User:MySmarterSelf/MPH-220

MPH-220 new article content ...

MPH-220 is a first-in-class anti-spastic drug candidate.

Mechanism of action
MPH-220 relaxes skeletal muscle by inhibiting directly myosin ATPase activity and this way acto-myosin based motility. It binds halfway between the nucleotide binding pocket and the actin binding cleft of myosin (blebbistatin binding site), predominantly in an actin detached conformation. This type of inhibition relaxes the acto-myosin myofilaments.

Specificity
A single amino acid difference between cardiac and skeletal muscle myosin-2 isoforms is responsible for the high selectivity of MPH-220.

Drug development status
MPH-220 is in preclinical phase of drug-development. Planned to enter clinical phase 1 soon sponsored by Motorpharma Ltd.