Biochemical profiling of anti-HIV prodrug Elsulfavirine (Elpida®) and its active form VM1500A against a panel of twelve human carbonic anhydrase isoforms. (1st January 2021)

• Record Type: Journal Article
• Authors: Supuran, Claudiu T.; Nocentini, Alessio; Yakubova, Elena; Savchuk, Nikolay; Kalinin, Stanislav; Krasavin, Mikhail
• Is Part Of: Journal of enzyme inhibition and medicinal chemistry. Volume 36:Number 1(2021)
• Page Start: 1056
• Page End: 1060
• Publication Date: 2021-01-01
• Subjects: Non-nucleoside reverse transcriptase inhibitor -- elsulfavirine -- N-acyl sulphonamide prodrug -- human carbonic anhydrase -- isoform selectivity -- neuropathic pain; Enzyme inhibitors -- Periodicals; Enzyme Inhibitors -- periodicals; Biochemistry -- periodicals; 572.7
• DOI: 10.1080/14756366.2021.1927007
• Languages: English
• ISSNs: 1475-6366

Abstract

Abstract: The non-nucleoside reverse transcriptase inhibitor VM1500A is approved for the treatment of HIV/AIDS in its N -acyl sulphonamide prodrug form elsulfavirine (Elpida ® ). Biochemical profiling against twelve human carbonic anhydrase (CA, EC 4.2.1.1) isoforms showed that while elsulfavirine was a weak inhibitor of all isoforms, VM1500A potently and selectively inhibited human (h) h CA VII isoform, a proven target for the therapy of neuropathic pain. The latter is a common neurologic complication of HIV infection and we hypothesise that by using Elpida ® in patients may help alleviate this debilitating symptom. Graphical Abstract: UF0001