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doc. RNDr. Pavlína Maloy Řezáčová, PhD

doc. RNDr. Pavlína Maloy Řezáčová, PhD

mail pavlina.rezacovainvalid-email-name@invalid-email-domainuochb.cas.cz
phone +420 220 183 144
Vedoucí skupiny
Skupina Pavlíny Maloy Řezáčové
Strukturní biologie
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Vybrané publikace

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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Protein crystallization and structure determination at room temperature in the CrystalChip
P. Pachl L. Coudray R. Vincent L. Nilles H. Scheer C. Ritzenthaler A. Fejfarová P. Řezáčová S. Engilberge C. Sauter
FEBS Open Bio 2024: Early View
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Practical courses on advanced methods in macromolecular crystallization: 20 years of history and future perspectives
J. Havlíčková J. A. Gavira J. R. Mesters A. Koutská B. Kaščáková T. Prudnikova R. Hilgenfeld J. M. Garcia-Ruiz P. Řezáčová I. Kutá Smatanová
Journal of Applied Crystallography 57 (Part 5): 1609-1617 (2024)
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Structure and function of bacterial transcription regulators of the SorC family
M. Šoltysová P. Řezáčová
Transcription 2024: Early View
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ABNOH-Linked Nucleotides and DNA for Bioconjugation and Cross-linking with Tryptophan-Containing Peptides and Proteins
A. Spampinato D. L. Leone R. Pohl J. Tarábek M. Šoltysová M. Polák A. Kádek V. Sýkorová P. Řezáčová M. Hocek
Chemistry - A European Journal 30 (49): e202402151 (2024)
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