the carotid vascular bed, were not mediated by either “M” or “D” receptors. When radioligand binding studies led to the identification of 5-HT1 and 5-HT2 “receptors” in the rat brain membranes, it became increasingly apparent that the two receptor classifications were not identical. Thus, a new framework for serotonin receptor nomenclature and classification was proposed: 5-HT 1 -like (5-HT 1), 5-HT 2 (formerly “D”) and 5-HT 3 (formerly “M”) receptors. At the present time, several subtypes of 5-HT 1 receptors as well as a 5-HT 4 receptor are also recognized. As the serotonin receptor classification was emerging to indicate that carotid vasoconstriction by serotonin is mediated by a subtype of 5-HT 1 receptors, on the migraine front it was being suggested that the disease is associated with vasodilatation within the cranial extracerebral circulation and deranged serotonin metabolism and that certain antimigraine drugs caused a selective carotid vasoconstriction, probably via serotonin receptors. Therefore, Humphrey and colleagues conceived that synthesis of serotonin derivatives may lead to a compound that would elicit highly selective carotid vasoconstriction and abort migraine attacks. Indeed, via the synthesis of 5-carboxamidotryptamine and AH25086, sumatriptan was designed. The drug acts as an agonist at the vasoconstrictor 5-HT 1 receptor subtype and has proved highly effective in the therapy of migraine attacks.

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Ashfaq, Muhammad, S. Mobasher Ali Abid, Khalid Rauf, Yasser Msa Alkahraman, Muhammad Zeeshan Haroon, Fawad Ahmad, Saima Ikram, and Jamshaid Ahmad. "Potential Role of Proton Pump Inhibitors Against Human DRD2 Receptor in Drug Induced Hyperprolactinemia." Revista de Chimie 71, no. 10 (November 3, 2020): 182–92. http://dx.doi.org/10.37358/rc.20.10.8362.

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Dopamine is a catecholamine neurotransmitter that control several important functions via different dopamine receptors(D1-D5). The Dopamine (DRD2) receptor and other D2 family receptors (D3 and D4) are predominantly involved in the inhibitory activities. One vital role of dopamine receptors is its involvement in the endocrine regulations including the hormone synthesis and their secretion. The regulation of prolactin hormone is mainly controlled through DRD2 receptors. Blocking the delivery of dopamine at these DRD2 receptors will cause an increase in serum prolactin levels. PPI�s are among the widely prescribed medications used for multiple gastric hypersecretory disorders and are shown to cause increase in serum prolactin level. This study focuses on computational methods to test PPIs interaction with dopamine D2 receptor through molecular docking & dynamics studies. The 3D structure of protein and the drugs were downloaded from PDB and PubChem databases. Protein and ligands were prepared followed by molecular docking. Complexes with best docking poses were then proceeded towards MD simulations of 60 ns. Results were then analyzed. This study confirmed that there is prospective affinity between proton pump inhibitors and dopamine D2 receptor, and dynamically stable complexes are formed after drug-receptor binding. MD simulations results confirmed the binding affinity between PPIs and Dopamine D2 receptor, concluding that the use of PPIs may be involved in drug induced hyperprolactinemia and other related effects.

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Thambidurai, Yuvarani, Sudarsanam Durairaj, Siddhardha Solosan S, Sewali Ghosh, and Habeeb Shaik Mohideen. "Binding Potential of Dysidea Herbacea Derived Small Molecules to Breast Cancer Implicating Targets Estrogen and Epidermal Growth Factor Receptors." Biomedical and Pharmacology Journal 14, no. 01 (March 28, 2021): 391–402. http://dx.doi.org/10.13005/bpj/2139.

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Identifying new targets and new drugs has always been a daunting task, especially in cancer research. This studyexamines the binding interaction and the drug-likeness properties of small molecules derived from marine sponge Dysideaherbacea to breast cancer receptors: epidermal growth factor receptor and estrogen receptor. The receptor’s interaction with the ligand was evaluated using the Schrodinger Glide package, and affinities were assessed based on the glide score. Ligand molecules that have higher binding affinity were evaluated further for their ADMET properties using Molinspiration.We found multiple ligands binding to these targets; however, Pyridine 3 carboxyamidewas found to have binding affinity to both the receptors. Compared to the other small molecules,further simulation studies could be taken up to ascertain its structural dynamics and ensuing in-vitro experiments that could prove growth inhibition of breast cancer cells.

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Dragan, Paulina, Kavita Joshi, Alessandro Atzei, and Dorota Latek. "Keras/TensorFlow in Drug Design for Immunity Disorders." International Journal of Molecular Sciences 24, no. 19 (October 9, 2023): 15009. http://dx.doi.org/10.3390/ijms241915009.

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Homeostasis of the host immune system is regulated by white blood cells with a variety of cell surface receptors for cytokines. Chemotactic cytokines (chemokines) activate their receptors to evoke the chemotaxis of immune cells in homeostatic migrations or inflammatory conditions towards inflamed tissue or pathogens. Dysregulation of the immune system leading to disorders such as allergies, autoimmune diseases, or cancer requires efficient, fast-acting drugs to minimize the long-term effects of chronic inflammation. Here, we performed structure-based virtual screening (SBVS) assisted by the Keras/TensorFlow neural network (NN) to find novel compound scaffolds acting on three chemokine receptors: CCR2, CCR3, and one CXC receptor, CXCR3. Keras/TensorFlow NN was used here not as a typically used binary classifier but as an efficient multi-class classifier that can discard not only inactive compounds but also low- or medium-activity compounds. Several compounds proposed by SBVS and NN were tested in 100 ns all-atom molecular dynamics simulations to confirm their binding affinity. To improve the basic binding affinity of the compounds, new chemical modifications were proposed. The modified compounds were compared with known antagonists of these three chemokine receptors. Known CXCR3 compounds were among the top predicted compounds; thus, the benefits of using Keras/TensorFlow in drug discovery have been shown in addition to structure-based approaches. Furthermore, we showed that Keras/TensorFlow NN can accurately predict the receptor subtype selectivity of compounds, for which SBVS often fails. We cross-tested chemokine receptor datasets retrieved from ChEMBL and curated datasets for cannabinoid receptors. The NN model trained on the cannabinoid receptor datasets retrieved from ChEMBL was the most accurate in the receptor subtype selectivity prediction. Among NN models trained on the chemokine receptor datasets, the CXCR3 model showed the highest accuracy in differentiating the receptor subtype for a given compound dataset.

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Mailavaram, Raghu P., Omar H. A. Al-Attraqchi, Supratik Kar, and Shinjita Ghosh. "Current Status in the Design and Development of Agonists and Antagonists of Adenosine A3 Receptor as Potential Therapeutic Agents." Current Pharmaceutical Design 25, no. 25 (October 3, 2019): 2772–87. http://dx.doi.org/10.2174/1381612825666190716114056.

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Adenosine receptors (ARs) belongs to the family of G-protein coupled receptors (GPCR) that are responsible for the modulation of a wide variety of physiological functions. The ARs are also implicated in many diseases such as cancer, arthritis, cardiovascular and renal diseases. The adenosine A3 receptor (A3AR) has emerged as a potential drug target for the progress of new and effective therapeutic agents for the treatment of various pathological conditions. This receptor’s involvement in many diseases and its validity as a target has been established by many studies. Both agonists and antagonists of A3AR have been extensively investigated in the last decade with the goal of developing novel drugs for treating diseases related to immune disorders, inflammation, cancer, and others. In this review, we shall focus on the medicinal chemistry of A3AR ligands, exploring the diverse chemical classes that have been projected as future leading drug candidates. Also, the recent advances in the therapeuetic applications of A3AR ligands are highlighted.

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Liu, Samuel, Preston J. Anderson, Sudarshan Rajagopal, Robert J. Lefkowitz, and Howard A. Rockman. "G Protein-Coupled Receptors: A Century of Research and Discovery." Circulation Research 135, no. 1 (June 21, 2024): 174–97. http://dx.doi.org/10.1161/circresaha.124.323067.

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GPCRs (G protein-coupled receptors), also known as 7 transmembrane domain receptors, are the largest receptor family in the human genome, with ≈800 members. GPCRs regulate nearly every aspect of human physiology and disease, thus serving as important drug targets in cardiovascular disease. Sharing a conserved structure comprised of 7 transmembrane α-helices, GPCRs couple to heterotrimeric G-proteins, GPCR kinases, and β-arrestins, promoting downstream signaling through second messengers and other intracellular signaling pathways. GPCR drug development has led to important cardiovascular therapies, such as antagonists of β-adrenergic and angiotensin II receptors for heart failure and hypertension, and agonists of the glucagon-like peptide-1 receptor for reducing adverse cardiovascular events and other emerging indications. There continues to be a major interest in GPCR drug development in cardiovascular and cardiometabolic disease, driven by advances in GPCR mechanistic studies and structure-based drug design. This review recounts the rich history of GPCR research, including the current state of clinically used GPCR drugs, and highlights newly discovered aspects of GPCR biology and promising directions for future investigation. As additional mechanisms for regulating GPCR signaling are uncovered, new strategies for targeting these ubiquitous receptors hold tremendous promise for the field of cardiovascular medicine.

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Reid, Ke Zhang, Brendan Matthew Lemezis, Tien-Chi Hou, and Rong Chen. "Epigenetic Modulation of Opioid Receptors by Drugs of Abuse." International Journal of Molecular Sciences 23, no. 19 (October 5, 2022): 11804. http://dx.doi.org/10.3390/ijms231911804.

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Chronic exposure to drugs of abuse produces profound changes in gene expression and neural activity associated with drug-seeking and taking behavior. Dysregulation of opioid receptor gene expression is commonly observed across a variety of abused substances including opioids, cocaine, and alcohol. Early studies in cultured cells showed that the spatial and temporal gene expression of opioid receptors are regulated by epigenetic mechanisms including DNA and histone modifications and non-coding RNAs. Accumulating evidence indicate that drugs of abuse can modulate opioid receptor gene expression by targeting various epigenetic regulatory networks. Based on current cellular and animal models of substance use disorder and clinical evidence, this review summarizes how chronic drug exposure alters the gene expression of mu, delta, kappa, and nociceptin receptors via DNA and histone modifications. The influence of drugs of abuse on epigenetic modulators, such as non-coding RNAs and transcription factors, is also presented. Finally, the therapeutic potential of manipulating epigenetic processes as an avenue to treat substance use disorder is discussed.

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Gras, J. "Cenobamate. Drug acting on GABAA receptors, Antiepileptic drug." Drugs of the Future 44, no. 8 (2019): 617. http://dx.doi.org/10.1358/dof.2019.44.8.3030644.

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Andijani, Yusra Saleh. "G Protein-coupled Receptors: One of the Most Important Drug Discovery Targets." Journal of King Abdulaziz University - Medical Sciences 25, no. 2 (December 31, 2018): 27–35. http://dx.doi.org/10.4197/med.25-2.3.

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G protein-coupled receptors are considered the most widely investigated drug discovery targets. They are the largest family of receptors with almost 800 genes in humans. Different types of ligands can activate these receptors, such as catecholamines, nucleotides, lipids, and gut microbiota, where some ligands could be bitopic. Nevertheless, some receptors have internal ligands bound to them. Activated G protein-coupled receptors have complex signaling pathways that are involved in almost all bodily functions. Furthermore, they constitute a large percentage of Food and Drug Administration marketed drugs and global share of drugs, in addition to a great proportion of drugs currently in clinical trials targeting these receptors. The approved G protein-coupled receptors targeted drugs and potential drugs are involved in the management of many diseases including cancer, inflammatory diseases, diabetes mellitus, hypertension, obesity, pain, and diseases of the central nervous system. Only 10% of G protein-coupled receptors are targeted. Different pharmacological approaches have been considered in drug discovery of these receptors including polypharmacology, allosteric modulators, biased agonism, tethered agonism, and pharmacogenomics. Advances in the technologies are promising to help in the discovery of new targets. The review's aim is to discuss the importance of G protein-coupled receptors as drug discovery targets.

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Johnston, Graham, Mary Chebib, Jane Hanrahan, and Kenneth Mewett. "GABAC Receptors as Drug Targets." Current Drug Target -CNS & Neurological Disorders 2, no. 4 (August 1, 2003): 260–68. http://dx.doi.org/10.2174/1568007033482805.

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Rossmann, Michael G. "Viral receptors and drug design." Nature 333, no. 6172 (June 1988): 392–93. http://dx.doi.org/10.1038/333392a0.

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Flower, Rod. "Drug receptors: A long engagement." Nature 415, no. 6872 (February 2002): 587. http://dx.doi.org/10.1038/415587a.

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Hannon, Jason P., Caroline Nunn, Barbara Stolz, Christian Bruns, Gisbert Weckbecker, ian lewis, Thomas Troxler, Konstanze Hurth, and Daniel Hoyer. "Drug Design at Peptide Receptors." Journal of Molecular Neuroscience 18, no. 1-2 (2002): 15–28. http://dx.doi.org/10.1385/jmn:18:1-2:15.

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North, R. Alan, and Michael F. Jarvis. "P2X Receptors as Drug Targets." Molecular Pharmacology 83, no. 4 (December 19, 2012): 759–69. http://dx.doi.org/10.1124/mol.112.083758.

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Olivier, Berend. "SEROTONIN RECEPTORS IN DRUG DISCRIMINATION." Behavioural Pharmacology 10, SUPPLEMENT 1 (August 1999): S68. http://dx.doi.org/10.1097/00008877-199908001-00172.

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Korpi, Esa R., Gerhard Gründer, and Hartmut Lüddens. "Drug interactions at GABAA receptors." Progress in Neurobiology 67, no. 2 (June 2002): 113–59. http://dx.doi.org/10.1016/s0301-0082(02)00013-8.

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Fredholm, Bertil B. "Adenosine receptors as drug targets." Experimental Cell Research 316, no. 8 (May 2010): 1284–88. http://dx.doi.org/10.1016/j.yexcr.2010.02.004.

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Kihara, Yasuyuki, Hirotaka Mizuno, and Jerold Chun. "Lysophospholipid receptors in drug discovery." Experimental Cell Research 333, no. 2 (May 2015): 171–77. http://dx.doi.org/10.1016/j.yexcr.2014.11.020.

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Maack, Thomas. "Cardiovascular receptors as drug targets." Molecular Medicine Today 3, no. 3 (March 1997): 101–2. http://dx.doi.org/10.1016/s1357-4310(97)01007-1.

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Bandoli, Giuliano, Marino Nicolini, Henri Lumbroso, Antonio Grassi, and Giuseppe C. Pappalardo. "Molecular determinants for drug-receptors." Journal of Molecular Structure 160, no. 3-4 (September 1987): 297–309. http://dx.doi.org/10.1016/0022-2860(87)80070-4.

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Eric Almeida Xavier. "Trazodone and chlorpromazine a proposal treatment for syndrome post-finasteride and syndrome of post-selective serotonin reuptake inhibitors (post-SSRI)." World Journal of Biology Pharmacy and Health Sciences 15, no. 1 (July 30, 2023): 075–60. http://dx.doi.org/10.30574/wjbphs.2023.15.1.0299.

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Erectile dysfunction caused by medications are probably caused by the disconnection of synaptic circuits responsible for linking libido to erection. For instance, it is well known that sexual dysfunction may occur in patients treated with antidepressants like selective serotonin reuptake inhibitors, syndrome known as (post-SSRI). A similar side effect has been also reported during treatment with finasteride, an inhibitor of the enzyme 5alpha-reductase, for androgenetic alopecia. Interestingly, sexual dysfunction persists in both cases after drug discontinuation. Trazodone is a multifunctional drug with hypnotic actions at low doses due to blockade of 5-HT2A receptors, as well as H1 histamine receptors and α1 adrenergic receptors therefore this drug can cause severe priaprism as a side effect and in many cases causing penile necrosis or permanent loss of erectile function. Thus the antipsychotic like chlorpromazine also induce priapism because the alpha receptor occupancy property of those drugs. Therefore we propose that these drugs can restore libido synaptic circuits, and trazodone or antipsychotic drugs such as chlorpromazine can also be a treatment for post-finasteride syndrome and post-SSRI.

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Wenzel, Christoph, Lisa Gödtke, Anne Reichstein, Markus Keiser, Diana Busch, Marek Drozdzik, and Stefan Oswald. "Gene Expression and Protein Abundance of Nuclear Receptors in Human Intestine and Liver: A New Application for Mass Spectrometry-Based Targeted Proteomics." Molecules 27, no. 14 (July 20, 2022): 4629. http://dx.doi.org/10.3390/molecules27144629.

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Background: Unwanted drug-drug interactions (DDIs), as caused by the upregulation of clinically relevant drug metabolizing enzymes and transporter proteins in intestine and liver, have the potential to threaten the therapeutic efficacy and safety of drugs. The molecular mechanism of this undesired but frequently occurring scenario of polypharmacy is based on the activation of nuclear receptors such as the pregnane X receptor (PXR) or the constitutive androstane receptor (CAR) by perpetrator agents such as rifampin, phenytoin or St. John’s wort. However, the expression pattern of nuclear receptors in human intestine and liver remains uncertain, which makes it difficult to predict the extent of potential DDIs. Thus, it was the aim of this study to characterize the gene expression and protein abundance of clinically relevant nuclear receptors, i.e., the aryl hydrocarbon receptor (AhR), CAR, farnesoid X receptor (FXR), glucocorticoid receptor (GR), hepatocyte nuclear factor 4 alpha (HNF4α), PXR and small heterodimer partner (SHP), in the aforementioned organs. Methods: Gene expression analysis was performed by quantitative real-time PCR of jejunal, ileal, colonic and liver samples from eight human subjects. In parallel, a targeted proteomic method was developed and validated in order to determine the respective protein amounts of nuclear receptors in human intestinal and liver samples. The LC-MS/MS method was validated according to the current bioanalytical guidelines and met the criteria regarding linearity (0.1–50 nmol/L), within-day and between-day accuracy and precision, as well as the stability criteria. Results: The developed method was successfully validated and applied to determine the abundance of nuclear receptors in human intestinal and liver samples. Gene expression and protein abundance data demonstrated marked differences in human intestine and liver. On the protein level, only AhR and HNF4α could be detected in gut and liver, which corresponds to their highest gene expression. In transfected cell lines, PXR and CAR could be quantified. Conclusions: The substantially different expression pattern of nuclear receptors in human intestinal and liver tissue may explain the different extent of unwanted DDIs in the dependence on the administration route of drugs.

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Blätter, W., and P. Schoch. "Potential Psychotropic Activity of Phlebotropic Drugs: Weak Interactions with Brain Benzodiazepine Receptors." Phlebology: The Journal of Venous Disease 9, no. 1 (March 1994): 32–36. http://dx.doi.org/10.1177/026835559400900110.

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Background: Epidemiological and psychometric studies have provided evidence that some symptoms of venous disease might reflect a psychosomatic rather than organic disorder. Traditionally, plant extracts are prescribed to alleviate such symptoms. Since benzodiazepines (BZ) and BZ-like compounds are present in various plants, we studied potential interactions of ‘phlebotropic’ drugs with BZ receptors. Methods: Six drug preparations used in phlebology and extracts of hop and valerian were tested for neuronal and mitochondrial BZ receptor binding activity in vitro. In addition, plasma samples of volunteers who ingested phlebotropic drugs for 3 weeks were assayed for the presence of BZ-like activity. Results: All phlebotropic drug preparations interacted weakly with central and/or peripheral BZ receptors in vitro. Their diazepam-equivalent concentrations were, however, too low to be of pharmacological relevance. No binding activity was recovered in the blood of volunteers pretreated with phlebotropic drugs. Conclusion: The positive influence of so-called ‘phlebotropic’ drugs on the subjective symptoms of venous disease is not mediated through BZ receptors.

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Neumann, Joachim, Britt Hofmann, Uwe Kirchhefer, Stefan Dhein, and Ulrich Gergs. "Function and Role of Histamine H1 Receptor in the Mammalian Heart." Pharmaceuticals 16, no. 5 (May 11, 2023): 734. http://dx.doi.org/10.3390/ph16050734.

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Histamine can change the force of cardiac contraction and alter the beating rate in mammals, including humans. However, striking species and regional differences have been observed. Depending on the species and the cardiac region (atrium versus ventricle) studied, the contractile, chronotropic, dromotropic, and bathmotropic effects of histamine vary. Histamine is present and is produced in the mammalian heart. Thus, histamine may exert autocrine or paracrine effects in the mammalian heart. Histamine uses at least four heptahelical receptors: H1, H2, H3 and H4. Depending on the species and region studied, cardiomyocytes express only histamine H1 or only histamine H2 receptors or both. These receptors are not necessarily functional concerning contractility. We have considerable knowledge of the cardiac expression and function of histamine H2 receptors. In contrast, we have a poor understanding of the cardiac role of the histamine H1 receptor. Therefore, we address the structure, signal transduction, and expressional regulation of the histamine H1 receptor with an eye on its cardiac role. We point out signal transduction and the role of the histamine H1 receptor in various animal species. This review aims to identify gaps in our knowledge of cardiac histamine H1 receptors. We highlight where the published research shows disagreements and requires a new approach. Moreover, we show that diseases alter the expression and functional effects of histamine H1 receptors in the heart. We found that antidepressive drugs and neuroleptic drugs might act as antagonists of cardiac histamine H1 receptors, and believe that histamine H1 receptors in the heart might be attractive targets for drug therapy. The authors believe that a better understanding of the role of histamine H1 receptors in the human heart might be clinically relevant for improving drug therapy.

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Dai, Xiaofeng, Erik W. Thompson, and Kostya (Ken) Ostrikov. "Receptor-Mediated Redox Imbalance: An Emerging Clinical Avenue against Aggressive Cancers." Biomolecules 12, no. 12 (December 15, 2022): 1880. http://dx.doi.org/10.3390/biom12121880.

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Cancer cells are more vulnerable to abnormal redox fluctuations due to their imbalanced antioxidant system, where cell surface receptors sense stress and trigger intracellular signal relay. As canonical targets of many targeted therapies, cell receptors sensitize the cells to specific drugs. On the other hand, cell target mutations are commonly associated with drug resistance. Thus, exploring effective therapeutics targeting diverse cell receptors may open new clinical avenues against aggressive cancers. This paper uses focused case studies to reveal the intrinsic relationship between the cell receptors of different categories and the primary cancer hallmarks that are associated with the responses to external or internal redox perturbations. Cold atmospheric plasma (CAP) is examined as a promising redox modulation medium and highly selective anti-cancer therapeutic modality featuring dynamically varying receptor targets and minimized drug resistance against aggressive cancers.

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Sharma, Geeta, and Sukumar Vijayaraghavan. "Nicotinic Receptors: Role in Addiction and Other Disorders of the Brain." Substance Abuse: Research and Treatment 1 (January 2008): 117822180800100. http://dx.doi.org/10.1177/117822180800100005.

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Nicotine, the addictive component of cigarette smoke has profound effects on the brain. Activation of its receptors by nicotine has complex consequences for network activity throughout the brain, potentially contributing to the addictive property of the drug. Nicotinic receptors have been implicated in psychiatric illnesses like schizophrenia and are also neuroprotective, potentially beneficial for neurodegenerative diseases. These effects of nicotine serve to emphasize the multifarious roles the drug, acting through multiple nicotinic acetylcholine receptor subtypes. The findings also remind us of the complexity of signaling mechanisms and stress the risks of unintended consequences of drugs designed to combat nicotine addiction.

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Eberle, Stefanie Alexandra, and Martin Gustavsson. "A Scintillation Proximity Assay for Real-Time Kinetic Analysis of Chemokine–Chemokine Receptor Interactions." Cells 11, no. 8 (April 13, 2022): 1317. http://dx.doi.org/10.3390/cells11081317.

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Chemokine receptors are extensively involved in a broad range of physiological and pathological processes, making them attractive drug targets. However, despite considerable efforts, there are very few approved drugs targeting this class of seven transmembrane domain receptors to date. In recent years, the importance of including binding kinetics in drug discovery campaigns was emphasized. Therefore, kinetic insight into chemokine–chemokine receptor interactions could help to address this issue. Moreover, it could additionally deepen our understanding of the selectivity and promiscuity of the chemokine–chemokine receptor network. Here, we describe the application, optimization and validation of a homogenous Scintillation Proximity Assay (SPA) for real-time kinetic profiling of chemokine–chemokine receptor interactions on the example of ACKR3 and CXCL12. The principle of the SPA is the detection of radioligand binding to receptors reconstituted into nanodiscs by scintillation light. No receptor modifications are required. The nanodiscs provide a native-like environment for receptors and allow for full control over bilayer composition and size. The continuous assay format enables the monitoring of binding reactions in real-time, and directly accounts for non-specific binding and potential artefacts. Minor adaptations additionally facilitate the determination of equilibrium binding metrics, making the assay a versatile tool for the study of receptor–ligand interactions.

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Gachet, Christian. "ADP Receptors of Platelets and their Inhibition." Thrombosis and Haemostasis 86, no. 07 (2001): 222–32. http://dx.doi.org/10.1055/s-0037-1616220.

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SummaryADP plays a crucial role in haemostasis and thrombosis and its receptors are potential targets for antithrombotic drugs. Two G-protein coupled P2 receptors contribute to platelet aggregation: the P2Y1 receptor initiates aggregation through mobilisation of calcium stores, while the more recently identified P2Y12 receptor coupled to adenylyl cyclase inhibition is essential for a full aggregation response to ADP and the stabilisation of aggregates. The latter is defective in certain patients with a selective congenital deficiency of aggregation to ADP. It is also the target of the antithrombotic drug clopidogrel and of ATP analogues and other compounds currently under evaluation. In addition, the P2X1 ionotropic receptor is present in platelets but its role is not yet completely known. Studies in P2Y1 knock-out mice and experimental thrombosis models using selective P2Y1 antagonists have shown that the P2Y1 receptor, like the P2Y12 receptor, is a potential target for new antithrombotic drugs.

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Kaur, Tarnjot, Jyoti Upadhyay, Sudeep Pukale, Ashish Mathur, and Mohd Nazam Ansari. "Investigation of Trends in the Research on Transferrin Receptor-Mediated Drug Delivery via a Bibliometric and Thematic Analysis." Pharmaceutics 14, no. 12 (November 23, 2022): 2574. http://dx.doi.org/10.3390/pharmaceutics14122574.

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This study systematically reviews and characterizes the existing literature on transferrin/transferrin receptor-mediated drug delivery. Transferrin is an iron-binding protein. It can be used as a ligand to deliver various proteins, genes, ions, and drugs to the target site via transferrin receptors for therapeutic or diagnostic purposes via transferrin receptors. This study is based on a cross-sectional bibliometric analysis of 583 papers limited to the subject areas of pharmacology, toxicology, and pharmaceutics as extracted from the Scopus database in mid-September 2022. The data were analyzed, and we carried out a performance analysis and science mapping. There was a significant increase in research from 2018 onward. The countries that contributed the most were the USA and China, and most of the existing research was found to be from single-country publications. Research studies on transferrin/transferrin receptor-mediated drug delivery focus on drug delivery across the blood–brain barrier in the form of nanoparticles. The thematic analysis revealed four themes: transferrin/transferrin receptor-mediated drug delivery to the brain, cancer cells, gene therapy, nanoparticles, and liposomes as drug delivery systems. This study is relevant to academics, practitioners, and decision makers interested in targeted and site-specific drug delivery.

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Smolinska, Sylwia, Darío Antolín-Amérigo, and Florin-Dan Popescu. "Bradykinin Metabolism and Drug-Induced Angioedema." International Journal of Molecular Sciences 24, no. 14 (July 19, 2023): 11649. http://dx.doi.org/10.3390/ijms241411649.

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Bradykinin (BK) metabolism and its receptors play a central role in drug-induced angioedema (AE) without urticaria through increased vascular permeability. Many cardiovascular and diabetic drugs may cause BK-mediated AE. Angiotensin-converting enzyme inhibitors (ACEIs) and neprilysin inhibitors impair BK catabolism. Dipeptidyl peptidase-IV (DPP-IV) inhibitors reduce the breakdown of BK and substance P (SP). Moreover, angiotensin receptor blockers, thrombolytic agents, and statins may also induce BK-mediated AE. Understanding pathophysiological mechanisms is crucial for preventing and treating drug-induced AE.

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Anil, Anisha Sara, Sonale S, and N. Venkateswaramurthy. "Cardiotoxic Drugs: An Insight into its Pathologic Mechanisms." Biosciences Biotechnology Research Asia 21, no. 1 (March 30, 2024): 45–56. http://dx.doi.org/10.13005/bbra/3201.

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ABSTRACT: Cardiovascular diseases are among the major causes of mortality and morbidity worldwide Cardiotoxicity due to drugs is a common and significant adverse effect on cardiovascular health, acting through multifactorial pathological mechanisms. Drug-induced cardiotoxicity limits the use and further development of certain drugs. Keeping this in mind, this review discusses the crucial drug-receptor interactions involved in cardiotoxicity induced by some drugs such as cocaine, trastuzumab, isoproterenol, antidiabetic drugs like pioglitazone, theophylline, ergotamine, methysergide, anthracyclines, fluoropyrimidines, cisplatin, NSAIDs, and antiviral agents. The key receptors involved in the pathological mechanism behind the cardiotoxicity induced by these drugs are discussed, aiming to provide in-depth knowledge for future drug discovery and prevention of drug-induced cardiotoxicity.

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Journal articles on the topic 'Drug receptors'

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