The HIV-1 CA protein is an attractive therapeutic target for the development of new antivirals. An inter-protomer pocket within the hexamer configuration of the CA, which is a binding site for key host dependency factors, is an especially appealing region for small molecule targeting. Using a field-based pharmacophore derived from an inhibitor known to interact with this region, coupled to biochemical and biological assessment, we have identified a new compound that inhibits HIV-1 infection and that targets the assembled CA hexamer. (C) 2015 Elsevier Ltd. All rights reserved.
Identification of a small molecule HIV-1 inhibitor that targets the capsid hexamer
Creators
Jimmy P. Xu - Drexel University
Jeffrey D. Branson - Drexel University
Rae Lawrence - Cresset, New Cambridge House, Bassingbourn Road, Litlington, Cambridgeshire SG8 0SS, UK.
Simon Cocklin - Drexel University
Publication Details
Bioorganic & medicinal chemistry letters, v 26(3), pp 824-828
Publisher
Elsevier
Number of pages
5
Grant note
R21AI104354 / NATIONAL INSTITUTE OF ALLERGY AND INFECTIOUS DISEASES; United States Department of Health & Human Services; National Institutes of Health (NIH) - USA; NIH National Institute of Allergy & Infectious Diseases (NIAID)
1R21AI10435401A1 / NIH/NIAID; United States Department of Health & Human Services; National Institutes of Health (NIH) - USA; NIH National Institute of Allergy & Infectious Diseases (NIAID)
Resource Type
Journal article
Language
English
Academic Unit
Biochemistry and Molecular Biology
Web of Science ID
WOS:000368797600025
Scopus ID
2-s2.0-85020320160
Other Identifier
991019167546304721
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