Laboratory of Medicinal Chemistry
Head: Milan Jakubek
Prague node
HOME INSTITUTION
First Faculty of Medicine CU
RESEARCH PROGRAMME(S)
RP 3 - Biomarkers of cancers and cancer diagnostics
Today’s research, tomorrow’s cure!
- Mission: Develop innovative therapeutic and diagnostic compounds for the treatment of cancer.
The aim of the group is to identify new treatment goals and design, preparation, characterization and verification of novel unique structural motifs for targeted anticancer therapy and diagnosis. We focus on new pharmacophores based on polymethinium salts (PMS), chelators or hybrid molecules with cytostatic and migrastatic properties (CyMi). The Laboratory of Medicinal Chemistry focuses on the design and synthesis of new diagnostically and therapeutically relevant biologically active organic molecules and nanomaterials for the diagnosis and treatment of various diseases.
SELECTED PUBLICATIONS
- Jakubek M, Kejík Z, Kaplánek R, Antonyová V, Hromádka R, Šandriková V, Sýkora D, Martásek P, Král V. Hydrazones as novel epigenetic modulators: Correlation between TET 1 protein inhibition activity and their iron(II) binding ability. Bioorg Chem. 2019 Jul;88:102809. DOI: 10.1016/j.bioorg.2019.02.034
- Antonyová V, Kejík Z, Brogyanyi T, Kaplánek R, Veselá K, Abramenko N, Ocelka T, Masařík M, Matkowski A, Gburek J, Abel R, Goede A, Preissner R, Novotný P, Jakubek M. Non-psychotropic cannabinoids as inhibitors of TET1 protein. Bioorg Chem. 2022 Jul;124:105793. DOI: 10.1016/j.bioorg.2022.105793
- Fialova JL, Hönigova K, Raudenska M, Miksatkova L, Zobalova R, Navratil J, Šmigová J, Moturu TR, Vicar T, Balvan J, Vesela K, Abramenko N, Kejik Z, Kaplanek R, Gumulec J, Rosel D, Martasek P, Brábek J, Jakubek M, Neuzil J, Masarik M. Pentamethinium salts suppress key metastatic processes by regulating mitochondrial function and inhibiting dihydroorotate dehydrogenase respiration. Biomed Pharmacother. 2022 Oct;154:113582. DOI: 10.1016/j.biopha.2022.113582
- Jakubek M, Kejík Z, Kaplánek R, Hromádka R, Šandriková V, Sýkora D, Antonyová V, Urban M, Dytrych P, Mikula I, Martásek P, Král V. Strategy for improved therapeutic efficiency of curcumin in the treatment of gastric cancer. Biomed Pharmacother. 2019 Oct;118:109278. DOI: 10.1016/j.biopha.2019.109278
- Brogyányi T, Kaplánek R, Kejík Z, Hosnedlová B, Antonyová V, Abramenko N, Veselá K, Martásek P, Vokurka M, Richardson DR, Jakubek M. Azulene hydrazide-hydrazones for selective targeting of pancreatic cancer cells. Biomed Pharmacother. 2022 Nov;155:113736. DOI: 10.1016/j.biopha.2022.113736
COLLABORATION WITHIN THE NICR
Aleksi Šedo
(Prague node, First Faculty of Medicine CU)
Jan Brábek
(Prague node, Faculty of Science CU)
Karel Smetana
(Prague node, First Faculty of Medicine CU)
Marián Hajdúch
(Olomouc node, Faculty of Medicine PU in Olomouc)
Petr Džubák
(Olomouc node, Faculty of Medicine PU in Olomouc)
SPECIALIZED EXPERTISE AND TECHNOLOGY
Organic synthesis
Formulation laboratory
Analytical and bioanalytical laboratory
COLLABORATION WITH LARGE RESEARCH INFRASTRUCTURES AND RESEARCH CENTRES
National infrastructure for translational medicine EATRIS-CZ
National infrastructure for biological and biomedical imaging Czech-Bioimaging
Biotechnology and Biomedicine Centre of the Czech Academy of Sciences and the Charles University BIOCEV
Center for Advanced Preclinical Imaging CAPI