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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Kinases of emerging relevance in cancer - structural characterization.

2012/07/E/NZ1/01907

Keywords:

kinases kinase inhibitors X-ray crystallography

Descriptors:

  • NZ1_4: Structural biology
  • NZ1_2: Biochemistry

Panel:

NZ1 - Molecular biology, structural biology, biotechnology: molecular biology, structural biology, biotechnology

Host institution :

Uniwersytet Jagielloński, Wydział Biochemii, Biofizyki i Biotechnologii

woj. małopolskie

Other projects carried out by the institution 

Principal investigator (from the host institution):

dr Grzegorz Dubin 

Number of co-investigators in the project: 5

Call: SONATA BIS 2 - announced on 2012-09-15

Amount awarded: 1 496 600 PLN

Project start date (Y-m-d): 2013-07-11

Project end date (Y-m-d): 2017-07-10

Project duration:: 48 months (the same as in the proposal)

Project status: Project settled

Equipment purchased [PL]

  1. Mieszadło magnetyczne.
  2. Sprzęt obliczeniowy (4 500 PLN)
  3. Zestaw do elektroforezy białek (7 500 PLN)
  4. Zestaw pipet laboratoryjnych (8 000 PLN)
  5. Zestaw kolumn chromatograficznych (18 000 PLN)

Information in the final report

  • Publication in academic press/journals (10)
  1. Crystal structure of Maternal Embryonic Leucine Zipper Kinase (MELK) in complex with dorsomorphin (Compound C)
    Authors:
    Rembacz, K. P., Zrubek, K. M., Golik, P., Michalik, K., Bogusz, J., Wladyka, B., Romanowska, M., Dubin, G.
    Academic press:
    Archives of Biochemistry and Biophysics (rok: 2019, tom: 671, strony: 45298), Wydawca: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.abb.2019.05.014 - link to the publication
  2. Structural basis for ADP-dependent glucokinase inhibition by 8-bromo-substituted adenosine nucleotide
    Authors:
    Grudnik, P., Kaminski, M. M., Rembacz, K. P., Kuska, K., Madej, M., Potempa, J., Dawidowski, M., Dubin, G.
    Academic press:
    Journal of Biological Chemistry (rok: 2018, tom: 293, strony: 11088-11099), Wydawca: American Society for Biochemistry and Molecular Biology
    Status:
    Published
    DOI:
    10.1074/jbc.RA117.001562 - link to the publication
  3. A novel, dual pan-PIM/FLT3 inhibitor SEL24 exhibits broad therapeutic potential in acute myeloid leukemia
    Authors:
    Czardybon, W., Windak, R., Golas, A., Galezowski, M., Sabiniarz, A., Dolata, I., Salwinska, M., Guzik, P., Zawadzka, M., Gabor-Worwa, E., Winnik, B., Zurawska, M., Kolasinska, E., Wincza, E., Bugaj, M., Danielewicz, M., Majewska, E., Mazan, M., Dubin, G., Noyszewska-Kania, M., Jablonska, E., Szydlowski, M., Sewastianik, T., Pula, B., Szumera-Cieckiewicz, A., Prochorec-Sobieszek, M., Madro, E., Lech-Maranda, E., Warzocha, K., Tamburini, J., Juszczynski, P., Brzozka, K.
    Academic press:
    Oncotarget (rok: 2018, tom: 9, strony: 16917-16931), Wydawca: Impact Journals
    Status:
    Published
    DOI:
    10.18632/oncotarget.24747 - link to the publication
  4. Bioactive Macrocyclic Inhibitors of the PD-1/PD-L1 Immune Checkpoint
    Authors:
    Magiera-Mularz, K., Skalniak, L., Zak, K. M., Musielak, B., Rudzinska-Szostak, E., Berlicki, L., Kocik, J., Grudnik, P., Sala, D., Zarganes-Tzitzikas, T., Shaabani, S., Domling, A., Dubin, G., Holak, T. A.
    Academic press:
    Angewandte Chemie International Edition (rok: 2017, tom: 56, strony: 13732-13735), Wydawca: Wiley
    Status:
    Published
    DOI:
    10.1002/anie.201707707 - link to the publication
  5. Small-Molecule Inhibitors of the Programmed Cell Death-1/Programmed Death-Ligand 1 (PD-1/PD-L1) Interaction via Transiently Induced Protein States and Dimerization of PD-L1.
    Authors:
    Guzik, K., Zak, K. M., Grudnik, P., Magiera, K., Musielak, B., Torner, R., Skalniak, L., Domling, A., Dubin, G., Holak, T. A.
    Academic press:
    Journal of Medicinal Chemistry (rok: 2017, tom: 60, strony: 5857-5867), Wydawca: American Chemical Society
    Status:
    Published
    DOI:
    10.1021/acs.jmedchem.7b00293 - link to the publication
  6. Structural basis for small molecule targeting of the programmed death ligand 1 (PD-L1).
    Authors:
    Zak, K. M., Grudnik, P., Guzik, K., Zieba, B. J., Musielak, B., Domling, A., Dubin, G., Holak, T. A.
    Academic press:
    Oncotarget (rok: 2016, tom: 7, strony: 30323-30335), Wydawca: Impact Journals
    Status:
    Published
    DOI:
    10.18632/oncotarget.8730 - link to the publication
  7. Structural biology of the immune checkpoint receptor PD-1 and its ligands PD-L1/PD-L2.
    Authors:
    Zak, K. M., Grudnik, P., Magiera, K., Domling, A., Dubin, G., Holak, T. A.
    Academic press:
    Structure (rok: 2017, tom: 25, strony: 1163-1174), Wydawca: Cell Press
    Status:
    Published
    DOI:
    10.1016/j.str.2017.06.011 - link to the publication
  8. Structural analysis of PIM1 kinase complexes with ATP-competitive inhibitors.
    Authors:
    Bogusz, J., Zrubek, K., Rembacz, K. P., Grudnik, P., Golik, P., Romanowska, M., Wladyka, B., Dubin, G.
    Academic press:
    Scientific Reports (rok: 2017, tom: 7, strony: 13399-13409), Wydawca: Nature Publishing Group
    Status:
    Published
    DOI:
    10.1038/s41598-017-13557-z - link to the publication
  9. Crystal structure of ADP-dependent glucokinase from Methanocaldococcus jannaschii in complex with 5-iodotubercidin reveals phosphoryl transfer mechanism
    Authors:
    Tokarz, P., Wisniewska, M., Kaminski, M. M., Dubin, G., Grudnik, P.
    Academic press:
    Protein Science (rok: 2018, tom: 27, strony: 790-797), Wydawca: Wiley
    Status:
    Published
    DOI:
    10.1002/pro.3377 - link to the publication
  10. Small-molecule inhibitors of PD-1/PD-L1 immune checkpoint alleviate the PD-L1-induced exhaustion of T-cells.
    Authors:
    Skalniak, L., Zak, K. M., Guzik, K., Magiera, K., Musielak, B., Pachota, M., Szelazek, B., Kocik, J., Grudnik, P., Tomala, M., Krzanik, S., Pyrc, K., Domling, A., Dubin, G., Holak, T. A.
    Academic press:
    Oncotarget (rok: 2017, tom: 8, strony: 72167-72181), Wydawca: Impact Journals
    Status:
    Published
    DOI:
    10.18632/oncotarget.20050 - link to the publication

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