EN
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
Vedoucí skupiny
Skupina Jana Konvalinky
Proteázy lidských patogenů
Kancelář ředitele
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.
Přejít na publikaci arrow
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)
Přejít na publikaci arrow
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)
Přejít na publikaci arrow
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)
Přejít na publikaci arrow
Všechny publikace

Nejnovější publikace

Predicting Effects of Site-Directed Mutagenesis on Enzyme Kinetics by QM/MM and QM Calculations: A Case of Glutamate Carboxypeptidase II
D. Bím M. Navrátil O. Gutten J. Konvalinka Z. Kutil M. Culka V. Navrátil A. Alexandrova C. Bařinka L. Rulíšek
Journal of Physical Chemistry B 126 (1): 132–143 (2022)
Přejít na publikaci arrow
The Development of a High-Affinity Conformation-Sensitive Antibody Mimetic Using a Biocompatible Copolymer Carrier (iBody)
K. Blažková J. Beranová M. Hradilek L. Kostka V. Šubr T. Etrych P. Šácha J. Konvalinka
Journal of Biological Chemistry 297 (5): 101342 (2021)
Přejít na publikaci arrow
Structure-activity relationship and biochemical evaluation of novel fibroblast activation protein and prolyl endopeptidase inhibitors with α-ketoamide warheads
A. Šimková T. Ormsby N. Sidej L. Poštová Slavětínská J. Brynda J. Beranová P. Šácha P. Majer J. Konvalinka
European Journal of Medicinal Chemistry 224: 113717 (2021)
Přejít na publikaci arrow
Synthesis and In Vitro Evaluation of C-7 and C-8 Luteolin Derivatives as Influenza Endonuclease Inhibitors
R. Reiberger K. Radilová M. Král V. Zima P. Majer J. Brynda M. Dračínský J. Konvalinka M. Kožíšek A. Machara
International Journal of Molecular Sciences 22 (14): 7735 (2021)
Přejít na publikaci arrow