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Prof. RNDr. Jan Konvalinka, CSc.

Prof. RNDr. Jan Konvalinka, CSc.

mail jan.konvalinkainvalid-email-name@invalid-email-domainuochb.cas.cz
phone +420 220 183 333
Ředitel ústavu
Vedoucí skupiny
Skupina Jana Konvalinky
Proteázy lidských patogenů
Všechny publikace

Vybrané publikace

Identification of Protein Targets of Bioactive Small Molecules Using Randomly Photomodified Probes
Identification of Protein Targets of Bioactive Small Molecules Using Randomly Photomodified Probes
P. Šimon T. Knedlík K. Blažková P. Dvořáková A. Březinová L. Kostka V. Šubr J. Konvalinka P. Šácha
ACS Chemical Biology 13 (12): 3333-3342 (2018)
Identifying protein targets of bioactive small molecules often requires complex, lengthy development of affinity probes. We present a method for stochastic modification of small molecules of interest with a photoactivatable phenyldiazirine linker. The resulting isomeric mixture is conjugated to a hydrophilic copolymer decorated with biotin and a fluorophore. We validated this approach using known inhibitors of several medicinally relevant enzymes. At least a portion of the stochastic derivatives retained their binding to the target, enabling target visualization, isolation, and identification. Moreover, the mix of stochastic probes could be separated into fractions and tested for binding affinity. The structure of the active probe could be determined and the probe resynthesized to improve binding efficiency. Our approach can thus enable rapid target isolation, identification, and visualization, while providing information required for subsequent synthesis of an optimized probe.
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DNA-linked Inhibitor Antibody Assay (DIANA) for sensitive and selective enzyme detection and inhibitor screening
V. Navrátil J. Schimer J. Tykvart T. Knedlík V. Vik P. Majer J. Konvalinka P. Šácha
Nucleic Acids Research 45 (2): e10 (2017)
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DNA-linked inhibitor antibody assay (DIANA) as a new method for screening influenza neuraminidase inhibitors
M. Kožíšek V. Navrátil K. Rojíková J. Pokorná C. Berenguer Albinana P. Pachl J. Zemanová A. Machara P. Šácha P. M. Hudlický P. Řezáčová J. Konvalinka
Biochemical Journal 475 (23): 3847-3860 (2018)
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iBodies: Modular Synthetic Antibody Mimetics Based on Hydrophilic Polymers Decorated with Functional Moieties
P. Šácha T. Knedlík J. Schimer J. Tykvart J. Parolek V. Navrátil P. Dvořáková F. Sedlák K. Ulbrich J. Strohalm P. Majer V. Šubr J. Konvalinka
Angewandte Chemie International Edition 55 (7): 2356-2360 (2016)
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Nejnovější publikace

3′-Dehydroxypurpurogallin-4-Carboxamides as Influenza A Endonuclease Inhibitors: Synthesis, Structure-Activity Relationship Analysis, and Structural Characterization of Protein Complex
M. Kráľ T. Kotačka R. Reiberger G. Panýrková K. Radilová Z. Osifová M. Flieger J. Konvalinka P. Majer M. Kožíšek A. Machara
ChemMedChem 2024: Early View
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Sensitive quantification of fibroblast activation protein and high-throughput screening for inhibition by FDA-approved compounds
K. Čermáková A. Šimková F. Wichterle R. Kryštůfek J. Staňurová Z. Vaníčková P. Bušek J. Konvalinka P. Šácha
European Journal of Medicinal Chemistry 280: 116948 (2024)
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