Progress in HIV-1 Integrase Inhibitors: A Review of their Chemical Structure Diversity

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HAJIMAHDI ZAHRA; ZARGHI AFSHIN

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Journal Paper

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Journal: Iranian Journal of Pharmaceutical Research Year:2016 | Volume:15 | Issue:4 Page(s): 595-628

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Title

Progress in HIV-1 Integrase Inhibitors: A Review of their Chemical Structure Diversity

Author(s)

HAJIMAHDI ZAHRA | ZARGHI AFSHIN | Issue Writer Certificate

Keywords

HIV-1

Integrase enzyme

SAR

Molecular diversity

IN Inhibitors

Abstract

HIV-1 integrase (IN) enzyme, one of the three main enzymes of HIV-1, catalyzed the insertion of the viral DNA into the genome of host cells. Because of the lack of its homologue in human cells and its essential role in HIV-1 replication, IN inhibition represents an attractive therapeutic target for HIV-1 treatment. Since identification of IN as a promising therapeutic target, a major progress has been made, which has facilitated and led to the approval of three drugs. This review focused on the structural features of the most important IN Inhibitors and categorized them structurally in 10 scaffolds. We also briefly discussed the structural and functional properties of HIV-1 IN and binding modes of IN Inhibitors. The SAR analysis of the known IN Inhibitors provides some useful clues to the possible future discovery of novel IN Inhibitors.

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APA: Copy

HAJIMAHDI, ZAHRA, & ZARGHI, AFSHIN. (2016). Progress in HIV-1 Integrase Inhibitors: A Review of their Chemical Structure Diversity. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR), 15(4), 595-628. SID. https://sid.ir/paper/289082/en

Vancouver: Copy

HAJIMAHDI ZAHRA, ZARGHI AFSHIN. Progress in HIV-1 Integrase Inhibitors: A Review of their Chemical Structure Diversity. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR)[Internet]. 2016;15(4):595-628. Available from: https://sid.ir/paper/289082/en

IEEE: Copy

ZAHRA HAJIMAHDI, and AFSHIN ZARGHI, “Progress in HIV-1 Integrase Inhibitors: A Review of their Chemical Structure Diversity,” IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR), vol. 15, no. 4, pp. 595–628, 2016, [Online]. Available: https://sid.ir/paper/289082/en

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