Indole-based allosteric inhibitors of HIV-1 integrase
نویسندگان
چکیده
منابع مشابه
Multimode, cooperative mechanism of action of allosteric HIV-1 integrase inhibitors.
The multifunctional HIV-1 enzyme integrase interacts with viral DNA and its key cellular cofactor LEDGF to effectively integrate the reverse transcript into a host cell chromosome. These interactions are crucial for HIV-1 replication and present attractive targets for antiviral therapy. Recently, 2-(quinolin-3-yl) acetic acid derivatives were reported to selectively inhibit the integrase-LEDGF ...
متن کاملA multimode, cooperative mechanism of action of allosteric HIV-1 integrase inhibitors
Center for Retrovirus Research and Comprehensive Cancer Center, College of Pharmacy, The Ohio State University, Columbus, OH 43210; Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, OH 43210; Department of Cancer Immunology and AIDS, Dana-Farber Cancer Institute, and Department of Medicine, Harvard Medical School, Boston, MA 02215; HIV ...
متن کاملProgress in HIV-1 integrase inhibitors: A review of their chemical structure diversity
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 h...
متن کاملProgress in HIV-1 integrase inhibitors: A review of their chemical structure diversity
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 h...
متن کاملPeptide inhibitors of the HIV-1 integrase protein
Prof. Assaf Friedler was born in Haifa, Israel, in 1971. He did his undergraduate studies in chemistry at the Hebrew University of Jerusalem, and Ph.D studies in chemistry at the Hebrew University of Jerusalem under the supervision of Prof. Chaim Gilon, in peptide chemistry and medicinal chemistry. After receiving his PhD degree, in 2000, Prof. Friedler moved to Cambridge, UK, to do his post-do...
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ژورنال
عنوان ژورنال: Bioorganic & Medicinal Chemistry Letters
سال: 2016
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2016.08.037