The integrase enzyme facilitates the incorporation of HIV-1 proviral DNA into the host cell genome and catalyses a function vital to viral replication. Inhibitors of this enzyme represent the newest class of antiretroviral drugs in our armamentarium to treat HIV-1 infection. Raltegravir, an ...
and over HIV-1 integrase strand transfer (INST) activity because of their active site similarities; (2) to a larger extent, the inability of active site inhibitors to confer significant antiviral effect, presumably due to a steep substrate barrier by which the pre-existing substrate prevents acces...
HIV integrase is a 32 kDa protein produced from the C-terminal portion of the Pol gene product, an enzyme produced by HIV that enables its genetic material to be integrated into the DNA of the infected cell [2]which are not to be confused with phage integrases and a key component in the...
A hallmark of retroviral replication is establishment of the proviral state, wherein a DNA copy of the viral RNA genome is stably incorporated into a host cell chromosome. Integrase is the viral enzyme responsible for the catalytic steps involved in this
Integrase Strand Transfer Inhibitors (INSTIs) played a pivotal role in sus- tained viral suppression, which disrupted the viral life cycle by inhibiting the integrase enzyme, leading to rapid viral load reduction [5]. Recent studies have emphasized the efficacy of second-generation INSTIs like bic...
Activity of IN is essential for the proliferation of the virus, as this enzyme catalyzes the irreversible incorporation of the viral DNA into the host genome. IN belongs to the superfamily of DDE(D) nucleotidyltransferases (4). The enzyme contains three domains, the N-terminal domain, the ...
HIV-1 integrase (IN) is a key enzyme in viral replication that catalyzes the covalent integration of viral cDNA into the host genome. Currently, five HIV-1 IN strand transfer inhibitors (INSTIs) are approved for clinical use. These drugs represent an important addition to the armamentarium for...
可溶性HIV-1整合酶重组蛋白的制备方法,属于生物技术领域. Soluble recombinant HIV-1 integrase protein preparation, which belongs to the field of biotechnology. 制备方法包括诱导表达,菌体破碎,纯化等步骤,所用表达培养基含有15-35g/L胰蛋白胨,10-20g/L酵母提取物,2-3g/L氯化钠,1g/L葡萄糖,10-15g/L...
There are a number of discrete steps involved in this process including processing of the viral cDNA by removal of two bases from each 3′-terminus and joining of the recessed ends to the host DNA. Studies have shown that in the absence of a functional integrase enzyme HIV is not ...
Title: Inhibitors of the Hiv Integrase Enzyme United States Patent Application 20070232644 Kind Code: A1 Abstract: The present invention relates to compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, pharmaceutical compositions comprising compounds of formula (I), and ...