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Prof. Jan Konvalinka

Prof. Jan Konvalinka

mail jan.konvalinkainvalid-email-name@invalid-email-domainuochb.cas.cz
telefon +420 220 183 333
Group leader
Jan Konvalinka Group
Proteases of Human Pathogens
All publications

Selected papers

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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All publications

Latest publications

Potent Competitive Inhibitors of Ecto-5′-nucleotidase (CD73) based on 6-(Het)aryl-7-deazapurine Ribonucleoside 5′-O-Bisphosphonates
U. Šinkevičiüté M. Šímová R. Staník L. Poštová Slavětínská K. Blažková P. Šácha M. Lepšík J. Řezáč J. Konvalinka T. Ormsby M. Tichý M. Hocek
ACS Pharmacology & Translational Science 2025: Early View
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Targeting the Rift Valley Fever Virus Polymerase: Resistance Mechanisms and Structural Insights
M. Kráľ A. Das T. Kotačka A. Blahošová V. Liščáková J. Hodek J. Konvalinka G. Demo M. Kožíšek
ACS Infectious Diseases 11 (11): 3364–3376 (2025)
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Identification of 6-Aryl-7-Deazapurine Ribonucleoside Phosphonates as Inhibitors of Ecto-5′-Nucleotidase (CD73)
M. Šímová T. Ormsby U. Šinkevičiüté L. Sirotová Veselovská K. Čermáková M. Hadzima L. Bartoň J. Staňurová A. Kramná P. Šácha M. Tichý M. Hocek J. Konvalinka K. Blažková
ACS Pharmacology & Translational Science 8 (8): 2575–2585 (2025)
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