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Статті в журналах з теми "Dual inhibitors"
Sipos, Ádám, Eszter Szennyes, Nikolett Éva Hajnal, Sándor Kun, Katalin E. Szabó, Karen Uray, László Somsák, Tibor Docsa, and Éva Bokor. "Dual-Target Compounds against Type 2 Diabetes Mellitus: Proof of Concept for Sodium Dependent Glucose Transporter (SGLT) and Glycogen Phosphorylase (GP) Inhibitors." Pharmaceuticals 14, no. 4 (April 15, 2021): 364. http://dx.doi.org/10.3390/ph14040364.
Повний текст джерелаGesinski, Dayna, and Sonali Kurup. "Abstract 5337: Design, synthesis and evaluation of dual-targeted mEGFR and AURK inhibitors as anticancer agents." Cancer Research 83, no. 7_Supplement (April 4, 2023): 5337. http://dx.doi.org/10.1158/1538-7445.am2023-5337.
Повний текст джерелаKim, Min-Jeong, Sarita Pandit, and Jun-Goo Jee. "Discovery of Kinase and Carbonic Anhydrase Dual Inhibitors by Machine Learning Classification and Experiments." Pharmaceuticals 15, no. 2 (February 16, 2022): 236. http://dx.doi.org/10.3390/ph15020236.
Повний текст джерелаBošković, Jelena, Vladimir Dobričić, Marija Mihajlović, Jelena Kotur-Stevuljević, and Olivera Čudina. "Synthesis, Evaluation of Enzyme Inhibition and Redox Properties of Potential Dual COX-2 and 5-LOX Inhibitors." Pharmaceuticals 16, no. 4 (April 6, 2023): 549. http://dx.doi.org/10.3390/ph16040549.
Повний текст джерелаWang, Q. May, Robert B. Johnson, Louis N. Jungheim, Jeffrey D. Cohen, and Elcira C. Villarreal. "Dual Inhibition of Human Rhinovirus 2A and 3C Proteases by Homophthalimides." Antimicrobial Agents and Chemotherapy 42, no. 4 (April 1, 1998): 916–20. http://dx.doi.org/10.1128/aac.42.4.916.
Повний текст джерелаLu, Haiying, Lan Bai, Yanping Zhou, Yongping Lu, Zhongliang Jiang, and Jianyou Shi. "Recent Study of Dual HDAC/PARP Inhibitor for the Treatment of Tumor." Current Topics in Medicinal Chemistry 19, no. 12 (July 30, 2019): 1041–50. http://dx.doi.org/10.2174/1568026619666190603092407.
Повний текст джерелаWen, Hui, Wen Qin, Guangzhong Yang, and Yanshen Guo. "Design and Synthesis of Arylamidine Derivatives as Serotonin/Norepinephrine Dual Reuptake Inhibitors." Molecules 24, no. 3 (January 30, 2019): 497. http://dx.doi.org/10.3390/molecules24030497.
Повний текст джерелаVest, Rebekah S., Kurtis D. Davies, Heather O'Leary, J. David Port, and K. Ulrich Bayer. "Dual Mechanism of a Natural CaMKII Inhibitor." Molecular Biology of the Cell 18, no. 12 (December 2007): 5024–33. http://dx.doi.org/10.1091/mbc.e07-02-0185.
Повний текст джерелаLambert, Que T., Stuart W. Ember, Muhammad Ayaz, Harshani R. Lawrence, Norbert Berndt, Steven Gunawan, Nicholas J. Lawrence, Ernst Schönbrunn, and Gary W. Reuther. "Single Molecule Dual JAK2-BET Inhibition As an MPN Therapeutic." Blood 126, no. 23 (December 3, 2015): 2826. http://dx.doi.org/10.1182/blood.v126.23.2826.2826.
Повний текст джерелаDyer, Richard D., and David T. Connor. "Dual Inhibitors Of Prostaglandin And Leukotriene Biosynthesis." Current Pharmaceutical Design 3, no. 5 (1997): 463–72. http://dx.doi.org/10.2174/138161280305221010095741.
Повний текст джерелаДисертації з теми "Dual inhibitors"
Meschini, Elisa. "Purine-based dual inhibitors of CDK2 and CDK7." Thesis, University of Newcastle Upon Tyne, 2011. http://hdl.handle.net/10443/1363.
Повний текст джерелаGreen, Ian. "The biology of novel dual histone methyltransferase inhibitors." Thesis, Imperial College London, 2015. http://hdl.handle.net/10044/1/25763.
Повний текст джерелаApsel, Beth. "Dual-specificity inhibitors of lipid and protein kinases." Diss., Search in ProQuest Dissertations & Theses. UC Only, 2008. http://gateway.proquest.com/openurl?url_ver=Z39.88-2004&rft_val_fmt=info:ofi/fmt:kev:mtx:dissertation&res_dat=xri:pqdiss&rft_dat=xri:pqdiss:3311357.
Повний текст джерелаRen, Baiping. "Molecular Design and Discovery of Single and Dual Inhibitors of Amyloid Peptides." University of Akron / OhioLINK, 2019. http://rave.ohiolink.edu/etdc/view?acc_num=akron1555257099229697.
Повний текст джерелаWong, Jacky Sui Ki. "The Evaluation of Dual PI3K/mTOR Inhibitors as a Superior Alternative to mTOR Inhibitors in Pre-B Acute Lymphoblastic Leukaemia." Thesis, The University of Sydney, 2014. http://hdl.handle.net/2123/13644.
Повний текст джерелаFraser, Sasha. "Development of Dual-Pathway Inhibitors of Raf/MEK/ERK and PI3K/Akt Signaling Pathways." VCU Scholars Compass, 2011. http://scholarscompass.vcu.edu/etd/2619.
Повний текст джерелаSteinemann, Gustav [Verfasser]. "Charakterisierung der Wirkmechanismen des neuartigen, dual wirksamen HDAC-Inhibitors „Animacroxam“ am Beispiel testikulärer Keimzelltumore / Gustav Steinemann." Berlin : Medizinische Fakultät Charité - Universitätsmedizin Berlin, 2021. http://d-nb.info/1234984474/34.
Повний текст джерелаTamhaev, Rasoul. "Conception, synthèse et caractérisation de dérivés diaryl éthers comme nouveaux inhibiteurs directs de la protéine InhA de Mycobacterium tuberculosis." Electronic Thesis or Diss., Université de Toulouse (2023-....), 2024. http://thesesups.ups-tlse.fr/6088/.
Повний текст джерелаTuberculosis, despite being a very ancient disease, remains one of the major causes of mortality due to a single infectious agent. In 2021, 10 million people contracted the disease and 1.5 million deaths were directly attributable to it. Despite the availability of a variety of antibiotics, few of them prove effective against the pathogen responsible for tuberculosis, Mycobacterium tuberculosis. This ineffectiveness is primarily due to the impermeable nature of the mycobacterial cell envelope, composed mainly of mycolic acids. Isoniazid, the most widely used first-line antitubercular drug, targets the biosynthesis of these mycolic acids through the protein InhA. Isoniazid acts as a pro-drug requiring activation by the protein KatG. However, the emergence of resistance during the activation stage of isoniazid necessitates the development of direct inhibitors of InhA. The work carried out during this thesis aimed to develop new direct inhibitors of InhA. These inhibitors were designed basedon the structure of a diaryl ether motif, known for its ability to inhibit the enzyme. Dynamic combinatorial chemistry combined with X-ray crystallography was used as a fragment screening method to discover new inhibitors. Three adducts, visualized directly within the active site of the protein, were characterized and showed interactions with the major portal of the protein. In another project, a new family of diaryl ethers with three pharmacophores was designed to fully occupy the substrate binding site. One of the synthesized molecules exhibited sub-micromolar inhibitory activity against InhA. The structure of the corresponding complex was resolved by X-ray crystallography, highlighting a wider opening of one of the protein's regions, called the minor portal. Finally, multi-target approaches, targeting both InhA and the dehydratase complex HadABC of the FAS II system, were also developed during this thesis. Several dual molecules were produced, showing inhibition of InhA activity in the nanomolar range. These molecules also demonstrated inhibition of the growth of different mycobacterial strains
Yule, Ian Andrew. "Design, synthesis and biological evaluation of novel, dual targeting inhibitors of bacterial DNA gyrase and topoisomerase IV." Thesis, University of Leeds, 2012. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.713881.
Повний текст джерелаFoka, Germaine Boulenoue. "Synthesis and evaluation of novel coumarin-donepezil derivatives as dual acting monoamine oxidase B and cholinesterase in Alzheimer's disease." University of the Western Cape, 2016. http://hdl.handle.net/11394/5549.
Повний текст джерелаAlzheimer's disease is a progressive neurodegenerative disease characterised by low acetylcholine (ACh) levels in the hippocampus and cortex of the brain, causing symptoms like progressive memory loss, decline in language skills and other cognitive impairments to occur. The hallmarks of AD include the presence of extracellular insoluble amyloid beta plaques, intracellular neurofibrillary tangles, and the decrease in ACh concentration. The pathophysiology of AD is not well understood, however, acetylcholinesterase (AChE), butyrylcholinesterase (BuChE) and monoamine oxidases (MAO) are conspicuous role players in AD pathogenesis. Based on the cholinergic hypothesis, the AChE inhibitor donepezil was developed and has been used effectively clinically in the management of AD, with minimal side effects. Studies regarding the binding interactions of donepezil with AChE has shown that the benzyl-piperidine moiety of this compound shows substantial binding interactions at the CAS site of AChE where it blocks AChE activity. Coumarin is a compound of natural source that has shown some MAO inhibitory activity. Further studies done to clarify the potential of coumarin as a drug against AD has shown that coumarin has the capacity to bind at the PAS site of AChE, thus giving it the potential to prevent AChE induced amyloid plaque formation. Due to the multifactorial nature of AD, the drugs in the market show limited therapeutic benefits and are mainly for symptomatic relief. In order to address this limitation in AD treatment, researchers are exploring the possibility of designing a multi-target-directed-ligand (MTDL). The aim of this study was to synthesise a series of compounds out of pharmacophoric groups of donepezil and coumarin that will be able to inhibit both cholinesterases and MAO B. Four series of 5 compounds per series were synthesised. The first series of compounds consisted of the coumarin moiety to which a 1,4-dibromo benzene moiety was attached. The second series represented the coumarin moiety to which a piperidine (donepezil moiety shown to confer cholinesterase inhibitory property) was attached. The third series represented the coumarin moiety to which bromobenzyl-piperazine was attached and in the last series were compounds similar in structure to series 1 with an unsubstituted benzyl moiety as opposed to the dibromobenzyl moiety. Prior to the synthesis, molecular modelling was conducted in order to have an idea of the binding capacity of the compounds to MAO A and B and cholinesterases. In vitro biological evaluation of the compounds was done and used to determine the IC₅₀ values of the compounds. Nineteen compounds were synthesised and purified successfully as shown by their NMR, MS and IR spectra. The compounds to which dual inhibitory activity was conferred were those in series 2 and 3, of which series 2 showed the best overall inhibitory activity with IC₅₀ values within the low μM range. The compound with the best overall activity was Cp 9. Molecular modelling of Cp 9 showed that the coumarin core was located in the PAS region of AChE while the benzyl-piperidine moiety was situated in the CAS region of the enzyme. This compound orientation demonstrates the potential of Cp 9 to inhibit AChE induced amyloid beta plaque formation. Cp 9 showed no inhibitory activity towards MAO A, but showed good inhibitory activity towards MAO B with an IC₅₀ value of 0.30 μM. Its inhibitory activity towards cholinesterases also fell within the low μM range (AChE IC50 = 9.1 μM and BuChE IC₅₀ = 5.9 μM). From the results, it can be concluded that Cp 9 was able to inhibit both cholinesterase and MAO B catalytic activities at low μM concentrations. This thus means that our novel compound will not only increase ACh levels in the brain thus improving cognitive activity, but it will also have neuroprotective effect from its MAO B inhibitory property and also potentially slow down amyloid plaque formation due to AChE activity.
National Research Foundation (NRF)
Книги з теми "Dual inhibitors"
Shepherd, Angela J., and Juliet M. Mckee. Osteoporosis. Oxford University Press, 2018. http://dx.doi.org/10.1093/med/9780190466268.003.0015.
Повний текст джерелаKuwabara, Satoshi. Neuromuscular junction disorders. Oxford University Press, 2015. http://dx.doi.org/10.1093/med/9780199658602.003.0014.
Повний текст джерелаFerro, Charles J., and Khai Ping Ng. Recommendations for management of high renal risk chronic kidney disease. Edited by David J. Goldsmith. Oxford University Press, 2015. http://dx.doi.org/10.1093/med/9780199592548.003.0099.
Повний текст джерелаCastellanos, Madeleine M. Female Sexual Biochemistry (DRAFT). Edited by Madeleine M. Castellanos. Oxford University Press, 2018. http://dx.doi.org/10.1093/med/9780190225889.003.0001.
Повний текст джерелаBueno, Héctor, and José A. Barrabés. Non-ST-segment elevation acute coronary syndromes. Oxford University Press, 2015. http://dx.doi.org/10.1093/med/9780199687039.003.0046.
Повний текст джерелаBueno, Héctor, and José A. Barrabés. Non-ST-segment elevation acute coronary syndromes. Oxford University Press, 2016. http://dx.doi.org/10.1093/med/9780199687039.003.0046_update_001.
Повний текст джерелаBueno, Héctor, and José A. Barrabés. Non-ST-segment elevation acute coronary syndromes. Oxford University Press, 2018. http://dx.doi.org/10.1093/med/9780199687039.003.0046_update_002.
Повний текст джерелаPirani, Tasneem, and Tony Rahman. Diagnosis and management of upper gastrointestinal haemorrhage in the critically ill. Oxford University Press, 2016. http://dx.doi.org/10.1093/med/9780199600830.003.0177.
Повний текст джерелаЧастини книг з теми "Dual inhibitors"
Fink, Cynthia A. "Dual inhibitors of angiotensin converting enzyme and neutral endopeptidase." In ACE Inhibitors, 155–62. Basel: Birkhäuser Basel, 2001. http://dx.doi.org/10.1007/978-3-0348-7579-0_11.
Повний текст джерелаFrye, Leah L., and Deborah A. Leonard. "Dual-Action Inhibitors of Cholesterol Biosynthesis." In ACS Symposium Series, 94–108. Washington, DC: American Chemical Society, 1992. http://dx.doi.org/10.1021/bk-1992-0497.ch009.
Повний текст джерелаTrapencieris, Peteris, Anete Parkova, and Ineta Vendina-Birzniece. "Carbonic Anhydrase Inhibitors with Dual Targeting." In Carbonic Anhydrase as Drug Target, 163–78. Cham: Springer International Publishing, 2019. http://dx.doi.org/10.1007/978-3-030-12780-0_12.
Повний текст джерелаFong, Alan Yean Yip, and Hwei Sung Ling. "Dual Antiplatelet and Glycoprotein Inhibitors in Emergency PCI." In Primary Angioplasty, 99–108. Singapore: Springer Singapore, 2018. http://dx.doi.org/10.1007/978-981-13-1114-7_8.
Повний текст джерелаAnighoro, Andrew, Luca Pinzi, Giulio Rastelli, and Jürgen Bajorath. "Virtual Screening for Dual Hsp90/B-Raf Inhibitors." In Methods in Pharmacology and Toxicology, 355–65. New York, NY: Springer New York, 2017. http://dx.doi.org/10.1007/7653_2017_1.
Повний текст джерелаWang, Huan, and Chao Wang. "Peptide-Based Dual HIV and Coronavirus Entry Inhibitors." In Advances in Experimental Medicine and Biology, 87–100. Singapore: Springer Singapore, 2022. http://dx.doi.org/10.1007/978-981-16-8702-0_6.
Повний текст джерелаAlbanell, J. "Dual/Pan-Her Tyrosine Kinase Inhibitors: Focus in Breast Cancer." In New trends in cancer for the 21st century, 329–40. Dordrecht: Springer Netherlands, 2006. http://dx.doi.org/10.1007/978-1-4020-5133-3_25.
Повний текст джерелаKarlsson, Andreas, and Carlos García-echeverría. "Chapter 13. Identification and Optimization of Dual PI3K/mTOR Inhibitors." In Drug Discovery, 206–20. Cambridge: Royal Society of Chemistry, 2012. http://dx.doi.org/10.1039/9781849734912-00206.
Повний текст джерелаSica, Domenic A. "Dual Inhibitors: RAAS Blockers/Combination Therapies: What Do All These Trials Mean?" In Chronic Kidney Disease and Hypertension, 57–68. New York, NY: Springer New York, 2014. http://dx.doi.org/10.1007/978-1-4939-1982-6_6.
Повний текст джерелаGiembycz, Mark A., and Robert Newton. "Harnessing the Clinical Efficacy of Phosphodiesterase 4 Inhibitors in Inflammatory Lung Diseases: Dual-Selective Phosphodiesterase Inhibitors and Novel Combination Therapies." In Phosphodiesterases as Drug Targets, 415–46. Berlin, Heidelberg: Springer Berlin Heidelberg, 2011. http://dx.doi.org/10.1007/978-3-642-17969-3_18.
Повний текст джерелаТези доповідей конференцій з теми "Dual inhibitors"
Chang, Wenteh, Ke Wei, and Glenn Rosen. "Suppression Of Lung Fibrosis By Dual MTOR Inhibitors." In American Thoracic Society 2011 International Conference, May 13-18, 2011 • Denver Colorado. American Thoracic Society, 2011. http://dx.doi.org/10.1164/ajrccm-conference.2011.183.1_meetingabstracts.a2718.
Повний текст джерелаQuinn, Elizabeth R., Pietro Ciceri, Susanne Müller-Knapp, Alison O'Mahony, Oleg Fedorov, Panagis Filippakopoulos, Jeremy P. Hunt, et al. "Abstract 5387: Dual kinase/bromodomain inhibitors for rationally designed polypharmacology." In Proceedings: AACR Annual Meeting 2014; April 5-9, 2014; San Diego, CA. American Association for Cancer Research, 2014. http://dx.doi.org/10.1158/1538-7445.am2014-5387.
Повний текст джерелаKeta, Otilija, Jelena Bošković, Vladana Petković, Neda Đorđević, Vladimir Dobričić, Olivera Čudina, and Snežana B. Pajović. "Synthesis and cytotoxic activity of selected dual COX-2 and 5-LOX inhibitors in HeLa and MIA PaCa-2 human cancer cell lines." In 2nd International Conference on Chemo and Bioinformatics. Institute for Information Technologies, University of Kragujevac, 2023. http://dx.doi.org/10.46793/iccbi23.503k.
Повний текст джерелаChang, Lei, Peter Graham, Jingli Hao, Jie Ni, Joseph Bucci, Paul Cozzi, John Kearseley, and Yong Li. "Abstract A283: PI3K/Akt/mTOR dual inhibitors have an advantage over single inhibitors in overcoming prostate cancer radioresistance." In Abstracts: AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics--Oct 19-23, 2013; Boston, MA. American Association for Cancer Research, 2013. http://dx.doi.org/10.1158/1535-7163.targ-13-a283.
Повний текст джерелаHannon, C. L., J. Gerstmann, F. B. Mansfeld, and Z. N. Sun. "Development of Improved Corrosion Inhibitors for Ammonia-Water Absorption Heat Pumps." In ASME 2000 International Mechanical Engineering Congress and Exposition. American Society of Mechanical Engineers, 2000. http://dx.doi.org/10.1115/imece2000-1294.
Повний текст джерелаHannon, C. L., J. Gerstmann, F. B. Mansfeld, and Z. Sun. "Development of Corrosion Inhibitors for Absorption Heat Pumps." In ASME 2002 International Mechanical Engineering Congress and Exposition. ASMEDC, 2002. http://dx.doi.org/10.1115/imece2002-33411.
Повний текст джерелаSaunders, Nicholas A., Rafael Erlich, Zoulika Kherrouche, Mehlika Hazar-Rethinam, Lilia Merida de Long, and Alexander Guminski. "Abstract 2559: Preclinical evaluation of dual PI3K-mTOR inhibitors and histone deacetylase inhibitors in head and neck squamous cell carcinoma." In Proceedings: AACR 102nd Annual Meeting 2011‐‐ Apr 2‐6, 2011; Orlando, FL. American Association for Cancer Research, 2011. http://dx.doi.org/10.1158/1538-7445.am2011-2559.
Повний текст джерелаChen, Chien-Yu, Fuu-Jen Tsai, Jing-Gung Chung, Chang-Hai Tsai, Yuan-Man Hsu, Hung-Jin Huang, Tin-Yun Ho, et al. "A Novel Strategy for Designing Dual-Target Inhibitors of KU86 and XRCC4." In 2009 2nd International Conference on Biomedical Engineering and Informatics. IEEE, 2009. http://dx.doi.org/10.1109/bmei.2009.5302325.
Повний текст джерелаSivanandhan, Dhanalakshmi, Sridharan Rajagopalan, Sreekala Nair, Purushottam Dewang, Durga Prasanna Kumar, Chandrika Mulakala, Lavanya Mahadevan, et al. "Abstract 3509: Novel dual inhibitors of LSD1-HDAC for treatment of cancer." In Proceedings: AACR 106th Annual Meeting 2015; April 18-22, 2015; Philadelphia, PA. American Association for Cancer Research, 2015. http://dx.doi.org/10.1158/1538-7445.am2015-3509.
Повний текст джерелаTaidi, Loubna, Amal Maurady, and Rajae Chahboune. "Dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase with molecular docking study." In NISS 2023: The 6th International Conference on Networking, Intelligent Systems & Security. New York, NY, USA: ACM, 2023. http://dx.doi.org/10.1145/3607720.3607737.
Повний текст джерелаЗвіти організацій з теми "Dual inhibitors"
Li, Pui-Kai. Development for Dual Acting Inhibitors for Breast Cancer. Fort Belvoir, VA: Defense Technical Information Center, August 2001. http://dx.doi.org/10.21236/ada398105.
Повний текст джерелаLi, Pui-Kai. Development of Dual Acting Inhibitors for Breast Cancer. Fort Belvoir, VA: Defense Technical Information Center, August 2002. http://dx.doi.org/10.21236/ada410197.
Повний текст джерелаLi, Pui-Kai. Development of Dual Acting Inhibitors for Breast Cancer. Fort Belvoir, VA: Defense Technical Information Center, November 2004. http://dx.doi.org/10.21236/ada432232.
Повний текст джерелаLi, Pui K. Development of Dual Acting Inhibitors for Breast Cancer. Fort Belvoir, VA: Defense Technical Information Center, August 2003. http://dx.doi.org/10.21236/ada421903.
Повний текст джерелаSimeonova, Rumiana, Vessela Vitcheva, Ivanka Kostadinova, Iva Valkova, Irena Philipova, Georgi Stavrakov, Nikolai Danchev, and Irini Doytchinova. In Vivo Studies on Novel Potent Acetylcholinesterase Inhibitors with Dual-site Binding for Treatment of Alzheimer’s Disease. "Prof. Marin Drinov" Publishing House of Bulgarian Academy of Sciences, June 2021. http://dx.doi.org/10.7546/crabs.2021.06.13.
Повний текст джерелаChagas, Gabriel, Rafael Chagas, and Amanda Rangel. Effectiveness and Safety of Single Antiplatelet Therapy with P2Y12 Inhibitor Monotherapy versus Dual Antiplatelet Therapy After Percutaneous Coronary Intervention for Acute Coronary Syndrome: A Systematic Review and Meta-Analysis. INPLASY - International Platform of Registered Systematic Review and Meta-analysis Protocols, July 2022. http://dx.doi.org/10.37766/inplasy2022.7.0097.
Повний текст джерелаGao, Tong, Yintang Wang, Chang Meng, Siyuan Li, Lei Bi, Yu Geng, and Ping Zhang. Aspirin Vs P2Y12 inhibitor monotherapy following dual antiplatelet therapy after coronary stenting in patients with ischemic heart disease: an updated systematic review and meta-analysis. INPLASY - International Platform of Registered Systematic Review and Meta-analysis Protocols, December 2022. http://dx.doi.org/10.37766/inplasy2022.12.0011.
Повний текст джерелаGafni, Yedidya, Moshe Lapidot, and Vitaly Citovsky. Dual role of the TYLCV protein V2 in suppressing the host plant defense. United States Department of Agriculture, January 2013. http://dx.doi.org/10.32747/2013.7597935.bard.
Повний текст джерела