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Pavlína Maloy Řezáčová

Pavlína Maloy Řezáčová

mail pavlina.rezacovainvalid-email-name@invalid-email-domainuochb.cas.cz
phone +420 220 183 144
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Pavlína Maloy Řezáčová Group
Structural Biology
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Selected papers

Sulfonamido carboranes as highly selective inhibitors of cancer-specific carbonic anhydrase IX
Sulfonamido carboranes as highly selective inhibitors of cancer-specific carbonic anhydrase IX
J. Štěpánková M. Kugler J. Holub V. Šícha V. Das J. Nekvinda S. El Anwar M. Havránek K. Pospíšilová M. Fábry V. Král M. Medvedíková S. Matějková B. Lišková S. Gurská P. Džubák J. Brynda M. Hajdúch B. Grüner P. Řezáčová
European Journal of Medicinal Chemistry 200: 112460 (2020)
Carbonic anhydrase IX (CA IX) is a transmembrane enzyme overexpressed in hypoxic tumors, where it plays an important role in tumor progression. Specific CA IX inhibitors potentially could serve as anti-cancer drugs. We designed a series of sulfonamide inhibitors containing carborane clusters based on prior structural knowledge of carborane binding into the enzyme active site. Two types of carborane clusters, 12-vertex dicarba-closo-dodecaborane and 11-vertex 7,8-dicarba-nido-undecaborate (dicarbollide), were connected to a sulfonamide moiety via aliphatic linkers of varying lengths (1–4 carbon atoms; n = 1–4). In vitro testing of CA inhibitory potencies revealed that the optimal linker length for selective inhibition of CA IX was n = 3. A 1-sulfamidopropyl-1,2-dicarba-closo-dodecaborane (3) emerged as the strongest CA IX inhibitor from this series, with a Ki value of 0.5 nM and roughly 1230-fold selectivity towards CA IX over CA II. X-ray studies of 3 yielded structural insights into…
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Latest publications

Imidazo[1,2-c]pyrimidin-5(6H)-one inhibitors of CDK2: Synthesis, kinase inhibition and co-crystal structure
J. Jansa R. Jorda J. Škerlová P. Pachl M. Peřina E. Řezníčková T. Heger T. Gucký P. Maloy Řezáčová A. Lyčka V. Kryštof
European Journal of Medicinal Chemistry 216: 113309 (2021)
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N-Glycosylation can selectively block or foster different receptor–ligand binding modes
J. Vuorio J. Škerlová M. Fábry V. Veverka I. Vattulainen P. Řezáčová H. Martinez-Seara
Scientific Reports 11: 5239 (2021)
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Cobalt Bis(dicarbollide) Alkylsulfonamides: Potent and Highly Selective Inhibitors of Tumor Specific Carbonic Anhydrase IX
B. Grüner M. Kugler S. El Anwar J. Holub J. Nekvinda D. Bavol Z. Růžičková K. Pospíšilová M. Fábry V. Král J. Brynda P. Řezáčová
ChemPlusChem 86 (3): 352-363 (2021)
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