1,4-Bis(5-(naphthalen-1-yl)thiophen-2-yl)naphthalene, a small molecule, functions as a novel anti-HIV-1 inhibitor targeting the interaction between integrase and cellular Lens epithelium-derived growth factor
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AbstractTranslocation of viral integrase (IN) into the nucleus is a critical precondition of integration during the life cycle of HIV, a causative agent of Acquired Immunodeficiency Syndromes (AIDS). As the first discovered cellular factor to interact with IN, Lens epithelium-derived growth factor (LEDGF/p75) plays an important role in the process of integration. Disruption of the LEDGF/p75-IN interaction has provided a great interest for anti-HIV agent discovery. In this work, we reported that one small molecular compound, 1,4-bis(5-(naphthalen-1-yl)thiophen-2-yl)naphthalene(Compound 15), potently inhibit the IN-LEDGF/ p75 interaction and affect the HIV-1 IN nuclear distribution at 1 mu M. The putative binding mode of Compound 15 was constructed by a molecular docking simulation to provide structural insights into the ligand-binding mechanism. Compound 15 suppressed viral replication by measuring p24 antigen production in HIV-1(IIIB) acute infected C8166 cells with EC50 value of 11.19 mu M. Compound 15 might supply useful structural information for further anti-HIV agent discovery. (C) 2014 Published by Elsevier Ireland Ltd.
All Author(s) ListGu WG, Ip DTM, Liu SJ, Chan JH, Wang Y, Zhang X, Zheng YT, Wan DCC
Journal nameChemico-Biological Interactions
Volume Number213
Pages21 - 27
LanguagesEnglish-United Kingdom
KeywordsHIV-1 integrase; Lens epithelium-derived growth factor (LEDGF/P75); Molecular docking
Web of Science Subject CategoriesBiochemistry & Molecular Biology; BIOCHEMISTRY & MOLECULAR BIOLOGY; Pharmacology & Pharmacy; PHARMACOLOGY & PHARMACY; Toxicology; TOXICOLOGY

Last updated on 2022-15-01 at 23:40