Identification of small molecule inhibitors of the hepatitis C virus RNA-dependent RNA polymerase from a pyrrolidine combinatorial mixture

被引：66

作者：

Burton, G

Ku, TW

Carr, TJ

Kiesow, T

Sarisky, RT

Lin-Goerke, J

Baker, A

Earnshaw, DL

Hofmann, GA

Keenan, RM

Dhanak, D

机构：

[1] GlaxoSmithKline, Collegeville, PA 19426 USA

[2] GlaxoSmithKline, King Of Prussia, PA 19406 USA

[3] GlaxoSmithKline, Harlow CM19 5AW, Essex, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 06期

关键词：

hepatitis C virus; RNA polymerase; pyrrolidine; combinatorial mixture;

D O I：

10.1016/j.bmcl.2005.01.076

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

HTS of the compound collection for inhibition of the HCV RNA dependent RNA polymerase identified two 168 member N-acyl pyrrolidine combinatorial mixture hits. Deconvolution and expansion of these mixtures by solid phase synthesis to establish initial SAR and identify a potent inhibitor is reported. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：1553 / 1556

页数：4

共 50 条

[41] DISCOVERY OF NATURALLY OCCURRING AURONES THAT ARE POTENT ALLOSTERIC INHIBITORS OF HEPATITIS C VIRUS RNA-DEPENDENT RNA POLYMERASE
Ahmed-belkacem, Abdelhakim
Haudecoeur, Romain
Yi, Wei
Antoine, Fortune
Brillet, Rozenn
Catherine, Belle
Edwige, Nicolle
Pallier, Coralie
Boumendjel, Ahcene
Pawlotsky, Jean-Michel
HEPATOLOGY, 2011, 54 : 538A - 538A
[42] Purification of Zika virus RNA-dependent RNA polymerase and its use to identify small-molecule Zika inhibitors
Xu, Hong-Tao
Hassounah, Said A.
Colby-Germinario, Susan P.
Oliveira, Maureen
Fogarty, Clare
Quan, Yudong
Han, Yingshan
Golubkov, Olga
Ibanescu, Ilinca
Brenner, Bluma
Stranix, Brent R.
Wainberg, Mark A.
JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY, 2017, 72 (03) : 727 - 734
[43] The advance on research of RNA-dependent RNA polymerase (RdRp) of hepatitis C virus.
Chen, ZB
Wang, SQ
PROGRESS IN BIOCHEMISTRY AND BIOPHYSICS, 2000, 27 (06) : 605 - 608
[44] Mutational analysis of the structure and functions of hepatitis C virus RNA-dependent RNA polymerase
Qin, WP
Yamashita, T
Shirota, Y
Lin, Y
Wei, WX
Murakami, S
HEPATOLOGY, 2001, 33 (03) : 728 - 737
[45] Resistance profile of a hepatitis C virus RNA-dependent RNA polymerase benzothiadiazine inhibitor
Nguyen, TT
Gates, AT
Gutshall, LL
Johnston, VK
Gu, BH
Duffy, KJ
Sarisky, RT
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 2003, 47 (11) : 3525 - 3530
[46] The Kinetics of Hepatitis C Virus RNA-Dependent RNA Polymerase Inhibition by Nucleoside Analogues
Villalba, Brian
Li, Jiawen
Johnson, Kenneth A.
BIOPHYSICAL JOURNAL, 2018, 114 (03) : 585A - 585A
[47] Activation of protein kinase R by hepatitis C virus RNA-dependent RNA polymerase
Suzuki, Ryosuke
Matsuda, Mami
Shimoike, Takashi
Watashi, Koichi
Aizaki, Hideki
Kato, Takanobu
Suzuki, Tetsuro
Muramatsu, Masamichi
Wakita, Takaji
VIROLOGY, 2019, 529 : 226 - 233
[48] RNA replication without RNA-dependent RNA polymerase: Surprises from hepatitis delta virus
Lai, MMC
JOURNAL OF VIROLOGY, 2005, 79 (13) : 7951 - 7958
[49] Identification of a Pyridoxine-Derived Small-Molecule Inhibitor Targeting Dengue Virus RNA-Dependent RNA Polymerase
Xu, Hong-Tao
Colby-Germinario, Susan P.
Hassounah, Said
Quashie, Peter K.
Han, Yingshan
Oliveira, Maureen
Stranix, Brent R.
Wainberg, Mark A.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 2016, 60 (01) : 600 - 608
[50] Initiation of RNA Synthesis by the Hepatitis C Virus RNA-Dependent RNA Polymerase Is Affected by the Structure of the RNA Template
Reich, Stefan
Kovermann, Michael
Lilie, Hauke
Knick, Paul
Geissler, Rene
Golbik, Ralph Peter
Balbach, Jochen
Behrens, Sven-Erik
BIOCHEMISTRY, 2014, 53 (44) : 7002 - 7012

← 1 2 3 4 5 →