Publications by authors named "Yoshitsugu Ohata"
Article Synopsis
- Researchers developed new allosteric inhibitors for HIV-1 integrase by using a spirocyclic design that limits the flexibility of the inhibitor's structure.
- One particularly effective compound (compound 5) demonstrated antiviral activity by targeting the LEDGF/p75 binding site on integrase, enhanced by a lipophilic amide in its structure.
- Another compound (compound 17) exhibited strong antiviral effects, effective absorption in the body, and low clearance rates in rat studies.
HIV-1 integrase (IN) is an essential enzyme for viral replication. Non-catalytic site integrase inhibitors (NCINIs) are allosteric HIV-1 IN inhibitors and a potential new class of antiretrovirals. In this report, we identified a novel NCINI, JTP-0157602, with an original scaffold.
View Article and Find Full Text PDFIntegrase (IN), an essential enzyme of human immunodeficiency virus (HIV), is an attractive antiretroviral drug target. The antiviral activity and resistance profile in vitro of a novel IN inhibitor, elvitegravir (EVG) (also known as JTK-303/GS-9137), currently being developed for the treatment of HIV-1 infection are described. EVG blocked the integration of HIV-1 cDNA through the inhibition of DNA strand transfer.
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