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 and improvement of anti-cancer properties of second generation antagonists of Mdm2 oncoprotein

2016/21/D/NZ7/00596

Keywords:

Mdm2 p53 drug resistance antagonist tumorigenesis apoptosis cell cycle arrest combined therapy

Descriptors:

  • NZ7_14: Pharmacy, pharmacotherapy, pharmacology
  • NZ1_1: Molecular biology
  • NZ3_3: Apoptosis

Panel:

NZ7 - Diagnostic tools, therapies and public health: public health, epidemiology, environmental health risks and occupational medicine, medical ethics, drug discovery and therapies, pharmacology

Host institution :

Uniwersytet Jagielloński, Wydział Chemii

woj. małopolskie

Other projects carried out by the institution 

Principal investigator (from the host institution):

dr Łukasz Skalniak 

Number of co-investigators in the project: 4

Call: SONATA 11 - announced on 2016-03-15

Amount awarded: 688 320 PLN

Project start date (Y-m-d): 2017-02-06

Project end date (Y-m-d): 2020-02-05

Project duration:: 36 months (the same as in the proposal)

Project status: Project settled

Project description

Download the project description in a pdf file

Note - project descriptions were prepared by the authors of the applications themselves and placed in the system in an unchanged form.

Equipment purchased [PL]

  1. Komora laminarna II klasy bezpieczeństwa mikrobiologicznego.
  2. Komora laminarna II klasy bezpieczeństwa mikrobiologicznego (17 958 PLN)
  3. Zestaw zwiększający możliwości mikroskopu fluorescencyjnego (95 000 PLN)

Information in the final report

  • Publication in academic press/journals (8)
  • Articles in post-conference publications (1)
  1. Helping the Released Guardian: Drug Combinations for Supporting the Anticancer Activity of HDM2 (MDM2) Antagonists
    Authors:
    Kocik J, Machula M, Wisniewska A, Surmiak E, Holak TA, Skalniak L
    Academic press:
    Cancers (Basel) (rok: 2019, tom: 11(7), strony: pii: E1014), Wydawca: MDPI, ST ALBAN-ANLAGE 66, CH-4052 BASEL, SWITZERLAND
    Status:
    Published
    DOI:
    10.3390/cancers11071014 - link to the publication
  2. Multicomponent Peptide Stapling as a Diversity-Driven Tool for the Development of Inhibitors of Protein-Protein Interactions
    Authors:
    Ricardo MG, Ali AM, Plewka J, Surmiak E, Labuzek B, Neochoritis CG, Atmaj J, Skalniak L, Zhang R, Holak TA, Groves M, Rivera DG, Dömling A
    Academic press:
    ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (rok: 2020, tom: 59(13), strony: 5235-5241), Wydawca: WILEY-V C H VERLAG GMBH, POSTFACH 101161, 69451 WEINHEIM, GERMANY
    Status:
    Published
    DOI:
    10.1002/anie.201916257 - link to the publication
  3. A therapeutic patent overview of MDM2/X-Targeted Therapies (2014-2018)
    Authors:
    Skalniak L, Surmial E, Holak TA
    Academic press:
    Expert Opinion On Therapeutic Patents (rok: 2019, tom: 45352, strony: 45311), Wydawca: TAYLOR & FRANCIS LTD, 2-4 PARK SQUARE, MILTON PARK, ABINGDON OR14 4RN, OXON, ENGLAND
    Status:
    Published
    DOI:
    10.1080/13543776.2019.1582645 - link to the publication
  4. Bioactive Macrocyclic Inhibitors of the PD‐1/PD‐L1 Immune Checkpoint
    Authors:
    Magiera-Mularz K, Skalniak L, Zak KM, Musielak B, Rudzinska-Szostak E, Berlicki L, Kocik J, Grudnik P, Sala D, Zarganes‐Tzitzikas T, Shaabani S, Domling A, Dubin G, Holak TA
    Academic press:
    Angewandte Chemie International Edition (rok: 2017, tom: 56, strony: 13732-13735), Wydawca: WILEY-V C H VERLAG GMBH, POSTFACH 101161, 69451 WEINHEIM, GERMANY
    Status:
    Published
    DOI:
    10.1002/anie.201707707 - link to the publication
  5. Fluorinated indole-based MDM2 antagonist selectively inhibits the growth of p53wt osteosarcoma cells
    Authors:
    Skalniak L, Twarda-Clapa A, Neochoritis CG, Surmiak E, Machula M, Wisniewska A, Labuzek B, Ali AM, Krzanik S, Dubin G, Groves M, Dömling A, Holak TA
    Academic press:
    FEBS Journal (rok: 2019, tom: 286(7), strony: 1360-1374), Wydawca: WILEY, 111 RIVER ST, HOBOKEN 07030-5774, NJ USA
    Status:
    Published
    DOI:
    10.1111/febs.14774 - link to the publication
  6. 1,4,5-Trisubstituted Imidazole-Based p53-MDM2/MDMX Antagonists with Aliphatic Linkers for Conjugation with Biological Carriers
    Authors:
    Twarda-Clapa A, Krzanik S, Kubica K, Guzik K, Labuzek B, Neochoritis CG, Khoury K, Kowalska K, Czub M, Dubin G, Dömling A, Skalniak L, Holak TA
    Academic press:
    Journal of Medicinal Chemistry (rok: 2017, tom: 60, strony: 4234-4244), Wydawca: AMER CHEMICAL SOC, 1155 16TH ST, NW, WASHINGTON, DC 20036 USA
    Status:
    Published
    DOI:
    10.1021/acs.jmedchem.7b00104 - link to the publication
  7. Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction
    Authors:
    Neochoritis CG, Atmaj J, Twarda-Clapa A, Surmiak E, Skalniak L, Köhler LM, Muszak D, Kurpiewska K, Kalinowska-Tłuścik J, Beck B, Holak TA, Dömling A
    Academic press:
    European Journal of Medicinal Chemistry (rok: 2019, tom: 182, strony: 111588), Wydawca: ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER, 65 RUE CAMILLE DESMOULINS, CS50083, 92442 ISSY-LES-MOULINEAUX, FRANCE
    Status:
    Published
    DOI:
    10.1016/j.ejmech.2019.111588 - link to the publication
  8. Prolonged Idasanutlin (RG7388) Treatment Leads to the Generation of p53-Mutated Cells
    Authors:
    Skalniak L, Kocik J, Polak J, Skalniak A, Rak M, Wolnicka-Glubisz A, Holak TA
    Academic press:
    Cancers (rok: 2018, tom: 10, strony: 11), Wydawca: MDPI, ST ALBAN-ANLAGE 66, CH-4052 BASEL, SWITZERLAND
    Status:
    Published
    DOI:
    10.3390/cancers10110396 - link to the publication
  1. Insufficient cancer cell elimination by p53-inducer Idasanutlin (R) (RG7388) leads to the generation of secondary drug-resistance
    Authors:
    Skalniak L, Kocik J, Rak M, Holak TA
    Conference:
    The 43'rd FEBS Congress (rok: 2018, ), Wydawca: WILEY, 111 RIVER ST, HOBOKEN 07030-5774, NJ USA
    Data:
    konferencja 7-12 lipca 2018
    Status:
    Published

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