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3D structure-based search for selective inhibitor of thymidylate synthase of nematodes, a potential drug in chemotherapy of diseases caused by parasitic nematodes

2011/01/B/NZ6/01781

Keywords

Descriptors

  • NZ6_6: Parazytologia
  • NZ1_9: Biotechnologia

Panel

NZ6 – Human and animal immunology and infection: immunity, immune disorders, immunotherapy, infectious and invasive diseases, microbiology, transplantology, allergology

Host institution

Instytut Biologii Doświadczalnej im. M. Nenckiego PAN

Voivodeship: mazowieckie

Other projects carried out by the institution »

Principal investigator (from the host institution)

prof. Wojciech Krzysztof Rode

Number of co-investigators in the project: 8

Call

OPUS 1 – announced on 2011-03-15

Amount awarded
396 000 PLN
Project start date
2011-12-12
Project end date
2015-12-11
Project duration
48 months (the same as in the proposal)
Project status
Project settled

Equipment purchased [PL]

  1. Mikroskop stereoskopowy. Cost: 50 000 PLN

Information in the final report

Publication in academic press/journals (7)

  1. Properties of phosphorylated thymidylate synthase

    Authors:
    Frączyk T, Ruman T, Wilk P, Palmowski P, Rogowska-Wrzesinska A, Cieśla J, Zieliński Z, Nizioł J, Jarmuła A, Maj P, Gołos B, Wińska P, Ostafil S, Wałajtys-Rode E, Shugar D, Rode W
    Academic press:
    Biochim Biophys Acta - Proteins Proteom (year: 2015, volume: 1854, pages: 1922-1934), Publisher: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.bbapap.2015.08.007 – link to the publication

  2. Crystal structure of phosphoramide-phosphorylated thymidylate synthase reveals pSer127, reflecting probably pHis to pSer phosphotransfer.

    Authors:
    Wilk P, Jarmuła A, Ruman T, Banaszak K, Rypniewski W, Cieśla J, Dowierciał A, Rode W
    Academic press:
    Bioorg Chem (year: 2014, volume: 52, pages: 44-49), Publisher: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.bioorg.2013.11.003 – link to the publication

  3. Crystal structures of thymidylate synthase from nematodes, Trichinella spiralis and Caenorhabditis elegans, as a potential template for species-specific drug design.

    Authors:
    Dowierciał A, Wilk P, Rypniewski W, Frączyk T, Jarmuła A, Banaszak K, Dąbrowska M, Cieśla J, Rode W
    Academic press:
    Pteridines (year: 2013, volume: 24, pages: 87-91), Publisher: DeGruyter
    Status:
    Published
    DOI:
    10.1515/pterid-2013-0011 – link to the publication

  4. Crystal structures of complexes of mouse thymidylate synthase crystallized with N4-OH-dCMP alone or in the presence of N5,10-methylenetetrahydrofolate.

    Authors:
    Dowierciał A, Jarmuła A, Wilk P, Rypniewski W, Kierdaszuk B, Rode W
    Academic press:
    Pteridines (year: 2013, volume: 24, pages: 93-98), Publisher: DeGruyter
    Status:
    Published
    DOI:
    10.1515/pterid-2013-0010 – link to the publication

  5. Uncommon and parallel developmental patterns of thymidylate synthase expression and localization in Trichinella spiralis and Caenorhabditis elegans.

    Authors:
    Dąbrowska M, Gołos B, Wałajtys-Rode E, Zieliński Z, Wińska P, Cieśla J, Moczoń T, Rode W
    Academic press:
    Pteridines (year: 2013, volume: 24, pages: 121-125), Publisher: DeGruyter
    Status:
    Published
    DOI:
    10.1515/pterid-2013-0009 – link to the publication

  6. Immunofluorescent localization of thymidylate synthase in the development of Trichinella spiralis and Caenorhabditis elegans.

    Authors:
    Gołos B, Dąbrowska M, Wałajtys-Rode E, Zieliński Z, Wińska P, Cieśla J, Jagielska E, Moczoń T, Rode W
    Academic press:
    Mol. Biochem. Parasitol. (year: 2012, volume: 183, pages: 63-69), Publisher: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.molbiopara.2012.02.002 – link to the publication

  7. Phosphorylation of thymidylate synthase affects slow-binding inhibition by 5-fluoro-dUMP and N4-hydroxy-dCMP

    Authors:
    Ludwiczak J, Maj P, Wilk P, Frączyk T, Ruman T, Kierdaszuk B, Jarmułaa A, Rode W
    Academic press:
    Mol. BioSyst. (year: 2016, volume: 12, pages: 1333-1341), Publisher: Royal Society of Chemistry
    Status:
    Published
    DOI:
    10.1039/C6MB00026F – link to the publication

Articles in post-conference publications (6)

  1. Mechanism of thymidylate synthase-catalyzed reaction inhibition by N4-OH-dCMP in view of crystallographic studies

    Authors:
    Dowierciał A, Wilk P, Jarmuła A, Krawiec K, Rypniewski W, Kierdaszuk B, Rode W/Rode W
    Conference:
    9th International Conference of Anticancer Research (year: 2014, pages: 60136-6139), Publisher: International Institute of Anticancer Research
    Date:
    conference 6-10.10. 2014
    Status:
    Published
    DOI:
    link to the publication

  2. Crystal structure of complexes of mouse thymidylate synthase crystallized with N4-OH-dCMP alone or in the presence of N10-methylenetetrahydrofolate()

    Authors:
    Dowierciał A, Wilk P, Jarmuła A, Rypniewski W, Kierdaszuk B, Rode W
    Conference:
    15th International Symposium on Pteridines and Folates, 2012, Antalya (year: 2012, pages: S41), Publisher: INT SOC PTERIDINOLOGY
    Date:
    conference 9-13 maja
    Status:
    Published

  3. Crystal structures of thymidylate synthase from nematodes, Trichinella spiralis and Caenorhabditis elegans, as a potential template for species-specific drug design.

    Authors:
    Wilk P, Dowierciał A, Rypniewski W, Frączyk T, Jarmuła A, Rode W
    Conference:
    15th International Symposium on Pteridines and Folates (year: 2012, pages: S41-42), Publisher: INT SOC PTERIDINOLOGY
    Date:
    conference 9-13 maja 2012
    Status:
    Published

  4. Mechanism of slow-binding inhibition of thymidylate synthase-catalyzed reaction by N4-OH-dCMP in view of crystallographic studies.

    Authors:
    Anna Dowierciał, Piotr Wilk, Adam Jarmuła, Krzysztof Krawiec, Wojciech Rypniewski, Borys Kierdaszuk, Wojciech Rode
    Conference:
    Prof. David Shugar 100th Anniversary Conference: Challenges in molecular biology, biophysics, and biomedicine (year: 2015, pages: Program, str 2), Publisher: Instytut Biochemii i Biofizyki PAN
    Date:
    conference 17-19 września
    Status:
    Published

  5. Unusual and parallel developmental patterns of thymidylate synthase expression and localization in Trichinella spiralis and Caenorhabditis elegans.

    Authors:
    Dąbrowska M, Gołos B, Wałajtys-Rode E, Zieliński Z, Wińska P, Cieśla J, Jagielska E, Moczoń T, Rode W
    Conference:
    15th International Symposium on Pteridines and Folates, Antalya (year: 2012, pages: S40), Publisher: INT SOC PTERIDINOLOGY
    Date:
    conference 9-13 maja 2012
    Status:
    Published

  6. SEARCHING FOR THE DIFFERENCES BETWEEN TRICHINELLA SPIRALIS AND MOUSE THYMIDYLATE SYNTHASES: A QUEST FOR SPECIES − SPECIFIC DRUGS

    Authors:
    A. Dowierciał, A. Jarmuła, W.R. Rypniewski, T. Frączyk1, P. Wilk and W. Rode
    Conference:
    ISSRNS 2012 (year: 2012, pages: 91), Publisher: Instytut Fizyki PAN
    Date:
    conference maj 2012
    Status:
    Published

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