%0 Journal Article %T Identification of a Novel Sulfonamide Non-Nucleoside Reverse Transcriptase Inhibitor by a Phenotypic HIV-1 Full Replication Assay. %+ Institut Pasteur Korea - Institut Pasteur de Corée %+ Department of Biotechnology, Translational Research Center for Protein Function Control %A Kim, Tae-Hee %A Ko, Yoonae %A Christophe, Thierry %A Cechetto, Jonathan %A Kim, Junwon %A Kim, Kyoung-Ae %A Boese, Annette S %A Garcia, Jean-Michel %A Fenistein, Denis %A Ju, Moon Kyeong %A Kim, Junghwan %A Han, Sung-Jun %A Kwon, Ho Jeong %A Brondani, Vincent %A Sommer, Peter %Z This work was supported by the National Research Foundation of Korea (NRF) grant (No.2010-01103) funded by the Korea government (MEST). HJK was supported by the National Research Foundation of Korea (2010-0017984). %< avec comité de lecture %@ 1932-6203 %J PLoS ONE %I Public Library of Science %V 8 %N 7 %P e68767 %8 2013 %D 2013 %R 10.1371/journal.pone.0068767 %M 23874756 %Z Life Sciences [q-bio]/Microbiology and Parasitology/VirologyJournal articles %X Classical target-based, high-throughput screening has been useful for the identification of inhibitors for known molecular mechanisms involved in the HIV life cycle. In this study, the development of a cell-based assay that uses a phenotypic drug discovery approach based on automated high-content screening is described. Using this screening approach, the antiviral activity of 26,500 small molecules from a relevant chemical scaffold library was evaluated. Among the selected hits, one sulfonamide compound showed strong anti-HIV activity against wild-type and clinically relevant multidrug resistant HIV strains. The biochemical inhibition, point resistance mutations and the activity of structural analogs allowed us to understand the mode of action and propose a binding model for this compound with HIV-1 reverse transcriptase. %G English %2 https://riip.hal.science/pasteur-00850251/document %2 https://riip.hal.science/pasteur-00850251/file/KIMetal2013.pdf %L pasteur-00850251 %U https://riip.hal.science/pasteur-00850251 %~ RIIP %~ RIIP_COREE