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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

Descriptors

  • ST5_16: Chemia biologiczna
  • NZ1_2: Biochemia
  • ST5_23: Chemia organiczna

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

Voivodeship: małopolskie

Other projects carried out by the institution »

Principal investigator (from the host institution)

prof. Tadeusz Andrzej 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
2013-03-25
Project end date
2018-05-24
Project duration
62 months (the same as in the proposal)
Project status
Project settled

Equipment purchased [PL]

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

Information in the final report

Publication in academic press/journals (18)

  1. 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 (year: 2017, volume: 60, pages: 4234-4244), Publisher: ACS Publications
    Status:
    Published
    DOI:
    10.1021/acs.jmedchem.7b00104 – link to the publication

  2. 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. (year: 2018, volume: 57, pages: 4840-4848), Publisher: Wiley
    Status:
    Published
    DOI:
    10.1002/anie.201710407 – link to the publication

  3. 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 (year: 2017, volume: 8, pages: 72167-72181), Publisher: Impact Journals
    Status:
    Published
    DOI:
    10.18632/oncotarget.20050 – link to the publication

  4. 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 (year: 2016, volume: --, pages: 30323-30335), Publisher: Impact Journals
    Status:
    Published
    DOI:
    10.18632/oncotarget.8730 – link to the publication

  5. 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 (year: 2016, volume: 29, pages: 973-977), Publisher: Taylor & Francis
    Status:
    Published
    DOI:
    10.1080/13543776.2016.1206527 – link to the publication

  6. 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 (year: 2017, volume: 60, pages: 5857-5867), Publisher: ACS Publications
    Status:
    Published
    DOI:
    10.1021/acs.jmedchem.7b00293 – link to the publication

  7. 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 (year: 2015, volume: 23, pages: 2341-2348), Publisher: Cell Press
    Status:
    Published
    DOI:
    10.1016/j.str.2015.09.010 – link to the publication

  8. 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. (year: 2017, volume: 56, pages: 10725-10729), Publisher: Wiley
    Status:
    Published
    DOI:
    10.1002/anie.201704426 – link to the publication

  9. 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. (year: 2018, volume: D74, pages: 695-701), Publisher: Wiley
    Status:
    Published
    DOI:
    10.1107/S2059798318007271 – link to the publication

  10. 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. (year: 2020, volume: 30, pages: 289-298), Publisher: Mary Ann Liebert, Inc.
    Status:
    Published
    DOI:
    10.1089/nat.2019.0833. – link to the publication

  11. 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. (year: 2020, volume: 59, pages: 5235-5241), Publisher: Wiley
    Status:
    Published
    DOI:
    10.1002/anie.201916257. – link to the publication

  12. 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. (year: 2019, volume: 286, pages: 1360-1374), Publisher: FEBS
    Status:
    Published
    DOI:
    10.1111/febs.14774 – link to the publication

  13. 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 (year: 2017, volume: 25, pages: 1163-1174), Publisher: Cell Press
    Status:
    Published
    DOI:
    10.1016/j.str.2017.06.011 – link to the publication

  14. 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. (year: 2019, volume: 1189, pages: 161-174), Publisher: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.molstruc.2019.03.089 – link to the publication

  15. 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. (year: 2018, volume: 82, pages: 284-289), Publisher: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.bioorg.2018.10.043 – link to the publication

  16. 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. (year: 2017, volume: 56, pages: 13732-13735), Publisher: Wiley
    Status:
    Published
    DOI:
    10.1002/anie.201707707 – link to the publication

  17. 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. (year: 2018, volume: 28, pages: 665-678), Publisher: Taylor & Francis
    Status:
    Published
    DOI:
    10.1080/13543776.2018.1512706 – link to the publication

  18. 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 (year: 2018, volume: 10, pages: 396), Publisher: MDPI
    Status:
    Published
    DOI:
    10.3390/cancers10110396 – link to the publication

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