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

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 i...

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Autores principales: Supuran, Claudiu T., Nocentini, Alessio, Yakubova, Elena, Savchuk, Nikolay, Kalinin, Stanislav, Krasavin, Mikhail
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Taylor & Francis 2021
Materias:
Research Paper
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8143618/
https://www.ncbi.nlm.nih.gov/pubmed/34000969
http://dx.doi.org/10.1080/14756366.2021.1927007
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author Supuran, Claudiu T.
Nocentini, Alessio
Yakubova, Elena
Savchuk, Nikolay
Kalinin, Stanislav
Krasavin, Mikhail
author_facet Supuran, Claudiu T.
Nocentini, Alessio
Yakubova, Elena
Savchuk, Nikolay
Kalinin, Stanislav
Krasavin, Mikhail
author_sort Supuran, Claudiu T.
collection PubMed
description 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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spelling pubmed-81436182021-06-07 Biochemical profiling of anti-HIV prodrug Elsulfavirine (Elpida(®)) and its active form VM1500A against a panel of twelve human carbonic anhydrase isoforms Supuran, Claudiu T. Nocentini, Alessio Yakubova, Elena Savchuk, Nikolay Kalinin, Stanislav Krasavin, Mikhail J Enzyme Inhib Med Chem Research Paper 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. Taylor & Francis 2021-05-17 /pmc/articles/PMC8143618/ /pubmed/34000969 http://dx.doi.org/10.1080/14756366.2021.1927007 Text en © 2021 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. https://creativecommons.org/licenses/by/4.0/This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) ), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Research Paper
Supuran, Claudiu T.
Nocentini, Alessio
Yakubova, Elena
Savchuk, Nikolay
Kalinin, Stanislav
Krasavin, Mikhail
Biochemical profiling of anti-HIV prodrug Elsulfavirine (Elpida(®)) and its active form VM1500A against a panel of twelve human carbonic anhydrase isoforms
title Biochemical profiling of anti-HIV prodrug Elsulfavirine (Elpida(®)) and its active form VM1500A against a panel of twelve human carbonic anhydrase isoforms
title_full Biochemical profiling of anti-HIV prodrug Elsulfavirine (Elpida(®)) and its active form VM1500A against a panel of twelve human carbonic anhydrase isoforms
title_fullStr Biochemical profiling of anti-HIV prodrug Elsulfavirine (Elpida(®)) and its active form VM1500A against a panel of twelve human carbonic anhydrase isoforms
title_full_unstemmed Biochemical profiling of anti-HIV prodrug Elsulfavirine (Elpida(®)) and its active form VM1500A against a panel of twelve human carbonic anhydrase isoforms
title_short Biochemical profiling of anti-HIV prodrug Elsulfavirine (Elpida(®)) and its active form VM1500A against a panel of twelve human carbonic anhydrase isoforms
title_sort biochemical profiling of anti-hiv prodrug elsulfavirine (elpida(®)) and its active form vm1500a against a panel of twelve human carbonic anhydrase isoforms
topic Research Paper
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8143618/
https://www.ncbi.nlm.nih.gov/pubmed/34000969
http://dx.doi.org/10.1080/14756366.2021.1927007
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