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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Design and synthesis of probes for RabGGTase profiling and their application for identification of the site of phosphonocarboxylate inhibitors's interaction with the enzyme and potential off-targets

2014/14/E/ST5/00491

Keywords:

phosphonocarboxylates bioorthogonal chemistry affinity-based probe fluorescent labeling LC MS activity-based protein profiling

Descriptors:

  • ST5_16:
  • ST5_23:

Panel:

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

Host institution :

Politechnika Łódzka, Wydział Chemiczny

woj. łódzkie

Other projects carried out by the institution 

Principal investigator (from the host institution):

dr hab. Katarzyna Błażewska 

Number of co-investigators in the project: 5

Call: SONATA BIS 4 - announced on 2014-06-16

Amount awarded: 1 998 749 PLN

Project start date (Y-m-d): 2015-05-18

Project end date (Y-m-d): 2021-05-17

Project duration:: 72 months (the same as in the proposal)

Project status: Project settled

Equipment purchased [PL]

  1. aparatura do chromatografii typu flash z detekcja UV-Vis i MS (500 000 PLN)
  2. kolumny Superdex (2 szt.) (20 000 PLN)
  3. Wyparka z chłodnicą pionową.
  4. lampa UV do naswietlania 365 nm (7 000 PLN)
  5. liofilizator (62 000 PLN)

Information in the final report

  • Publication in academic press/journals (10)
  1. Synthesis of the 6-Substituted Imidazo[1,2-a]Pyridine-3-yl-2-Phosphonopropionic Acids as Potential Inhibitors of Rab Geranylgeranyl Transferase
    Authors:
    D. Kusy, A. Marchwicka, J. Małolepsza, K. Justyna, E. Gendaszewska-Darmach, K. M. Błażewska
    Academic press:
    Frontiers in Chemistry (rok: 2021, tom: 8, strony: Article 596162), Wydawca: Frontiers
    Status:
    Published
    DOI:
    10.3389/fchem.2020.596162 - link to the publication
  2. Rational design, optimization, and biological evaluation of novel α-Phosphonopropionic acids as covalent inhibitors of Rab geranylgeranyl transferase
    Authors:
    J. Małolepsza, A. Marchwicka, R. A. Serwa, S. P. Niinivehmas, O. T. Pentikäinen, E. Gendaszewska-Darmach, K. M. Błażewska
    Academic press:
    Journal of Enzyme Inhibition and Medicinal Chemistry (rok: 2022, tom: 37, strony: 940-951), Wydawca: Taylor & Francis
    Status:
    Published
    DOI:
    10.1080/14756366.2022.2053525 - link to the publication
  3. Targeting small GTPases and their prenylation in diabetes mellitus
    Authors:
    E. Gendaszewska-Darmach, M. Garstka, K. Błażewska
    Academic press:
    Journal of Medicinal Chemistry (rok: 2021, tom: 64, strony: brak), Wydawca: American Chemical Society
    Status:
    Published
    DOI:
    10.1021/acs.jmedchem.1c00410 - link to the publication
  4. Aza-Michael addition of imidazole analogs
    Authors:
    J. Gmach, Ł. Joachimiak, K. M. Błażewska
    Academic press:
    Synthesis (rok: 2016, tom: 48, strony: 2681-2704), Wydawca: Georg Thieme Verlag Stuttgart - New York
    Status:
    Published
    DOI:
    10.1055/s-0035-1560451 - link to the publication
  5. Functionalization of the imidazo[1,2-a]pyridine ring in α-phosphonoacrylates and α-phosphonopropionates via microwave-assisted Mizoroki–Heck reaction
    Authors:
    D. Kusy, A. Wojciechowska, J. Małolepsza, K. M. Błażewska
    Academic press:
    Beilstein Journal of Organic Chemistry (rok: 2020, tom: 16, strony: 15), Wydawca: Beilstein-Institut
    Status:
    Published
    DOI:
    10.3762/bjoc.16.3 - link to the publication
  6. Phosphorus-based probes as molecular tools for proteme studies: recent advances in probe development and applications
    Authors:
    Ł. Joachimiak, K. M. Błażewska
    Academic press:
    J. Med. Chem. (rok: 2018, tom: 61, strony: 8536-8562), Wydawca: American Chemical Society
    Status:
    Published
    DOI:
    10.1021/acs.jmedchem.8b00249 - link to the publication
  7. Identification of the Privileged Position in the Imidazo[1,2‐a]pyridine Ring of Phosphonocarboxylates for Development of Rab Geranylgeranyl Transferase (RGGT) Inhibitors
    Authors:
    A. Kaźmierczak, D. Kusy, S. P. Niinivehmas, J. Gmach, Ł. Joachimiak, O. T. Pentikaïnen, E. Gendaszewska-Darmach, Katarzyna M.Błazėwska
    Academic press:
    J. Med. Chem. (rok: 2017, tom: 60, strony: 8781-8800), Wydawca: American Chemical society
    Status:
    Published
    DOI:
    10.1021/acs.jmedchem.7b00811 - link to the publication
  8. Microwave-assisted synthesis of 3-formyl substituted imidazo[1,2-a] pyridines
    Authors:
    D. Kusy, W. Maniukiewicz, K. M. Błażewska
    Academic press:
    Tetrahedron Letters (rok: 2019, tom: 60, strony: 151244), Wydawca: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.tetlet.2019.151244 - link to the publication
  9. Synthesis and Biological Evaluation of Imidazole-Bearing a-Phosphonocarboxylates as Inhibitors of Rab Geranylgeranyl Transferase (RGGT)
    Authors:
    Ł. Joachimiak, A. Marchwicka, E. Gendaszewska-Darmach, K. M. Błażewska
    Academic press:
    ChemMedChem (rok: 2018, tom: 13, strony: 842-851), Wydawca: Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim
    Status:
    Published
    DOI:
    10.1002/cmdc.201700791 - link to the publication
  10. The McKenna reaction – avoiding side reactions in phosphonate deprotection
    Authors:
    K. Justyna, J. Małolepsza, D. Kusy, W. Maniukiewicz, K. M. Błażewska
    Academic press:
    Beilstein Journal of Organic Chemistry (rok: 2020, tom: 16, strony: 1436–1446), Wydawca: Beilstein-Institut
    Status:
    Published
    DOI:
    10.3762/bjoc.16.119 - link to the publication

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