Insights into the myosin II inhibitory potency of A-ring-modified (S)-blebbistatin analogs |
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| Authors: | Sigrid Verhasselt Christian V Stevens Tom Van den broecke Marc E Bracke Bart I Roman |
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| Institution: | 1. SynBioC Research Group, Department of Sustainable Organic Chemistry and Technology, Campus Coupure, Ghent University, Coupure Links 653, 9000 Ghent, Belgium;2. Laboratory of Experimental Cancer Research, Department of Radiation Oncology and Experimental Cancer Research, Ghent University, De Pintelaan 185, 9000 Ghent, Belgium |
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| Abstract: | Myosin II is an interesting target for therapeutic intervention, as it is involved in a large number of motility-based diseases. (S)-Blebbistatin is a known micromolar inhibitor of this protein. A new series of (S)-blebbistatin derivatives with a modified A-ring was synthesized and the myosin II inhibitory properties were evaluated in vitro. In this way, we gained insight into the influence of structural modifications in this part of the scaffold on myosin II inhibitory potency. Our results indicate there are few possibilities for potency enhancement via ring A modification of the blebbistatin scaffold. |
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| Keywords: | Blebbistatin A-ring modification Myosin II |
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