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OtherDrug Discovery and Translational Medicine

Improved inhibitory and ADMET properties of blebbistatin derivatives indicate that blebbistatin scaffold is ideal for drug development targeting myosin-2

Máté Gyimesi, Anna Á. Rauscher, Sharad Kumar Suthar, Kamirán Á. Hamow, Kinga Oravecz, István Lőrincz, Zsolt Borhegyi, Máté T. Déri, Ádám F. Kiss, Katalin Monostory, Pál Tamás Szabó, Suman Nag, Ivan Tomasic, Jacob Krans, Patrick J. Tierney, Mihály Kovács, László Kornya and András Málnási-Csizmadia
Journal of Pharmacology and Experimental Therapeutics January 19, 2021, JPET-AR-2020-000167; DOI: https://doi.org/10.1124/jpet.120.000167
Máté Gyimesi
1Department of Biochemistry, ELTE Eötvös Loránd University, Hungary
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  • ORCID record for Máté Gyimesi
Anna Á. Rauscher
2Biochemistry, Eötvös Loránd University, Hungary
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Sharad Kumar Suthar
3Printnet Ltd, Hungary
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Kamirán Á. Hamow
4Plant Protection Institute, Centre for Agricultural Research, Hungary
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Kinga Oravecz
5ELTE Eötvös Loránd University, Hungary
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István Lőrincz
3Printnet Ltd, Hungary
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Zsolt Borhegyi
5ELTE Eötvös Loránd University, Hungary
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Máté T. Déri
6Hungarian Academy of Sciences Research Centre for Natural Sciences, Hungary
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Ádám F. Kiss
6Hungarian Academy of Sciences Research Centre for Natural Sciences, Hungary
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Katalin Monostory
6Hungarian Academy of Sciences Research Centre for Natural Sciences, Hungary
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Pál Tamás Szabó
6Hungarian Academy of Sciences Research Centre for Natural Sciences, Hungary
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Suman Nag
7MyoKardia Inc, United States
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Ivan Tomasic
7MyoKardia Inc, United States
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Jacob Krans
8Western New England University, United States
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Patrick J. Tierney
8Western New England University, United States
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Mihály Kovács
5ELTE Eötvös Loránd University, Hungary
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László Kornya
9Central Hospital of Southern Pest, National Institute of Hematology and Infectious Diseases, Hungary
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  • For correspondence: malna@elte.hu
András Málnási-Csizmadia
5ELTE Eötvös Loránd University, Hungary
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  • For correspondence: malna@elte.hu

Data Supplement

  • Supplemental Data -

    Supplemental methods and results

    Supplementary Figure S1 – Stability of blebbistatin, NBleb and AmBleb in rat blood.

    Supplementary Figure S2 – MS chromatograms of blebbistatin, NBleb and AmBleb, and the major metabolites.

    Supplementary Table S1. Solubility of blebbistatin, NBleb and AmBleb in different buffer conditions.

  View article

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