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Optimizing the Multimerization Properties of Quinoline-Based Allosteric HIV-1 Integrase Inhibitors

التفاصيل البيبلوغرافية
العنوان: Optimizing the Multimerization Properties of Quinoline-Based Allosteric HIV-1 Integrase Inhibitors
المؤلفون: Jian Sun, Jacques J. Kessl
المصدر: Viruses, Vol 16, Iss 2, p 200 (2024)
بيانات النشر: MDPI AG, 2024.
سنة النشر: 2024
المجموعة: LCC:Microbiology
مصطلحات موضوعية: HIV, integrase, virus maturation, allosteric integrase inhibitor, ALLINI, quinoline, Microbiology, QR1-502
الوصف: Allosteric HIV-1 Integrase (IN) Inhibitors or ALLINIs bind at the dimer interface of the IN, away from the enzymatic catalytic site, and disable viral replication by inducing over-multimerization of IN. Interestingly, these inhibitors are capable of impacting both the early and late stages of viral replication. To better understand the important binding features of multi-substituted quinoline-based ALLINIs, we have surveyed published studies on IN multimerization and antiviral properties of various substituted quinolines at the 4, 6, 7, and 8 positions. Here we show how the efficacy of these inhibitors can be modulated by the nature of the substitutions at those positions. These features not only improve the overall antiviral potencies of these compounds but also significantly shift the selectivity toward the viral maturation stage. Thus, to fully maximize the potency of ALLINIs, the interactions between the inhibitor and multiple IN subunits need to be simultaneously optimized.
نوع الوثيقة: article
وصف الملف: electronic resource
اللغة: English
تدمد: 16020200
1999-4915
Relation: https://www.mdpi.com/1999-4915/16/2/200; https://doaj.org/toc/1999-4915
DOI: 10.3390/v16020200
URL الوصول: https://doaj.org/article/8be272e2c5b8483b93db95e9e02e3edb
رقم الأكسشن: edsdoj.8be272e2c5b8483b93db95e9e02e3edb
قاعدة البيانات: Directory of Open Access Journals
الوصف
تدمد:16020200
19994915
DOI:10.3390/v16020200