Bioorganic and medicinal chemistry of nucleic acids
Head: Michal Hocek
Prague node
HOME INSTITUTION
Institute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences
RESEARCH PROGRAMME(S)
RP 1 - Molecular basis of cancer and molecular targets
RP 2 - Research and development of anticancer pharmaceuticals and therapeutic methods
Chemistry for Biology and Medicine!
- Mission: Chemical synthesis, medicinal chemistry and chemical biology for therapy and diagnostics of tumors.
- Vision: Develop small molecule and oligonucleotide therapeutics and probes for diagnostics of cancer.
The Hocek group is dealing with the design and synthesis of modified heterocycles, nucleosides, nucleotides and oligonucleotides. In medicinal chemistry we are particularly interested in development of novel potential small molecule cytostatics based on heterocyclic enzyme inhibitors, nucleosides and nucleotide prodrugs, as well as in development of oligonucleotide and nucleic acid therapeutics targeting cancer. In chemical biology we design and synthesize modified nucleotide and nucleic acid probes for studying key biological processes and for imaging and bioanalysis of nucleic acids in live cells and for applications in diagnostics.
SELECTED PUBLICATIONS
- Yang, Ch.; Slavĕtínská Poštová, L.; Fleuti, M.; Klepetářová, B.; Tichý, M.; Gurská, S.; Pavliš, P.; Džubák, P.; Hajdúch, M. and Hocek, M.: Synthesis of Polycyclic Hetero-Fused 7-Deazapurine Heterocycles and Nucleosides through C–H Dibenzothiophenation and Negishi Coupling. J. Am. Chem. Soc. 2022, 144 (42), 19437-19446. DOI: 10.1021/jacs.2c07517
- Vavřina, Z.; Perlíková, P.; Milisavljevic, N.; Chevrier, F.; Smola, M.; Smith, J.; Dejmek, M.; Havlíček, V.; Budešínský, M.; Liboska, R.; Vaneková, L.; Brynda, J.; Bouřa, E.; Řezáčová, P.; Hocek, M. and Birkuš,G.: Design, Synthesis, and Biochemical and Biological Evaluation of Novel 7-Deazapurine Cyclic Dinucleotide Analogues as STING Receptor Agonists. J. Med. Chem. 2022, 65 (20), 14082-14103. DOI: 10.1021/acs.jmedchem.2c01305
- Ortiz, M.; Jauset-Rubio, M.; Kodr, D.; Simonova, A.; Hocek, M.; O´Sullivan, C. K.: Solid-phase recombinase polymerase amplification using ferrocene-labelled dNTPs for electrochemical detection of single nucleotide polymorphisms. Biosens. Bioelectron. 2022, 198, 113825. DOI: 10.1016/j.bios.2021.113825
- Yang, C.; Tichý, M.; Poštová Slavĕtínská, L.; Vaiedelich, E.; Gurská, S.; Džubák, P.; Hajdúch, M.; Hocek, M.: Synthesis and Biological Profiling of Benzofuro-Fused 7-Deazapurine Nucleosides. Eur. J. Org. Chem. 2023, e202300723. DOI: 10.1002/ejoc.202300723
- Fleuti, M.; Sanchez-Quirante, T.; Poštová Slavĕtínská, L.; Tloušťová, E.; Tichý, M.; Gurská, S.; Džubák, P.; Hajdúch, M. and Hocek, M.: Synthesis and Biological Profiling of Quinolino-Fused 7-Deazapurine Nucleosides. ACS Omega 2024, 9, 20557–20570. DOI: 10.1021/acsomega.4c02031
COLLABORATION WITHIN THE NICR
Marián Hajdúch
(Olomouc node, Faculty of Medicine PU in Olomouc)
Martin Mistrík
(Olomouc node, Faculty of Medicine PU in Olomouc)
Pavel Klener
(Prague node, First Faculty of Medicine CU)
Pavlína Maloy Řezáčová
(Prague node, Institute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences)
Petr Džubák
(Olomouc node, Faculty of Medicine PU in Olomouc)
Tomáš Etrych
(Prague node, Institute of Macromolecular Chemistry of the Czech Academy of Sciences)
Zuzana Kečkéšová
(Prague node, Institute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences)
SPECIALIZED EXPERTISE AND TECHNOLOGY
Chemical synthesis of nucleosides, nucleotides and oligonucleotides
Enzymatic synthesis of modified nucleic acids
Design and synthesis of molecular probes