Laboratory of Medicinal Chemistry

dr Dorota Jakubczyk

Head of Laboratory

djakubczyk@ibch.poznan.pl
ext. 1184

Research Projects

Keywords:

Medicinal chemistry
“Hit to lead” – molecules optimisation
Chemical Synthesis
Biosynthesis, biocatalysis, semi-synthesis
Isolation and identification of products
Natural products
Chemoinformatics

Offer

Chemical synthesis of bioactive molecules
“Hit to lead” – molecules optimisation – chemoinformatic design and the synthesis
Biosynthesis, biocatalysis, semi-synthesis for compounds difficult to synthesise using classical synthetic chemistry
Selection of already existing libraries for bioactivity tests
Automated isolation and purification of chemical compounds - from biological material or enzymatic reactions

Equipment

Chromatograph Flash Agilent Technologies 971-FP
LCMS-8040 Shimadzu
HPLC semi-preparative Thermo Scientific UltiMate 3000

Projekty badawcze

Preliminary research on the chemical programming of fungi using Ramularia collo-cygni as a model. The aim of the project was to create and optimise a method for producing new analogues of fungal metabolites with potential bioactivity. Preliminary results on the biosynthetic pathways of rubellin metabolites were confirmed by spectral observation of the key intermediate, chrysophanol, which was recently published. Several new rubellin derivatives have also been observed - Miniatura 4 - 2020/04/X/NZ1/01959 (PI dr. Dorota Jakubczyk)

Selected publications

Dussart F., Jakubczyk D.*, Biosynthesis of Rubellins in Ramularia collo-cygni — Genetic Basis and Pathway Proposition. Int. J. Mol. Sci. (2022), 23, 3475
Baud D., Ladkau N., Moody T.S., Ward J.M., Hailes H.C., Stereoselective transaminase-mediated synthesis of serotonin and melatonin receptor agonists. Adv. Syn. Cat. (2022), 364, 1564
Jakubczyk D.*, Francois D. Selected Fungal Natural Products with Antimicrobial Properties. Molecules (2020), 25, 911: 1-18
Gavara L., Sevaille L., De Luca F., Mercuri P., Bebrone C., Feller G., Legru A., Cerboni G., Tanfoni S., Baud D., Cutolo G., Bestgen B., Chelini G., Verdirosa F., Sannio F., Pozzi C., Benvenuti M., Kwapien K., Fischer M., Becker K., Frère J-M. , Mangani S., Gresh N., Berthomieu D., Galleni M., Docquier J-D., Hernandez J-F., 4-Amino-1,2,4-triazole-3-thione-derived Schiff bases as metallo-β-lactamase inhibitors. Eur. J. Med. Chem. (2020), 15, 208
Jakubczyk D., Caputi L., Stevenson C. E. M., Lawson D. M., O’Connor S. E. Structural characterization of EasH (Aspergillus japonicus) – an oxidase involved in cycloclavine biosynthesis. Chem. Comm. (2016) 52: 14306-14309
Jakubczyk D., O’Connor S. E. Privileged scaffolds in medicinal chemistry: Design, synthesis, evaluation. The Royal Society of Chemistry (2016) Chapter 14: Ergot Alkaloids
Baud D., Ladkau N., Moody T.S., Ward J.M., Hailes H.C., A rapid, sensitive colorimetric assay for the high-throughput screening of transaminases in liquid or solid-phase. Chem. Comm. (2015), 51, 17225
Jakubczyk D., Caputi L., Hatsch A., Nielsen C. A. F., Diefenbacher M., Klein J., Molt A., Schroeder H., Cheng J. Z., Naesby M., O’Connor S. E. Discovery and reconstitution of the cycloclavine biosynthetic pathway — enzymatic formation of a cyclopropyl group. Angew. Chem. Int. Ed. (2015) 54: 5117 –5121
Baud D., Saaidi P.L., Monfleur A., Harari M., Cuccaro J., Fossey A., Besnard M., Debard A., Mariage A., Pellouin V., Petit J.L., Salanoubat M., Weissenbach J., de Berardinis V. et Zaparucha A.,Synthesis of mono- and dihydroxylated amino acids with new -ketoglutarate-dependent dioxygenases: Biocatalytic Oxidation of C-H bonds. ChemCatChem (2014), 6, 3012
Jakubczyk D., Cheng J. Z., O'Connor S. E. Biosynthesis of the ergot alkaloids. Nat. Prod. Rep. (2014) 31: 1328-1338
Jakubczyk D., Brenner-Weiß G., Bräse S. Synthesis of tritium labelled and photoactivatable N-acyl-L-homoserine lactones: Inter-kingdom signalling molecules. Eur. J. Org. Chem. (2014) 3: 592–597

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