Structural highlights
Publication Abstract from PubMed
Hepatitis C virus (HCV) infection is treated with a combination of peginterferon alfa-2a/b and ribavirin. To address the limitations of this therapy, numerous small molecule agents are in development, which act by directly affecting key steps in the viral life-cycle. Herein we describe our discovery of quinolone derivatives, novel small-molecules that inhibit NS5b polymerase, a key enzyme of the viral life-cycle. A crystal structure of a quinoline analog bound to NS5B reveals that this class of compounds binds to allosteric site-II (non-nucleoside inhibitor-site 2, NNI-2) of this protein.
Quinolones as HCV NS5B polymerase inhibitors.,Kumar DV, Rai R, Brameld KA, Somoza JR, Rajagopalan R, Janc JW, Xia YM, Ton TL, Shaghafi MB, Hu H, Lehoux I, To N, Young WB, Green MJ Bioorg Med Chem Lett. 2011 Jan 1;21(1):82-7. Epub 2010 Nov 21. PMID:21145235[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Kumar DV, Rai R, Brameld KA, Somoza JR, Rajagopalan R, Janc JW, Xia YM, Ton TL, Shaghafi MB, Hu H, Lehoux I, To N, Young WB, Green MJ. Quinolones as HCV NS5B polymerase inhibitors. Bioorg Med Chem Lett. 2011 Jan 1;21(1):82-7. Epub 2010 Nov 21. PMID:21145235 doi:10.1016/j.bmcl.2010.11.068
