ALesner group peptide and proteases

Submitted by adamlesner on Tue, 03/16/2021 - 09:37
Faculty of Chemistry
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PI name
Adam Lesner
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Contact person
Adam Lesner
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Short description of research profile

Main focus on biochemical characteristic of proteolytic enzymes using combinatorial chemistry methods. Design and synthesis of selective substrates of particular protease. Main interest: neutrophil proteases, diagnostic, molecular probes ect. Using our techniques we are able to characterized substrate specificity of any proteolytic enzyme. Also we are involoved in antimcrobial and immunostimulating peptides.

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Representative publications

A Peptidomimetic Fluorescent Probe to Detect the Trypsin β2 Subunit of the Human 20S Proteasome. Wysocka M, Romanowska A, Gruba N, Michalska M, Giełdoń A, Lesner A.Int J Mol Sci. 2020 Mar 31;21(7):2396. doi: 10.3390/ijms21072396.
Structure-based design and in vivo anti-arthritic activity evaluation of a potent dipeptidyl cyclopropyl nitrile inhibitor of cathepsin C. Korkmaz B, Lesner A, Wysocka M, Gieldon A, Håkansson M, Gauthier F, Logan DT, Jenne DE, Lauritzen C, Pedersen J.Biochem Pharmacol. 2019 Jun;164:349-367. doi: 10.1016/j.bcp.2019.04.006.
  Design, Synthesis, and Enzymatic Evaluation of Novel ZnO Quantum Dot-Based Assay for Detection of Proteinase 3 Activity. Popow-Stellmaszyk J, Bajorowicz B, Malankowska A, Wysocka M, Klimczuk T, Zaleska-Medynska A, Lesner A.Bioconjug Chem. 2018 May 16;29(5):1576-1583. doi: 10.1021/acs.bioconjchem.8b00100.
Exploiting the S4-S5 Specificity of Human Neutrophil Proteinase 3 to Improve the Potency of Peptidyl Di(chlorophenyl)-phosphonate Ester Inhibitors: A Kinetic and Molecular Modeling Analysis. Guarino C, Gruba N, Grzywa R, Dyguda-Kazimierowicz E, Hamon Y, Łȩgowska M, Skoreński M, Dallet-Choisy S, Marchand-Adam S, Kellenberger C, Jenne DE, Sieńczyk M, Lesner A, Gauthier F, Korkmaz B.J Med Chem. 2018 Mar 8;61(5):1858-1870. doi: 10.1021/acs.jmedchem.7b01416.
Bladder cancer detection using a peptide substrate of the 20S proteasome. Gruba N, Wysocka M, Brzezińska M, Dębowski D, Sieńczyk M, Gorodkiewicz E, Guszcz T, Czaplewski C, Rolka K, Lesner A.FEBS J. 2016 Aug;283(15):2929-48. doi: 10.1111/febs.13786. Epub 2016 Jul 14.

Link to extended list of publication