Fragment-Based Discovery of 8-Hydroxyquinoline Inhibitors of the HIV-1 Integrase-LEDGF/p75 Interaction

On the basis of an initial molecular modeling study suggesting the favorable binding of the “privileged” fragment 8-hydroxyquinoline with IN at the IN-LEDGF/p75 interface, we developed a set of modified 8-hydroxyquinoline fragments demonstrating micromolar IC(50) values for inhibition of the IN-LEDG...

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Bibliographic Details
Published in:J Med Chem
Main Authors: Serrao, Erik, Debnath, Bikash, Otake, Hiroyuki, Kuang, Yuting, Christ, Frauke, Debyser, Zeger, Neamati, Nouri
Format: Artigo
Language:Inglês
Published: 2013
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Article
Online Access:https://ncbi.nlm.nih.gov/pmc/articles/PMC6188675/
https://ncbi.nlm.nih.gov/pubmed/23445471
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm301632e
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