Combining carbonic anhydrase and thioredoxin reductase inhibitory motifs within a single molecule dramatically increases its cytotoxicity
A hypothesis that simultaneous targeting cancer-related carbonic anhydrase hCA IX and hCA XII isoforms (whose overexpression is a cancer cell's defence mechanism against hypoxia) along with thioredoxin reductase (overexpressed in cancers as a defence against oxidative stress) may lead to synerg...
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| Main Authors: | , , , , , , , |
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| Format: | Book |
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Taylor & Francis Group,
2020-01-01T00:00:00Z.
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| LEADER | 00000 am a22000003u 4500 | ||
|---|---|---|---|
| 001 | doaj_9fbf8a07c7cf4db2bb258d9ed824a75f | ||
| 042 | |a dc | ||
| 100 | 1 | 0 | |a Mikhail Krasavin |e author |
| 700 | 1 | 0 | |a Tatiana Sharonova |e author |
| 700 | 1 | 0 | |a Vladimir Sharoyko |e author |
| 700 | 1 | 0 | |a Daniil Zhukovsky |e author |
| 700 | 1 | 0 | |a Stanislav Kalinin |e author |
| 700 | 1 | 0 | |a Raivis Žalubovskis |e author |
| 700 | 1 | 0 | |a Tatiana Tennikova |e author |
| 700 | 1 | 0 | |a Claudiu T. Supuran |e author |
| 245 | 0 | 0 | |a Combining carbonic anhydrase and thioredoxin reductase inhibitory motifs within a single molecule dramatically increases its cytotoxicity |
| 260 | |b Taylor & Francis Group, |c 2020-01-01T00:00:00Z. | ||
| 500 | |a 1475-6366 | ||
| 500 | |a 1475-6374 | ||
| 500 | |a 10.1080/14756366.2020.1734800 | ||
| 520 | |a A hypothesis that simultaneous targeting cancer-related carbonic anhydrase hCA IX and hCA XII isoforms (whose overexpression is a cancer cell's defence mechanism against hypoxia) along with thioredoxin reductase (overexpressed in cancers as a defence against oxidative stress) may lead to synergistic antiproliferative effects was confirmed by testing combinations of the two inhibitor classes against pancreatic cancer cells (PANC-1). Combining both pharmacophoric motifs within one molecule led to a sharp increase of cytotoxicity. This preliminary observation sets the ground for a fundamentally new approach to anticancer agent design. | ||
| 546 | |a EN | ||
| 690 | |a anticancer agents | ||
| 690 | |a carbonic anhydrase inhibition | ||
| 690 | |a thioredoxin reductase inhibition | ||
| 690 | |a synergistic effect | ||
| 690 | |a dual pharmacophores | ||
| 690 | |a michael acceptors | ||
| 690 | |a zinc-binding group | ||
| 690 | |a hypoxia | ||
| 690 | |a oxidative stress | ||
| 690 | |a cancer cell defence mechanisms | ||
| 690 | |a Therapeutics. Pharmacology | ||
| 690 | |a RM1-950 | ||
| 655 | 7 | |a article |2 local | |
| 786 | 0 | |n Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 35, Iss 1, Pp 665-671 (2020) | |
| 787 | 0 | |n http://dx.doi.org/10.1080/14756366.2020.1734800 | |
| 787 | 0 | |n https://doaj.org/toc/1475-6366 | |
| 787 | 0 | |n https://doaj.org/toc/1475-6374 | |
| 856 | 4 | 1 | |u https://doaj.org/article/9fbf8a07c7cf4db2bb258d9ed824a75f |z Connect to this object online. |