Projects funded by the NCN

Information on the principal investigator and host institution

Information of the project and the call

Keywords

Equipment

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Synthesis of fluorogenic substrates, inhibitors and activity-based probes of human neutrophil proteinase NSP4 and its evolutionary homologs

2014/15/B/ST5/05311

Keywords:

proteinases fluorogenic substrates irreversible inhibitors activity based probes

Descriptors:

  • ST4_10: Polymer and biopolymer chemistry
  • ST5_16:
  • ST5_9: Biomaterials, biocompatible materials

Panel:

ST5 - Materials: materials synthesis, structure-properties relations, advanced and functional materials with designed properties, (macro)molecular architecture, material engineering

Host institution :

Uniwersytet Gdański, Wydział Chemii

woj. pomorskie

Other projects carried out by the institution 

Principal investigator (from the host institution):

prof. Adam Lesner 

Number of co-investigators in the project: 6

Call: OPUS 8 - announced on 2014-09-15

Amount awarded: 877 040 PLN

Project start date (Y-m-d): 2015-10-01

Project end date (Y-m-d): 2019-03-31

Project duration:: 42 months (the same as in the proposal)

Project status: Project settled

Equipment purchased [PL]

  1. zamrażarka niskotemperaturowa -80 C (50 000 PLN)
  2. System chromatografii HPLC (150 000 PLN)

Information in the final report

  • Publication in academic press/journals (4)
  1. 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
    Authors:
    Carla Guarino, Natalia Gruba, Renata Grzywa, Edyta Dyguda-Kazimierowicz, Yveline Hamon, Monika Łegowska, Marcin Skorenski, Sandrine Dallet-Choisy, Sylvain Marchand-Adam, Christine Kellenberger, Dieter E. Jenne, Marcin Sienczyk, Adam Lesner, Francis Gauthier, Brice Korkmaz
    Academic press:
    Journal of Medicinal Chemistry (rok: 2018, tom: 61, strony: 1858-1870), Wydawca: ACS
    Status:
    Published
    DOI:
    10.1021/acs.jmedchem.7b01416. - link to the publication
  2. PEGylated substrates of NSP4 protease: A tool to study protease specificity
    Authors:
    Magdalena Wysocka, Natalia Gruba, Renata Grzywa, Artur Giełdoń, Remigiusz Bąchor, Krzysztof Brzozowski, Marcin Sieńczyk, Jenne Dieter, Zbigniew Szewczuk, Krzysztof Rolka & Adam Lesner
    Academic press:
    Scientific Reports (rok: 2016, tom: 6, strony: 45302), Wydawca: nature group
    Status:
    Published
    DOI:
    10.1038/srep22856 - link to the publication
  3. Lung Protection by Cathepsin C Inhibition: A New Hope for COVID-19 and ARDS?
    Authors:
    Brice Korkmaz*, Adam Lesner, Sylvain Marchand-Adam, Celia Moss, and Dieter E. Jenne
    Academic press:
    J Med Chem , Wydawca: ACS
    Status:
    Accepted for publication
    DOI:
    10.1021/acs.jmedchem.0c00776 - link to the publication
  4. Structure-based design and in vivo anti-arthritic activity evaluation of a potent dipeptidyl cyclopropyl nitrile inhibitor of cathepsin C.
    Authors:
    Korkmaz B, Lesner A, Wysocka M, Gieldon A, Håkansson M, Gauthier F, Logan DT, Jenne D, Lauritzen C, Pedersen J.
    Academic press:
    Biochemical Pharmacology (rok: 2019, tom: 164, strony: 349-367), Wydawca: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.bcp.2019.04.006 - link to the publication

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