Journal
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
Volume 35, Issue 1, Pages 1555-1561Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1080/14756366.2020.1801674
Keywords
Carbonic anhydrase inhibitors; cancer-related IX and XII isoforms; anticancer agents; screening funnel; enrichment factor
Funding
- Russian Federation Government Mega grant [14.W03.031.0025]
- Russian Foundation for Basic Research [19-33-90017]
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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 thein vitroinhibition 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 thein vitro,in vivoand more recently, in-patient data.
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