Literature DB >> 16087332

Hepatitis C virus NS3-4A serine protease inhibitors: SAR of P'2 moiety with improved potency.

A Arasappan1, F G Njoroge, T-Y Chan, F Bennett, S L Bogen, K Chen, H Gu, L Hong, E Jao, Y-T Liu, R G Lovey, T Parekh, R E Pike, P Pinto, B Santhanam, S Venkatraman, H Vaccaro, H Wang, X Yang, Z Zhu, B Mckittrick, A K Saksena, V Girijavallabhan, J Pichardo, N Butkiewicz, R Ingram, B Malcolm, A Prongay, N Yao, B Marten, V Madison, S Kemp, O Levy, M Lim-Wilby, S Tamura, A K Ganguly.   

Abstract

We have discovered that introduction of appropriate amino acid derivatives at P'2 position improved the binding potency of P3-capped alpha-ketoamide inhibitors of HCV NS3 serine protease. X-ray crystal structure of one of the inhibitors (43) bound to the protease revealed the importance of the P'2 moiety.

Entities:  

Mesh:

Substances:

Year:  2005        PMID: 16087332     DOI: 10.1016/j.bmcl.2005.06.091

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  5 in total

1.  Drug resistance against HCV NS3/4A inhibitors is defined by the balance of substrate recognition versus inhibitor binding.

Authors:  Keith P Romano; Akbar Ali; William E Royer; Celia A Schiffer
Journal:  Proc Natl Acad Sci U S A       Date:  2010-11-17       Impact factor: 11.205

2.  Viral and therapeutic control of IFN-beta promoter stimulator 1 during hepatitis C virus infection.

Authors:  Yueh-Ming Loo; David M Owen; Kui Li; Andrea K Erickson; Cynthia L Johnson; Penny M Fish; D Spencer Carney; Ting Wang; Hisashi Ishida; Mitsutoshi Yoneyama; Takashi Fujita; Takeshi Saito; William M Lee; Curt H Hagedorn; Daryl T-Y Lau; Steven A Weinman; Stanley M Lemon; Michael Gale
Journal:  Proc Natl Acad Sci U S A       Date:  2006-04-03       Impact factor: 11.205

Review 3.  Organic carbamates in drug design and medicinal chemistry.

Authors:  Arun K Ghosh; Margherita Brindisi
Journal:  J Med Chem       Date:  2015-01-07       Impact factor: 7.446

4.  Hepatitis E Virus Cysteine Protease Has Papain Like Properties Validated by in silico Modeling and Cell-Free Inhibition Assays.

Authors:  Shweta Saraswat; Meenakshi Chaudhary; Deepak Sehgal
Journal:  Front Cell Infect Microbiol       Date:  2020-01-23       Impact factor: 5.293

5.  Rapid synthesis of internal peptidyl α-ketoamides by on resin oxidation for the construction of rhomboid protease inhibitors.

Authors:  Tim Van Kersavond; Raphael Konopatzki; Merel A T van der Plassche; Jian Yang; Steven H L Verhelst
Journal:  RSC Adv       Date:  2021-01-20       Impact factor: 3.361

  5 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.