0

Targeting Myosin by Blebbistatin Derivatives: Optimization and Pharmacological Potential

Anna Á Rauscher, Máté Gyimesi, Mihály Kovács, András Málnási-Csizmadia

Trends Biochem Sci. 2018 Sep;43(9):700-713.

PMID: 30057142

Abstract:

Blebbistatin is a widely used inhibitor of myosin 2 that enables the study of a broad range of cytoskeleton-related processes. However, blebbistatin has several limitations hindering its applicability: it is fluorescent, poorly water soluble, cytotoxic, and prone to (photo)degradation. Despite these adverse effects, being the only available myosin 2-specific inhibitor, blebbistatin is rather a choice of necessity. Blebbistatin has been modified to improve its properties and some of the new compounds have proven to be useful replacements of the original molecule. This review summarizes recent results on blebbistatin development. We also discuss the pharmacological perspectives of these efforts, as myosins are becoming promising drug target candidates for a variety of conditions ranging from neurodegeneration to muscle disease, wound healing, and cancer metastasis.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP856925718 (−)-Blebbistatin (−)-Blebbistatin 856925-71-8 Price
qrcode