This old version of Proteopedia is provided for student assignments while the new version is undergoing repairs. Content and edits done in this old version of Proteopedia after March 1, 2026 will eventually be lost when it is retired in about June of 2026.
Apply for new accounts at the new Proteopedia. Your logins will work in both the old and new versions.
2dxs
From Proteopedia
|
Crystal structure of HCV NS5B RNA polymerase complexed with a tetracyclic inhibitor
Overview
We report a new series of hepatitis C virus NS5B RNA polymerase inhibitors containing a conformationally constrained tetracyclic scaffold. SAR studies led to the identification of 6,7-dihydro-5H-benzo[5,6][1,4]diazepino[7,1-a]indoles (19 and 20) bearing a basic pendent group with high biochemical and cellular potencies. These compounds displayed a very small shift in cellular potency when the replicon assay was performed in the presence of human serum albumin.
About this Structure
2DXS is a Single protein structure of sequence from Hepatitis c virus with as ligand. Active as RNA-directed RNA polymerase, with EC number 2.7.7.48 Full crystallographic information is available from OCA.
Reference
Discovery of conformationally constrained tetracyclic compounds as potent hepatitis C virus NS5B RNA polymerase inhibitors., Ikegashira K, Oka T, Hirashima S, Noji S, Yamanaka H, Hara Y, Adachi T, Tsuruha J, Doi S, Hase Y, Noguchi T, Ando I, Ogura N, Ikeda S, Hashimoto H, J Med Chem. 2006 Nov 30;49(24):6950-3. PMID:17125247
Page seeded by OCA on Thu Feb 21 17:03:49 2008
Categories: Hepatitis c virus | RNA-directed RNA polymerase | Single protein | Adachi, T. | Doi, S. | Ikegashira, K. | Kamada, M. | Murase, K. | Nomura, A. | Orita, T. | Tsuruha, J. | Uehara, K. | Watanabe, S. | JTP | Hcv | Ns5b | Rna polymerase
