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Inhibitory activity against carbonic anhydrase IX and XII as a candidate selection criterion in the development of new anticancer agents. / Krasavin, Mikhail; Kalinin, Stanislav; Sharonova, Tatiana; Supuran, Claudiu T.

In: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol. 35, No. 1, 01.01.2020, p. 1555-1561.

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@article{71a1d9c49d0040c495f9caf4c3018439,
title = "Inhibitory activity against carbonic anhydrase IX and XII as a candidate selection criterion in the development of new anticancer agents",
abstract = "Analysis of the literature data reveals that while inhibition of cancer-related carbonic anhydrase IX and XII isoforms continues to be an important enrichment factor for designing anticancer agent development libraries, exclusive reliance on the in vitro inhibition of these two recombinant isozymes in nominating candidate compounds for evaluation of their effects on cancer cells may lead not only to identifying numerous compounds devoid of the desired cellular efficacy but also to overlooking many promising candidates which may not display the best potency in biochemical inhibition assay. However, SLC-0111, now in phase Ib/II clinical trials, was developed based on the excellent agreement between the in vitro, in vivo and more recently, in-patient data.",
keywords = "anticancer agents, cancer-related IX and XII isoforms, Carbonic anhydrase inhibitors, enrichment factor, screening funnel",
author = "Mikhail Krasavin and Stanislav Kalinin and Tatiana Sharonova and Supuran, {Claudiu T.}",
year = "2020",
month = jan,
day = "1",
doi = "10.1080/14756366.2020.1801674",
language = "English",
volume = "35",
pages = "1555--1561",
journal = "Journal of Enzyme Inhibition and Medicinal Chemistry",
issn = "1475-6366",
publisher = "Taylor & Francis",
number = "1",

}

RIS

TY - JOUR

T1 - Inhibitory activity against carbonic anhydrase IX and XII as a candidate selection criterion in the development of new anticancer agents

AU - Krasavin, Mikhail

AU - Kalinin, Stanislav

AU - Sharonova, Tatiana

AU - Supuran, Claudiu T.

PY - 2020/1/1

Y1 - 2020/1/1

N2 - Analysis of the literature data reveals that while inhibition of cancer-related carbonic anhydrase IX and XII isoforms continues to be an important enrichment factor for designing anticancer agent development libraries, exclusive reliance on the in vitro inhibition of these two recombinant isozymes in nominating candidate compounds for evaluation of their effects on cancer cells may lead not only to identifying numerous compounds devoid of the desired cellular efficacy but also to overlooking many promising candidates which may not display the best potency in biochemical inhibition assay. However, SLC-0111, now in phase Ib/II clinical trials, was developed based on the excellent agreement between the in vitro, in vivo and more recently, in-patient data.

AB - Analysis of the literature data reveals that while inhibition of cancer-related carbonic anhydrase IX and XII isoforms continues to be an important enrichment factor for designing anticancer agent development libraries, exclusive reliance on the in vitro inhibition of these two recombinant isozymes in nominating candidate compounds for evaluation of their effects on cancer cells may lead not only to identifying numerous compounds devoid of the desired cellular efficacy but also to overlooking many promising candidates which may not display the best potency in biochemical inhibition assay. However, SLC-0111, now in phase Ib/II clinical trials, was developed based on the excellent agreement between the in vitro, in vivo and more recently, in-patient data.

KW - anticancer agents

KW - cancer-related IX and XII isoforms

KW - Carbonic anhydrase inhibitors

KW - enrichment factor

KW - screening funnel

UR - http://www.scopus.com/inward/record.url?scp=85088960864&partnerID=8YFLogxK

U2 - 10.1080/14756366.2020.1801674

DO - 10.1080/14756366.2020.1801674

M3 - Article

C2 - 32746643

AN - SCOPUS:85088960864

VL - 35

SP - 1555

EP - 1561

JO - Journal of Enzyme Inhibition and Medicinal Chemistry

JF - Journal of Enzyme Inhibition and Medicinal Chemistry

SN - 1475-6366

IS - 1

ER -

ID: 61393734