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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Characterization of CD44/p53 signaling involved in the CD44-dependent cancer stem cells: small molecules and peptides, their conjugates, off-target binding, and structures of CD44 and Stad2

2012/06/A/ST5/00224

Keywords:

CD44 p53 cancer structure genomics

Descriptors:

  • ST5_16:
  • NZ1_2: Biochemistry
  • ST5_23:

Panel:

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

Host institution :

Uniwersytet Jagielloński, Wydział Chemii

woj. małopolskie

Other projects carried out by the institution 

Principal investigator (from the host institution):

prof. Tadeusz Holak 

Number of co-investigators in the project: 6

Call: MAESTRO 3 - announced on 2012-06-15

Amount awarded: 2 964 988 PLN

Project start date (Y-m-d): 2013-03-25

Project end date (Y-m-d): 2018-05-24

Project duration:: 62 months (the same as in the proposal)

Project status: Project settled

Equipment purchased [PL]

  1. Lampa UV (1 785 PLN)
  2. aparaty do elektroforezy białek i transferu.
  3. mieszadła magnetyczne.
  4. mieszadło hematologiczne.
  5. pompa próżniowa do filtrowania buforów.
  6. wirówka na probówki typu Falcon.
  7. Dewar (3 923 PLN)
  8. aparat do generowania lodu.
  9. lodówka duża.
  10. wytrząsarka kołyskowa.
  11. zestaw do chromatografii FPLC (typu akta).
  12. Licencja Microsoft Office Professional 2016 PL.
  13. Spektrofotometr na małe objętości.
  14. kuchenka mikrofalowa.
  15. zamrażarka duża.
  16. zamrażarka mała.
  17. Spectrofluorometer-reader (Tecan Ultra Evolution 384-plate reader) wraz z robotic sampler (274 992 PLN)
  18. Waga precyzyjna.
  19. Zamrażarka -80oC: (42 000 PLN)
  20. wirówka na probówki typu Eppendorf.
  21. wytrząsarka typu termomixer.
  22. Pipetor (3 512 PLN)
  23. Urządzenie wielofunkcyjne (1 283 PLN)

Information in the final report

  • Publication in academic press/journals (18)
  1. The synthesis and characterization of tetramic acid derivatives as Mdm2-p53 inhibitors
    Authors:
    Muszak, D., Łabuzek., Brela, M.Z., Twarda-Clapa, A., Czub, M., Musielak, B., Ewa Surmiak, E., Holak, T.A.
    Academic press:
    J. Mol. Str. (rok: 2019, tom: 1189, strony: 161-174), Wydawca: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.molstruc.2019.03.089 - link to the publication
  2. A fluorinated indole-based MDM2 antagonist selectively inhibits the growth of p53wt osteosarcoma cells
    Authors:
    Skalniak, L., Twarda-Clapa, A., Neochoritis, C.G, Surmiak, E., Machula, M., Wisniewska, A., Labuzek, B., Ali, A.M., Krzanik, S., Dubin, G., Groves, M., Domling, A., Holak, T.A.
    Academic press:
    FEBS J. (rok: 2019, tom: 286, strony: 1360-1374), Wydawca: FEBS
    Status:
    Published
    DOI:
    10.1111/febs.14774 - link to the publication
  3. A patent review on PD-1/PD-L1 antagonists: small molecules, peptides, and macrocycles (2015-2018)
    Authors:
    Shaabani, S., Huizinga, H.P.S., Butera, R., Kouchi, A., Guzik, K., Magiera-Mularz, K., Holak, T.A., Domling, A.
    Academic press:
    Expert Opin. Therapeutic Pat. (rok: 2018, tom: 28, strony: 665-678), Wydawca: Taylor & Francis
    Status:
    Published
    DOI:
    10.1080/13543776.2018.1512706 - link to the publication
  4. Crystal structure of the FAS1 domain of the hyaluronic acid receptor stabilin-2
    Authors:
    Twarda-Clapa, A., Labuzek, B., Krzemien, D., Musielak, B., Grudnik, P., Dubin, G., Holak, T.A.
    Academic press:
    Acta Cryst. (rok: 2018, tom: D74, strony: 695-701), Wydawca: Wiley
    Status:
    Published
    DOI:
    10.1107/S2059798318007271 - link to the publication
  5. Multicomponent Peptide Stapling as a Diversity‐Driven Tool for the Development of Inhibitors of Protein–Protein Interactions
    Authors:
    18.Manuel G. Ricardo; Ameena M. Ali; Jacek Plewka; Ewa Surmiak; Beata Labuzek; Constantinos G. Neochoritis; Jack Atmaj; Lukasz Skalniak; Ran Zhang; Tad A. Holak; Matthew Groves; Daniel G. Rivera; Alexander Domling
    Academic press:
    Angew. Chem. Int. Ed. (rok: 2020, tom: 59, strony: 5235-5241), Wydawca: Wiley
    Status:
    Published
    DOI:
    10.1002/anie.201916257. - link to the publication
  6. Structure of the Complex of Human Programmed Death-1 (PD-1) and Its Ligand PD-L1
    Authors:
    Krzysztof M. Zak, Radoslaw Kitel, Sara Przetocka, Przemyslaw Golik, Katarzyna Guzik, Bogdan Musielak, Alexander Domling, Grzegorz Dubin, Tad A. Holak
    Academic press:
    Structure (rok: 2015, tom: 23, strony: 2341-2348), Wydawca: Cell Press
    Status:
    Published
    DOI:
    10.1016/j.str.2015.09.010 - link to the publication
  7. 1,4,5-Trisubstituted Imidazole-Based p53-MDM2/MDMX Antagonists with Aliphatic Linkers for Conjugation with Biological Carriers.
    Authors:
    Aleksandra Twarda-Clapa, Sylwia Krzanik, Katarzyna Kubica, Katarzyna Guzik, Beata Labuzek, Constantinos G. Neochoritis, Kareem Khoury, Kaja Kowalska, Miroslawa Czub, Grzegorz Dubin, Alexander Dömling, Lukasz Skalniak, Tad A. Holak
    Academic press:
    Journal of Medicinal Chemistry (rok: 2017, tom: 60, strony: 4234-4244), Wydawca: ACS Publications
    Status:
    Published
    DOI:
    10.1021/acs.jmedchem.7b00104 - link to the publication
  8. NMR fragment-based screening for development of the CD44-binding small molecules
    Authors:
    Marcin Pustuła, Mirosława Czub, Beata Łabuzek, Ewa Surmiak, Marcin Tomala, Aleksandra Twarda-Clapa, Katarzyna Guzik, Grzegorz M. Popowicz, Tad A. Holak
    Academic press:
    Bioorg. Chem. (rok: 2018, tom: 82, strony: 284-289), Wydawca: Elsevier
    Status:
    Published
    DOI:
    10.043 - link to the publication
  9. Prolonged idasanutlin (RG7388) treatment leads to the generation of p53-mutated cells
    Authors:
    Lukasz Skalniak, Justyna Kocik, Justyna Polak, Anna Skalniak, Monika Rak, Agnieszka Wolnicka-Głubisz and Tad A. Holak
    Academic press:
    Cancers (rok: 2018, tom: 10, strony: 396), Wydawca: MDPI
    Status:
    Published
    DOI:
    10.3390/cancers10110396 - link to the publication
  10. Structural Biology of the Immune Checkpoint Receptor PD-1 and Its Ligands PD-L1/PD-L2.
    Authors:
    Krzysztof M. Zak, Przemyslaw Grudnik, Katarzyna Magiera, Alexander Dömling, Grzegorz Dubin, Tadeusz A. Holak
    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
  11. Anti-CD44 DNA aptamers selectively target cancer cells
    Authors:
    Pecak, A., Skalniak, L., Pels, K., Książek, M., Madej, M., Krzemeń, D., Malicki, S., Dubin, A., Holak, T.A., Dubin, D. (2020). Anti-CD44 DNA aptamers selectively target cancer cells.
    Academic press:
    Nucl. Acid Therap. (rok: 2020, tom: 30, strony: 289-298), Wydawca: Mary Ann Liebert, Inc.
    Status:
    Published
    DOI:
    10.1089/nat.2019.0833. - link to the publication
  12. Bioactive Macrocyclic Inhibitors of the PD-1/PD-L1 Immune Checkpoint.
    Authors:
    Katarzyna Magiera-Mularz, Lukasz Skalniak, Krzysztof M. Zak, Bogdan Musielak,Ewa Rudzinska-Szostak, Łukasz Berlicki, Justyna Kocik, Przemyslaw Grudnik, Dominik Sala, Tryfon Zarganes-Tzitzikas, Shabnam Shaabani, Alexander Dömling, Grzegorz Dubin, Tad A. Holak
    Academic press:
    Angew. Chem. Int. Ed. (rok: 2017, tom: 56, strony: 13732-13735), Wydawca: Wiley
    Status:
    Published
    DOI:
    10.1002/anie.201707707 - link to the publication
  13. Immune Checkpoint PD-1/PD-L1: Is There Life Beyond Antibodies?
    Authors:
    Markella Konstantinidou, Tryfon Zarganes-Tzitzikas, Katarzyna Magiera-Mularz, Tad A. Holak, Alexander Dömling
    Academic press:
    Angew. Chem. Int. Ed. (rok: 2018, tom: 57, strony: 4840-4848), Wydawca: Wiley
    Status:
    Published
    DOI:
    10.1002/anie.201710407 - link to the publication
  14. Inhibitors of programmed cell death 1 (PD-1): a patent review (2010-2015).
    Authors:
    Zarganes-Tzitzikas, T., Konstantinidou, M., Gao, Y., Krzemien, D., Zak, K., Dubin, G., Holak, T.A., Domling A
    Academic press:
    Expert. Opin. Therapeutic Patents (rok: 2016, tom: 29, strony: 973-977), Wydawca: Taylor & Francis
    Status:
    Published
    DOI:
    10.1080/13543776.2016.1206527 - link to the publication
  15. 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:
    Katarzyna Guzik, Krzysztof M. Zak, Przemyslaw Grudnik, Katarzyna Magiera, Bogdan Musielak, Ricarda Törner, Lukasz Skalniak, Alexander Dömling, Grzegorz Dubin, Tad A. Holak
    Academic press:
    Journal of Medicinal Chemistry (rok: 2017, tom: 60, strony: 5857-5867), Wydawca: ACS Publications
    Status:
    Published
    DOI:
    10.1021/acs.jmedchem.7b00293 - link to the publication
  16. Small-molecule inhibitors of PD-1/PD-L1 immune checkpoint alleviate the PD-L1-induced exhaustion of T-cells.
    Authors:
    Lukasz Skalniak ,Krzysztof M Zak, Katarzyna Guzik, Katarzyna Magiera, Bogdan Musielak, Magdalena Pachota, Bozena Szelazek, Justyna Kocik, Przemyslaw Grudnik, Marcin Tomala, Sylwia Krzanik, Krzysztof Pyrc, Alexander Dömling, Grzegorz Dubin, Tadeusz A. Holak
    Academic press:
    Oncotarget (rok: 2017, tom: 8, strony: 72167-72181), Wydawca: Impact Journals
    Status:
    Published
    DOI:
    10.18632/oncotarget.20050 - link to the publication
  17. Structural basis for small molecule targeting of the programmed death ligand 1 (PD-L1)
    Authors:
    Krzysztof M. Zak, Przemyslaw Grudnik, Katarzyna Guzik, Bartosz J. Zieba, Bogdan Musielak, Alexander Dömling, Grzegorz Dubin & Tad A. Holak
    Academic press:
    Oncotarget (rok: 2016, tom: --, strony: 30323-30335), Wydawca: Impact Journals
    Status:
    Published
    DOI:
    10.18632/oncotarget.8730 - link to the publication
  18. Two-Step Synthesis of Complex Artificial Macrocyclic Compounds
    Authors:
    Rudrakshula Madhavachary, Eman M. M. Abdelraheem, Arianna Rossetti, Aleksandra Twarda-Clapa, Bogdan Musielak, Katarzyna Kurpiewska, Justyna Kalinowska-Tłuścik, Tad A. Holak, Alexander Dömling
    Academic press:
    Angew Chem Int Ed Engl. (rok: 2017, tom: 56, strony: 10725-10729), Wydawca: Wiley
    Status:
    Published
    DOI:
    10.1002/anie.201704426 - link to the publication

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