Treatment of HIV Infections with HIV Integrase Inhibitors
نویسندگان
چکیده
منابع مشابه
Integrase inhibitors in the treatment of HIV-1 infection.
Agents active against HIV type 1 (HIV-1) that target the viral integrase by inhibiting the strand transfer step of integration have now entered the clinical arena. Raltegravir is the first in this new class. Clinical trials in treatment-experienced and in treatment-naive patients have shown that raltegravir-containing regimens have potent antiretroviral activity and are well tolerated. Drug res...
متن کاملNovel HIV integrase inhibitors with anti-HIV activity: insights into integrase inhibition from docking studies.
The mechanism of integrase is generally accepted to be dependant on the presence of two divalent metal ions in the active site. However, the only available crystal structures of HIV-1 integrase contain either one or no metal ions, hampering structure-based design studies of integrase inhibitors. For this reason, a two-metal ion model of integrase was constructed. This model was used for computa...
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 کاملProbing chelation motifs in HIV integrase inhibitors.
A series of HIV integrase (HIV-1 IN) inhibitors were synthesized to evaluate the role of the metal-binding group (MBG) in this class of metalloenzyme inhibitors. A total of 21 different raltegravir-chelator derivative (RCD) compounds were prepared that differed only in the nature of the MBG. These IN strand-transfer inhibitors (INSTIs) were evaluated in vitro in cell-free enzyme activity assays...
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ژورنال
عنوان ژورنال: ACS Medicinal Chemistry Letters
سال: 2016
ISSN: 1948-5875,1948-5875
DOI: 10.1021/acsmedchemlett.6b00456