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Allosteric small-molecule kinase inhibitors [PDF]
Pharmacology & Therapeutics, 2015 Small-molecule kinase inhibitors are invaluable targeted therapeutics for the treatment of various human diseases, especially cancers. While the majority of approved and developed preclinical small-molecule inhibitors are characterized as type I or type II inhibitors that target the ATP-binding pocket of kinases, the remarkable sequential and ...
Thomas E Nielsen +2 more
exaly +5 more sources
Molecules, 2020 Protein kinase (CK2) has emerged as an attractive cancer therapeutic target and recent efforts have been made to develop its inhibitors. However, the development of selective inhibitors remains challenging because of the highly conserved ATP-binding ...
Xiaolan Chen +4 more
doaj +4 more sources
Molecules, 2016 Cyclin-dependent kinase 2 (CDK2), a member of Cyclin-dependent kinases (CDKs), plays an important role in cell division and DNA replication. It is regarded as a desired target to treat cancer and tumor by interrupting aberrant cell proliferation ...
Fang Lu +5 more
doaj +4 more sources
Discovery of a Potent Fluorescence Polarization Probe for Identifying USP1 Allosteric Inhibitors [PDF]
Advanced ScienceThe deubiquitinating enzyme, ubiquitin‐specific protease 1 (USP1), is overexpressed in various tumor types, making it a promising target for cancer therapy.
Jiawei Cheng +12 more
doaj +2 more sources
Structural biology of HIV-1 reverse transcriptase allosteric inhibitors for drug design [PDF]
Acta Pharmaceutica Sinica BHIV-1 reverse transcriptase (RT) is responsible for reverse transcription of viral single-stranded RNA to double-stranded DNA, which plays an important role in the replication cycle of HIV-1 and has been identified as a key target for anti-HIV-1 drug ...
Zhenzhen Zhou +8 more
doaj +2 more sources
Allosteric IGF-1R Inhibitors [PDF]
ACS Medicinal Chemistry Letters, 2010 Targeting allosteric protein sites is a promising approach to interfere selectively with cellular signaling cascades. We have discovered a novel class of allosteric insulin-like growth factor-I receptor (IGF-1R) inhibitors. 3-Cyano-1H-indole-7-carboxylic acid {1-[4-(5-cyano-1H-indol-3-yl)butyl]piperidin-4-yl}amide (10) was found with nanomolar ...
Timo Heinrich +2 more
exaly +4 more sources
Small-molecule allosteric inhibitors of GPX4. [PDF]
Cell Chem Biol, 2022 Encouraged by the dependence of drug-resistant, metastatic cancers on GPX4, we examined biophysical mechanisms of GPX4 inhibition, which revealed an unexpected allosteric site. We found that this site was involved in native regeneration of GPX4 under low glutathione conditions.
Liu H +7 more
europepmc +3 more sources
Development of Novel Proline- and Pipecolic Acid-Based Allosteric Inhibitors of Dengue and Zika Virus NS2B/NS3 Protease [PDF]
PharmaceuticalsBackground: In this study, we report a novel series of proline- and pipecolic acid-based small molecules designed as allosteric inhibitors of the NS2B/NS3 serine proteases from dengue and Zika viruses, key targets in antiviral drug discovery.
Josè Starvaggi +10 more
doaj +2 more sources
Computational drug repurposing of Akt-1 allosteric inhibitors for non-small cell lung cancer [PDF]
Scientific Reports, 2023 Non-small cell lung carcinomas (NSCLC) are the predominant form of lung malignancy and the reason for the highest number of cancer-related deaths. Widespread deregulation of Akt, a serine/threonine kinase, has been reported in NSCLC.
Krishnaprasad Baby +7 more
doaj +2 more sources
Off-target autophagy inhibition by SHP2 allosteric inhibitors contributes to their antitumor activity in RAS-driven cancers [PDF]
The Journal of Clinical InvestigationAberrant activation of RAS/MAPK signaling is common in cancer, and efforts to inhibit pathway components have yielded drugs with promising clinical activities.
Yiming Miao +12 more
doaj +2 more sources