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) hCA 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.
journal_name
J Enzyme Inhib Med Chemjournal_title
Journal of enzyme inhibition and medicinal chemistryauthors
Supuran CT,Nocentini A,Yakubova E,Savchuk N,Kalinin S,Krasavin Mdoi
10.1080/14756366.2021.1927007keywords:
["N-acyl sulphonamide prodrug","Non-nucleoside reverse transcriptase inhibitor","elsulfavirine","human carbonic anhydrase","isoform selectivity","neuropathic pain"]subject
Has Abstractpub_date
2021-12-01 00:00:00pages
1056-1060issue
1eissn
1475-6366issn
1475-6374journal_volume
36pub_type
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