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

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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.

в: Journal of Enzyme Inhibition and Medicinal Chemistry, Том 36, № 1, 2021, стр. 1056-1060.

Результаты исследований: Научные публикации в периодических изданиях › статья › Рецензирование

BibTeX

@article{a1f951fae0104def8b286d859aefd27a,

title = "Biochemical profiling of anti-HIV prodrug Elsulfavirine (Elpida{\textregistered}) and its active form VM1500A against a panel of twelve human carbonic anhydrase isoforms",

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{\textregistered}). 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{\textregistered} in patients may help alleviate this debilitating symptom.",

keywords = "elsulfavirine, human carbonic anhydrase, isoform selectivity, N-acyl sulphonamide prodrug, neuropathic pain, Non-nucleoside reverse transcriptase inhibitor, DESIGN, PROTEIN, CRYSTAL-STRUCTURE, SULFONAMIDES, IX, MOLECULES, REVERSE-TRANSCRIPTASE INHIBITORS, SELECTIVITY, INSIGHTS",

author = "Supuran, {Claudiu T.} and Alessio Nocentini and Elena Yakubova and Nikolay Savchuk and Stanislav Kalinin and Mikhail Krasavin",

year = "2021",

doi = "10.1080/14756366.2021.1927007",

language = "English",

volume = "36",

pages = "1056--1060",

journal = "Journal of Enzyme Inhibition and Medicinal Chemistry",

issn = "1475-6366",

publisher = "Taylor & Francis",

number = "1",

}

RIS

TY - JOUR

T1 - Biochemical profiling of anti-HIV prodrug Elsulfavirine (Elpida®) and its active form VM1500A against a panel of twelve human carbonic anhydrase isoforms

AU - Supuran, Claudiu T.

AU - Nocentini, Alessio

AU - Yakubova, Elena

AU - Savchuk, Nikolay

AU - Kalinin, Stanislav

AU - Krasavin, Mikhail

PY - 2021

Y1 - 2021

N2 - 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.

AB - 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.

KW - elsulfavirine

KW - human carbonic anhydrase

KW - isoform selectivity

KW - N-acyl sulphonamide prodrug

KW - neuropathic pain

KW - Non-nucleoside reverse transcriptase inhibitor

KW - DESIGN

KW - PROTEIN

KW - CRYSTAL-STRUCTURE

KW - SULFONAMIDES

KW - IX

KW - MOLECULES

KW - REVERSE-TRANSCRIPTASE INHIBITORS

KW - SELECTIVITY

KW - INSIGHTS

UR - http://www.scopus.com/inward/record.url?scp=85106314106&partnerID=8YFLogxK

U2 - 10.1080/14756366.2021.1927007

DO - 10.1080/14756366.2021.1927007

M3 - Article

C2 - 34000969

AN - SCOPUS:85106314106

VL - 36

SP - 1056

EP - 1060

JO - Journal of Enzyme Inhibition and Medicinal Chemistry

JF - Journal of Enzyme Inhibition and Medicinal Chemistry

SN - 1475-6366

IS - 1

ER -

ID: 77796982