Relevant bibliographies by topics / Peptidomimetic inhibitors

Academic literature on the topic 'Peptidomimetic inhibitors'

Author: Grafiati

Published: 10 December 2022

Last updated: 28 January 2023

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Journal articles on the topic "Peptidomimetic inhibitors"

Kikelj, Danijel. "Peptidomimetic Thrombin Inhibitors." Pathophysiology of Haemostasis and Thrombosis 33, no. 5-6 (2003): 487–91. http://dx.doi.org/10.1159/000083850.

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Dong, Guangping, Iredia D. Iyamu, Jonah Z. Vilseck, Dongxing Chen, and Rong Huang. "Improved Cell-Potent and Selective Peptidomimetic Inhibitors of Protein N-Terminal Methyltransferase 1." Molecules 27, no. 4 (February 18, 2022): 1381. http://dx.doi.org/10.3390/molecules27041381.

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Protein N-terminal methyltransferase 1 (NTMT1) recognizes a unique N-terminal X-P-K/R motif (X represents any amino acid other than D/E) and transfers 1–3 methyl groups to the N-terminal region of its substrates. Guided by the co-crystal structures of NTMT1 in complex with the previously reported peptidomimetic inhibitor DC113, we designed and synthesized a series of new peptidomimetic inhibitors. Through a focused optimization of DC113, we discovered a new cell-potent peptidomimetic inhibitor GD562 (IC50 = 0.93 ± 0.04 µM). GD562 exhibited improved inhibition of the cellular N-terminal methylation levels of both the regulator of chromosome condensation 1 and the oncoprotein SET with an IC50 value of ~50 µM in human colorectal cancer HCT116 cells. Notably, the inhibitory activity of GD562 for the SET protein increased over 6-fold compared with the previously reported cell-potent inhibitor DC541. Furthermore, GD562 also exhibited over 100-fold selectivity for NTMT1 against several other methyltransferases. Thus, this study provides a valuable probe to investigate the biological functions of NTMT1.

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Turkson, James, Joon S. Kim, Shumin Zhang, Jing Yuan, Mei Huang, Matthew Glenn, Eric Haura, Said Sebti, Andrew D. Hamilton, and Richard Jove. "Novel peptidomimetic inhibitors of signal transducer and activator of transcription 3 dimerization and biological activity." Molecular Cancer Therapeutics 3, no. 3 (March 1, 2004): 261–69. http://dx.doi.org/10.1158/1535-7163.261.3.3.

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Abstract The critical role of signal transducer and activator of transcription 3 (Stat3) in the growth and survival of human tumor cells identifies it as a promising target for cancer drug discovery. We previously identified a Stat3 SH2 domain-binding phosphopeptide, PY*LKTK, and its tripeptide derivatives, PY*L and AY*L (where Y* represents phosphotyrosine), which inhibit Stat3 biochemical activity and biological function. Here, we report novel peptidomimetic compounds based on PY*L (or AY*L) with substitution of the Y-1 residue by benzyl, pyridyl, or pyrazinyl derivatives that are selective and greater than 5-fold more potent in disrupting Stat3 activity in vitro than lead tripeptides. The biological activities of these derivatives mirror that originally observed for peptides. In this context, the representative peptidomimetic ISS 610 with 4-cyanobenzoate substitution inhibits constitutive Stat3 activity in Src-transformed mouse fibroblasts and human breast and lung carcinoma cells. This effect is not evident with the non-phosphorylated counterpart, ISS 610NP, consistent with interaction of peptidomimetics with the SH2 domain of Stat3. Moreover, ISS 610 induces cell growth inhibition and apoptosis of Src-transformed fibroblasts that contain persistently active Stat3. We present the first report of a peptidomimetic approach to design of small-molecule inhibitors of Stat3 that are also among the first examples of disruptors of transcription factor dimerization with the potential for novel cancer therapy.

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Randolph, John, and David DeGoey. "Peptidomimetic Inhibitors of HIV Protease." Current Topics in Medicinal Chemistry 4, no. 10 (June 1, 2004): 1079–95. http://dx.doi.org/10.2174/1568026043388330.

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Cameron Black, W. "Peptidomimetic Inhibitors of Cathepsin K." Current Topics in Medicinal Chemistry 10, no. 7 (May 1, 2010): 745–51. http://dx.doi.org/10.2174/156802610791113450.

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Marsters, James C., Robert S. McDowell, Mark E. Reynolds, David A. Oare, Todd C. Somers, Mark S. Stanley, Thomas E. Rawson, et al. "Benzodiazepine peptidomimetic inhibitors of farnesyltransferase." Bioorganic & Medicinal Chemistry 2, no. 9 (September 1994): 949–57. http://dx.doi.org/10.1016/s0968-0896(00)82044-1.

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Marsters, James C., Robert S. McDowelll, Mark E. Reynolds, Todd C. Somers, Joseph L. Goldstein, Michael S. Brown, and Guy L. James. "Peptidomimetic inhibitors of Ras farnesylation." Chemistry & Biology 1 (April 1994): viii—ix. http://dx.doi.org/10.1016/1074-5521(94)90021-3.

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Santos, André L. S., Filipe P. Matteoli, Leandro S. Sangenito, Marta H. Branquinha, Bruno A. Cotrim, and Gabriel O. Resende. "Asymmetric peptidomimetics containing L-tartaric acid core inhibit the aspartyl peptidase activity and growth of Leishmania amazonensis promastigotes." Acta Parasitologica 63, no. 1 (March 26, 2018): 114–24. http://dx.doi.org/10.1515/ap-2018-0013.

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AbstractAspartyl-type peptidases are promising chemotherapeutic targets in protozoan parasites. In the present work, we identified an aspartyl peptidase activity from the soluble extract ofLeishmania amazonensispromastigotes, which cleaved the fluorogenic peptide 7-methoxycoumarin-4-acetyl-Gly-Lys-Pro-Ile-Leu-Phe-Phe-Arg-Leu-Lys(DNP)-D-Arg-amide (cathepsin D substrate) under acidic pH conditions at 37°C, showing aKMof 0.58 μM andVmaxof 129.87 fluorescence arbitrary units/s mg protein. The leishmanial aspartyl peptidase activity was blocked by pepstatin A (IC50= 6.8 μM) and diazo-acetyl-norleucinemetilester (IC50= 10.2 μM), two classical aspartyl peptidase inhibitors. Subsequently, the effects of 6 asymmetric peptidomimetics, containingL-tartaric acid core, were tested on both aspartyl peptidase and growth ofL.amazonensispromastigotes. The peptidomimetics named 88, 154 and 158 promoted a reduction of 50% on the leishmanial aspartyl peptidase activity at concentrations ranging from 40 to 85 μM, whereas the peptidomimetic 157 was by far the most effective, presenting IC50of 0.04 μM. Furthermore, the peptidomimetics 157 and 154 reduced the parasite proliferation in a dose-dependent manner, displaying IC50values of 33.7 and 44.5 μM, respectively. Collectively, the peptidomimetic 157 was the most efficient compound able to arrest both aspartyl peptidase activity and leishmanial proliferation, which raises excellent perspectives regarding its use against this human pathogenic protozoan.

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Barbotte, Laetitia, Abdelhakim Ahmed-Belkacem, Stéphane Chevaliez, Alexandre Soulier, Christophe Hézode, Henri Wajcman, Doug J. Bartels, et al. "Characterization of V36C, a Novel Amino Acid Substitution Conferring Hepatitis C Virus (HCV) Resistance to Telaprevir, a Potent Peptidomimetic Inhibitor of HCV Protease." Antimicrobial Agents and Chemotherapy 54, no. 6 (April 5, 2010): 2681–83. http://dx.doi.org/10.1128/aac.01796-09.

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ABSTRACT We characterized a novel substitution conferring moderate resistance to telaprevir, a peptidomimetic inhibitor of hepatitis C virus protease. V36C conferred a 4.0-fold increase in the telaprevir 50% inhibitory concentration in an enzyme assay and a 9.5-fold increase in the replicon model. The replication capacity of a replicon harboring V36C was close to that of the wild-type protease. This case emphasizes the complexity of hepatitis C virus resistance to protease inhibitors.

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Kinena, Linda, Gundars Leitis, Iveta Kanepe-Lapsa, Raitis Bobrovs, Kristaps Jaudzems, Vita Ozola, Edgars Suna, and Aigars Jirgensons. "Azole-based non-peptidomimetic plasmepsin inhibitors." Archiv der Pharmazie 351, no. 9 (July 31, 2018): 1800151. http://dx.doi.org/10.1002/ardp.201800151.

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Dissertations / Theses on the topic "Peptidomimetic inhibitors"

Appiah, Kubi George. "Development of Peptidomimetic Inhibitors Against Intracellular Targets." The Ohio State University, 2020. http://rave.ohiolink.edu/etdc/view?acc_num=osu1587519549871245.

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Hirsch, Brett M. "Mechanism-Based Peptidic and Peptidomimetic Human Sirtuin Inhibitors." University of Akron / OhioLINK, 2011. http://rave.ohiolink.edu/etdc/view?acc_num=akron1302055499.

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Allwood, Daniel Martin. "Discovery and development of novel non-peptidomimetic inhibitors of XIAP." Thesis, University of Cambridge, 2013. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.607657.

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Vicari, Daniele. "Evaluation Of VEGF Peptide Mimics As Inhibitors Of Angiogenesis." The Ohio State University, 2008. http://rave.ohiolink.edu/etdc/view?acc_num=osu1221509932.

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Breuer, Christian [Verfasser]. "Design and Synthesis of Covalent Peptidomimetic Inhibitors for Human Cysteine Cathepsins / Christian Breuer." Bonn : Universitäts- und Landesbibliothek Bonn, 2020. http://d-nb.info/1227990499/34.

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Watkins, Andrew M. "An in silico pipeline for the design of peptidomimetic protein-protein interaction inhibitors." Thesis, New York University, 2016. http://pqdtopen.proquest.com/#viewpdf?dispub=10188557.

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Protein-protein interactions have historically been branded “undruggable” due to their intrinsic challenges above and beyond protein-small molecule interactions. Incrementally, system after system has been approached by a variety of specialized design strategies. Still, the vast majority of interactions are intractable, and the profusion of individualized strategies leave few general approaches that might be able to extend to recalcitrant systems.

The ecosystem of tools available for developing inhibitors of protein-protein interactions suggests a potential modular strategy for proceeding from protein structure to plausible interaction inhibitors. My dissertation describes an analysis of all the protein-protein interactions containing key interfacial structural motifs found in protein structures catalogued by the Protein Data Bank. This work provides both data on extant protein interactions and specific conclusions regarding directions for further peptidomimetic design. We describe the incorporation of our lab’s peptidomimetic scaffolds into Rosetta and the validation of those methods against valuable biological systems. Finally, I chronicle substantial extension to Rosetta’s capacity to accurately model and design peptidomimetic structures.

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Nurbo, Johanna. "Peptidomimetic Enzyme Inhibitors Targeting M. tuberculosis Ribonucleotide Reductase and Hepatitis C Virus NS3 Protease /." Doctoral thesis, Uppsala : Acta Universitatis Upsaliensis, 2010. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-112345.

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Knuhtsen, Astrid. "Searching for inhibitors of the protein arginine methyl transferases : synthesis and characterisation of peptidomimetic ligands." Thesis, University of British Columbia, 2016. http://hdl.handle.net/2429/57228.

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Within the last two decades research in the field of epigenetics has increased significantly as targeting the epigenetic enzymes has the potential to alter the transcription of genes. Aberrant regulation of transcription is seen in several disease states, and drugs targeting the epigenetic histone deacetylases and DNA methylases are already marketed for cancer treatment. The Protein Arginine Methyl Transferases (PRMTs) belong to an epigenetic enzyme family that is upregulated in several cancers. However, currently no inhibitors of the PRMTs have been marketed. In this thesis several peptidomimetic strategies were utilised to modify the tryptophan residues in two peptide leads in order to discover new inhibitors of the PRMTs. One of these strategies involved constraining the side chain indole of tryptophan to the peptide backbone, thus producing a seven membered azepinone mimetic, Aia. The peptidomimetic efforts resulted in a structure-activity relationship study from which a constrained peptidomimetic containing two Aias was discovered to be a low micromolar inhibitor of several PRMTs. To characterise the inhibitor the conformation of the inhibitor was examined using solution-phase NMR and was shown to display an interesting turn-structure. The original peptide lead was fluorescently tagged and investigated in a cellular setting, but did not reveal any PRMT-specific localisation. In an effort to study the binding of the discovered inhibitor with the PRMTs, protein expression in E. coli and purification was performed. This resulted in the optimisation of PRMT6 purification in order to obtain highly pure PRMT6 for isothermal titration calorimetry (ITC) studies. Unfortunately these ITC studies were unsuccessful. Furthermore, as the constrained tryptophan mimetic had proven very useful in the peptidomimetic inhibitors of the PRMTs, we attempted to synthesise a lysine/arginine dipeptide mimetic using aziridine chemistry.
Pharmaceutical Sciences, Faculty of
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Kamath, Jayesh Ramrao. "Development of pseudosubstrate-based peptide and peptidomimetic inhibitors of p60ᶜ⁻ˢʳᶜ protein tyrosine kinase using combinatorial chemistry technology." Diss., The University of Arizona, 2000. http://hdl.handle.net/10150/289173.

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Several protein tyrosine kinases and the signaling pathways in which they participate have emerged as attractive targets for drug design. Specific and potent PTK inhibitors not only represent a new class of anticancer agents but may also be used as a powerful research tool to study the role of PTK-dependent cellular pathways in normal or tumor cell growth and to dissect the redundancy in signal transduction pathways. Dr. Lam's laboratory has previously reported identification of efficient and specific peptide substrates for p60ᶜ⁻ˢʳᶜ PTK using one-bead one-peptide combinatorial library method (Lam et al., 1995; Lou et al., 1996a and b). Based on the structure of these peptide substrates, I have identified and characterized potent and selective peptide inhibitors of p60ᶜ⁻ˢʳᶜ PTK. Some of the identified peptide inhibitors were used as a research tool in this dissertation to investigate the active site of the enzyme p60ᶜ⁻ˢʳᶜ PTK. In addition to potency and selectivity, a major criterion for a successful src inhibitor is its cell permeability as src is located inside the cell. Peptides are generally impermeable to cell membrane. A major accomplishment of this dissertation is development of cell permeable peptidomimetic inhibitors of p60ᶜ⁻ˢʳᶜ PTK based on the identified dipeptide motif --Ile-Tyr- (-I-Y-). This dissertation describes identification of tetrameric and trimeric peptidomimetic inhibitors using a combination of two combinatorial methods, the 'one-bead one-compound' combinatorial method and the 'iterative' combinatorial method. Some of the identified inhibitors seem to selectively affect transformed cells versus normal cells at lower concentrations. A lot of still needs to be done to optimize these inhibitors. However, the accomplished work in this dissertation proves the feasibility of the pseudosubstrate peptide-based approach for the development of cell permeable peptidomimetic inhibitors as anti-cancer therapeutic agents.

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Doligalski, Michael Lawrence. "Design and Development of Peptidomimetic Ligands for Targeting Radiopharmaceuticals, Imaging Probes, and Immunotherapeutics in Oncologic Disease." Scholar Commons, 2016. http://scholarcommons.usf.edu/etd/6492.

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Cancer is a leading cause of morbidity and mortality in the developed world. While much has been learned about these diseases in the last few decades, one of the main barriers to widespread advancement is the heterogeneity of cancer biology. A growing body of evidence supports the idea that certain protein receptors are overexpressed on the surface of tumor cells as compared to normal tissues. These extracellular biomarkers provide a unique opportunity to selectively target the tumor with both imaging and therapeutic modalities. The research in this dissertation focuses on targeting proteins on the tumor cell surface with peptidomimetic ligands. Following a description of various extracellular receptors, chapter one discusses targeting ligands designed to specifically and selectively bind these receptors. It reviews recent literature on targeted alpha-particle therapy and ends with an explanation of the advantages of peptide ligands. Three distinct approaches to imaging and therapeutic modalities are then discussed in subsequent chapters. First, a peptide ligand was designed to target radionuclides to malignant melanoma cells in an effort to develop companion radiotherapeutics and diagnostic imaging agents. The second research project describes the synthesis of a novel antagonist peptide ligand with conjugated near infrared dye, and its utility for real-time intraoperative guidance during pancreatic adenocarcinoma resection. Finally, the last chapter describes how the relatively new field of immunomodulatory effectors may be enhanced by their derivatization with peptide targeting ligands.

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Books on the topic "Peptidomimetic inhibitors"

Atta-ur-Rahman, ed. Advances in Organic Synthesis: Volume 17. BENTHAM SCIENCE PUBLISHERS, 2022. http://dx.doi.org/10.2174/97898150405241221701.

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Advances in Organic Synthesis is a book series devoted to the latest advances in synthetic approaches towards challenging structures. The series presents comprehensive reviews written by eminent authorities on different synthetic approaches to selected target molecules and new methods developed to achieve specific synthetic transformations or optimal product yields. Advances in Organic Synthesis is essential for all organic chemists in academia and the industry who wish to keep abreast of rapid and important developments in the field. Contents of this volume include these 6 reviews: - Multicomponent synthesis of heterocycles by microwave irradiation - Stereoselective procedures for the synthesis of olefines - Advanced microwave assisted organic synthesis method in organic chemistry - Five and six-membered n-heterocycle rings from diaminomaleonitrile - Peptidomimetics: current and future perspectives on hiv protease inhibitors - A review on synthesis, chemistry, and medicinal properties of benzothiazines and their related scaffolds

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Book chapters on the topic "Peptidomimetic inhibitors"

Mayo, Kevin H. "From Carbohydrate to Peptidomimetic Inhibitors of Galectins." In ACS Symposium Series, 61–77. Washington, DC: American Chemical Society, 2012. http://dx.doi.org/10.1021/bk-2012-1115.ch003.

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Ro, Seonggu, Jinho Lee, Seon-Goan Baek, Hae Yeon Cho, Jong Hyun Kim, Dong-Kyu Shin, Won-Hee Jung, et al. "Design of peptidomimetic farnesyltransferase inhibitors as anticancer agents." In Peptides for the New Millennium, 461–62. Dordrecht: Springer Netherlands, 2002. http://dx.doi.org/10.1007/0-306-46881-6_183.

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Iserloh, Ulrich, and Jared N. Cumming. "Peptidomimetic BACE1 Inhibitors for Treatment of Alzheimer's Disease: Design and Evolution." In Aspartic Acid Proteases as Therapeutic Targets, 441–79. Weinheim, Germany: Wiley-VCH Verlag GmbH & Co. KGaA, 2011. http://dx.doi.org/10.1002/9783527630943.ch16.

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Kiso, Yoshiaki, Hikaru Matsumoto, Tomonori Hamawaki, Youhei Sohma, Tooru Kimura, and Yoshio Hayashi. "Prodrug Forms of Peptidomimetic HIV Protease Inhibitors Using Intramolecular Cyclization Reaction." In Peptides: The Wave of the Future, 650–51. Dordrecht: Springer Netherlands, 2001. http://dx.doi.org/10.1007/978-94-010-0464-0_302.

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Almquist, Ronald G., Cris Olsen, Charles K. Hiebert, Srinivasa R. Kadambi, Susan Brandt, and Lawrence R. Toll. "Development of peptidomimetic inhibitors of a newly isolated atrial peptide-degrading enzyme." In Peptides, 791–92. Dordrecht: Springer Netherlands, 1992. http://dx.doi.org/10.1007/978-94-011-2264-1_318.

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Bursavich, Matthew G., and Daniel H. Rich. "Solution and Solid Phase Synthesis of Non-Peptide Peptidomimetic Aspartic Peptidase Inhibitors." In Peptides: The Wave of the Future, 537–38. Dordrecht: Springer Netherlands, 2001. http://dx.doi.org/10.1007/978-94-010-0464-0_249.

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Plummer, M., J. Hamby, E. Lunney, G. Hingorani, C. Humblet, B. Batley, and S. Rapundalo. "Topographically designed peptidomimetic inhibitors of human renin: Incorporation of novel, tethered P1 → P3 side chain functionalization." In Peptides, 634–36. Dordrecht: Springer Netherlands, 1994. http://dx.doi.org/10.1007/978-94-011-0683-2_209.

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Kamath, Jayesh R., Ruiwu Liu, Amanda M. Enstrom, Gang Liu, and Kit S. Lam. "Development of Peptidomimetic Substrates and Inhibitors that Bind to the Peptide Binding Pocket of the Catalytic Site of p60c-src Protein Tyrosine Kinase." In Peptides: The Wave of the Future, 183–84. Dordrecht: Springer Netherlands, 2001. http://dx.doi.org/10.1007/978-94-010-0464-0_81.

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Sham, Hing L. "Fluorine-Containing Peptidomimetics as Inhibitors of Aspartyl Proteases." In ACS Symposium Series, 184–95. Washington, DC: American Chemical Society, 1996. http://dx.doi.org/10.1021/bk-1996-0639.ch014.

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S Mainkar, Prathama, Surender Singh Jadav, and Kiranmai Nayani. "Peptidomimetics: Current and Future Perspectives on HIV Protease Inhibitors." In Advances in Organic Synthesis, 174–290. BENTHAM SCIENCE PUBLISHERS, 2022. http://dx.doi.org/10.2174/9789815040524122170007.

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The peptidomimetic-based design and synthesis of HIV-1 protease and other entry inhibitors are generally oriented to block the viral receptor functionalities in the host cells. Most of the drugs classified under HIV-1 protease inhibitors are primarily optimized through substrate-based design strategies. The peptidomimetic drugs present in the market are non-hydrolyzable by the catalytic aspartic acid residues, an indispensable approach still used in designing potential pharmacophores for protease inhibitors. Thus, a variety of amino acid-containing hybrid small molecules are tested against the HIV-1 protease enzyme by incorporating essential fragments required to block protease functionalities. However, the appearance of mutations in HIV polyproteins is a key parameter to be seriously considered while designing peptidomimetics. Hence, comprehensive knowledge regarding HIV peptidomimetic/medicinal chemistry along with optimization strategy and organic synthesis awareness is critical in the current scenario. The present chapter is aimed to provide in-depth literature on medicinally optimized HIV-1 protease inhibitors, Tat TAR RNA blockers with their synthesis, and later it is expanded to the peptidomimetics (entry inhibitors) involved in the envelope glycoprotein (gp120/gp41) and capsid inhibitors. Furthermore, the knowledge-based classification of HIV-1 protease inhibitors, anti-dimer agents, Tat-TAR RNA blockers, and entry inhibitors, along with their synthetic procedures, would serve as a single model template for scientific as well as academic research towards the development of anti-HIV peptidomimetics.

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Conference papers on the topic "Peptidomimetic inhibitors"

Wang, Xiaoju. "Abstract 189: Development of peptidomimetic inhibitors of theERGgene fusion product in prostate cancer." In Proceedings: AACR Annual Meeting 2017; April 1-5, 2017; Washington, DC. American Association for Cancer Research, 2017. http://dx.doi.org/10.1158/1538-7445.am2017-189.

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Wang, Xiaoju. "Abstract 5535: Development of peptidomimetic inhibitors of the ERG transcription factor in prostate cancer." In Proceedings: AACR 104th Annual Meeting 2013; Apr 6-10, 2013; Washington, DC. American Association for Cancer Research, 2013. http://dx.doi.org/10.1158/1538-7445.am2013-5535.

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Tymecka, Dagmara, Patrycja Redkiewicz, Piotr F. J. Lipiński, and Aleksandra Misicka. "Search for Peptidomimetic Inhibitors of the VEGF-A165 / NRP-1 Complex with Modification of the C-Terminal Arginine." In 36th European Peptide Symposium. The European Peptide Society, 2022. http://dx.doi.org/10.17952/36eps/36eps.2022.109.

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Senapedis, William T., Erkan Baloglu, Doriana Froim, Dilara McCauley, Yuh Min Chook, Michael Kauffman, Sharon Shacham, et al. "Abstract PR1:In silicodesigned covalent peptidomimetic inhibitors (KPT-SINE) of CRM1 modulate tumor suppressor protein nuclear export and induce apoptosis in cancer cells." In Proceedings: AACR Special Conference on Chemical Systems Biology: Assembling and Interrogating Computational Models of the Cancer Cell by Chemical Perturbations--Jun 27-30, 2012; Boston, MA. American Association for Cancer Research, 2012. http://dx.doi.org/10.1158/1538-7445.csb12-pr1.

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Ettouati, Laurent, Marie-Emmanuelle Million, Ophélie Arnaud, Géraldine Agusti, Waël Zeinyeh, Lucia Gonzalez-Lobato, Ali Koubeissi, et al. "Advances in peptidomimetics as inhibitors of ABC transporters." In 1st International Electronic Conference on Medicinal Chemistry. Basel, Switzerland: MDPI, 2015. http://dx.doi.org/10.3390/ecmc-1-a043.

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Silva-Júnior, Edeildo, Érica Rodrigues, Hannah Maus, Stefan Hammerschmidt, João Araújo-Júnior, and Tanja Schirmeister. "A new furin-based peptidomimetic as an inhibitor of NSB2-NS3 protease from Zika virus (ZIKV)." In 7th International Electronic Conference on Medicinal Chemistry. Basel, Switzerland: MDPI, 2021. http://dx.doi.org/10.3390/ecmc2021-11431.

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Anbalagan, Murali, Mei Sheng, Brian Fleischer, David Hangauer, and Brian G. Rowan. "Abstract 3859: Peptidomimetic Src kinase inhibitor KX-01 sensitizes estrogen receptor α-negative breast tumor xenografts to tamoxifen by inducing ERα re-expression." In Proceedings: AACR 107th Annual Meeting 2016; April 16-20, 2016; New Orleans, LA. American Association for Cancer Research, 2016. http://dx.doi.org/10.1158/1538-7445.am2016-3859.

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Chittamuru, Sumathi, Timothy M. Murphy, Sara A. Little, Andrew A. Taylor, Roseanne Wexler, and Laxman Desai. "Abstract P39: Pre-clinical evaluation of NEOS-223, an (S)-valine-thiazole derived peptidomimetic N-heterocycle, as an anticancer agent and P-glycoprotein inhibitor." In Abstracts: AACR Virtual Meeting: COVID-19 and Cancer; February 3-5, 2021. American Association for Cancer Research, 2021. http://dx.doi.org/10.1158/1557-3265.covid-19-21-p39.

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Reports on the topic "Peptidomimetic inhibitors"

Altstein, Miriam, and Ronald Nachman. Rationally designed insect neuropeptide agonists and antagonists: application for the characterization of the pyrokinin/Pban mechanisms of action in insects. United States Department of Agriculture, October 2006. http://dx.doi.org/10.32747/2006.7587235.bard.

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The general objective of this BARD project focused on rationally designed insect neuropeptide (NP) agonists and antagonists, their application for the characterization of the mechanisms of action of the pyrokinin/PBAN (PK-PBAN) family and the development of biostable, bioavailable versions that can provide the basis for development of novel, environmentally-friendly pest insect control agents. The specific objectives of the study, as originally proposed, were to: (i) Test stimulatory potencies of rationally designed backbone cyclic (BBC) peptides on pheromonotropic, melanotropic, myotropic and pupariation activities; (ii) Test the inhibitory potencies of the BBC compounds on the above activities evoked either by synthetic peptides (PBAN, LPK, myotropin and pheromonotropin) or by the natural endogenous mechanism; (iii) Determine the bioavailability of the most potent BBC compounds that will be found in (ii); (iv) Design, synthesize and examine novel PK/PBAN analogs with enhanced bioavailability and receptor binding; (v) Design and synthesize ‘magic bullet’ analogs and examine their ability to selectively kill cells expressing the PK/PBAN receptor. To achieve these goals the agonistic and antagonistic activities/properties of rationally designed linear and BBC neuropeptide (NP) were thoroughly studied and the information obtained was further used for the design and synthesis of improved compounds toward the design of an insecticide prototype. The study revealed important information on the structure activity relationship (SAR) of agonistic/antagonistic peptides, including definitive identification of the orientation of the Pro residue as trans for agonist activity in 4 PK/PBANbioassays (pheromonotropic, pupariation, melanotropic, & hindgut contractile) and a PK-related CAP₂b bioassay (diuretic); indications that led to the identification of a novel scaffold to develop biostbiostable, bioavailable peptidomimetic PK/PBANagonists/antagonists. The work led to the development of an arsenal of PK/PBAN antagonists with a variety of selectivity profiles; whether between different PKbioassays, or within the same bioassay between different natural elicitors. Examples include selective and non-selective BBC and novel amphiphilic PK pheromonotropic and melanotropic antagonists some of which are capable of penetrating the moth cuticle in efficacious quantities. One of the latter analog group demonstrated unprecedented versatility in its ability to antagonize a broad spectrum of pheromonotropic elicitors. A novel, transPro mimetic motif was proposed & used to develop a strong, selective PK agonist of the melanotropic bioassay in moths. The first antagonist (pure) of PK-related CAP₂b diuresis in flies was developed using a cisPro mimetic motif; an indication that while a transPro orientation is associated with receptor agonism, a cisPro orientation is linked with an antagonist interaction. A novel, biostablePK analog, incorporating β-amino acids at key peptidase-susceptible sites, exhibited in vivo pheromonotropic activity that by far exceeded that of PBAN when applied topically. Direct analysis of neural tissue by state-of-the-art MALDI-TOF/TOF mass spectrometry was used to identify specific PK/PK-related peptides native to eight arthropod pest species [house (M. domestica), stable (S. calcitrans), horn (H. irritans) & flesh (N. bullata) flies; Southern cattle fever tick (B. microplus), European tick (I. ricinus), yellow fever mosquito (A. aegypti), & Southern Green Stink Bug (N. viridula)]; including the unprecedented identification of mass-identical Leu/Ile residues and the first identification of NPs from a tick or the CNS of Hemiptera. Evidence was obtained for the selection of Neb-PK-2 as the primary pupariation factor of the flesh fly (N. bullata) among native PK/PK-related candidates. The peptidomic techniques were also used to map the location of PK/PK-related NP in the nervous system of the model fly D. melanogaster. Knowledge of specific PK sequences can aid in the future design of species specific (or non-specific) NP agonists/antagonists. In addition, the study led to the first cloning of a PK/PBAN receptor from insect larvae (S. littoralis), providing the basis for SAR analysis for the future design of 2ⁿᵈgeneration selective and/or nonselective agonists/antagonists. Development of a microplate ligand binding assay using the PK/PBAN pheromone gland receptor was also carried out. The assay will enable screening, including high throughput, of various libraries (chemical, molecular & natural product) for the discovery of receptor specific agonists/antagonists. In summary, the body of work achieves several key milestones and brings us significantly closer to the development of novel, environmentally friendly pest insect management agents based on insect PK/PBANNPs capable of disrupting critical NP-regulated functions.

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