Research output: Contribution to journal › Article › peer-review
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.Research output: Contribution to journal › Article › peer-review
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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