Journal of Enzyme Inhibition and Medicinal Chemistry (Jan 2021)

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

  • Claudiu T. Supuran,
  • Alessio Nocentini,
  • Elena Yakubova,
  • Nikolay Savchuk,
  • Stanislav Kalinin,
  • Mikhail Krasavin

DOI
https://doi.org/10.1080/14756366.2021.1927007
Journal volume & issue
Vol. 36, no. 1
pp. 1056 – 1060

Abstract

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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.

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