WebbThe hepatitis C virus NS3 protein contains a serine protease domain with a chymotrypsin-like fold, which is a target for development of therapeutics. We report the crystal structures of this domain complexed with NS4A cofactor and with two potent, reversible covalent inhibitors spanning the P1–P4 residues. Both inhibitors bind in an extended backbone … Webb5 feb. 2024 · Terminalia chebula Retz. forms a key component of traditional folk medicine and is also reported to possess antihepatitis C virus (HCV) and immunomodulatory activities. However, information on the intermolecular interactions of phytochemicals from this plant with HCV and human proteins are yet to be established. Thus, by this current …
Pim-1 inhibitor SMI-4a suppresses tumor growth in non-small …
Webb23 apr. 2024 · Background: In the present study, we aimed to investigate the effect of proviral integration site for moloney murine leukemia virus-1 (Pim-1) inhibitor (SMI-4a) on the progression of non-small cell lung cancer (NSCLC). Materials and methods: The effects of SMI-4a on proliferation, apoptosis, and cell cycle of NSCLC cells were examined by … WebbDyngo-4a is a potent dynamin inhibitor with IC50 of 0.38 μM, 1.1 μM, and 2.3 μM for DynI (brain), DynI (rec), and DynII (rec), respectively. Dyngo-4a inhibits dynamin-dependent endocytosis of transferrin in multiple cell types with IC₅₀ of 5.7 μM, and reduces synaptic vesicle endocytosis and activity-dependent bulk endocytosis in ... jerome thurman endocrinologist
Inhibition of the Hepatitis C Virus NS3/4A Protease
Webb29 nov. 2024 · SMI-4a is a pan-PIM small molecule inhibitor, and this agent exhibits demonstrable preclinical antitumour activity in a wide range of hematologic malignant cell lines. To further explore the effect of SMI-4a on B-ALL cells, B-ALL cell lines CCRF-SB and Sup-B15 were treated with this small molecule inhibitor, and the results showed that … WebbPDE4 inhibitors inhibit PDE4 activity, consequently increasing cAMP levels. This results in an anti-inflammatory effect, improving lung function. Roflumilast is a selective and … Webb31 jan. 2000 · Inhibition of the Hepatitis C Virus NS3/4A Protease. The Crystal Structures of Two Protease-Inhibitor Complexes (inhibitor I) PDB DOI: 10.2210/pdb1DY9/pdb; Classification: HYDROLASE/HYDROLASE INHIBITOR; Organism(s): Hepatitis C virus (isolate Taiwan) Expression System: Escherichia coli BL21(DE3) Mutation(s): Yes ; … jerome thornton