Abstract
Photoreactive compounds are important tools in life sciences that allow precisely timed covalent crosslinking of ligands and targets. Using a novel large-scale technique we have synthesized azidoblebbistatin, which is a new derivative of blebbistatin, the most widely used myosin inhibitor. Without UV irradiation azidoblebbistatin exhibits identical inhibitory properties to those of blebbistatin. Using UV irradiation azidoblebbistatin can be covalently crosslinked to myosin, which greatly enhances its in vitro and in vivo effectiveness. Photocrosslinking also eliminates limitations associated with the relatively low myosin affinity and water solubility of blebbistatin. Irradiating light used for photocrosslinking is not toxic for cells and tissues, which confers a great advantage in in vivo tests. As the crosslink results in an irreversible association of the inhibitor to myosin and the irradiation eliminates the residual activity of unbound inhibitor molecules, azidoblebbistatin has a great potential to become a highly effective tool in both structural studies of actomyosin contractility and the investigation of cellular and physiological functions of myosin II.
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