User:MySmarterSelf/MPH-220

MPH-220
Names
	IUPAC name S-4a-hydroxy-2-methyl-7-(4-morpholinophenyl)-4a,5,6,7-tetrahydro-4H-pyrrolo[2,3-b]thieno[3,2-e]pyridine-4-one
Identifiers
PubChem CID	440111967;
Properties
Chemical formula	C20H21N3O3S
Molar mass	383.47 g·mol−1
Appearance	orange solid
Solubility in water	50 μM
	Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). Infobox references

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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.^[1]

Specificity

MPH-220 co-crystallized with skeletal muscle myosin

A single amino acid difference between cardiac and skeletal muscle myosin-2 isoforms is responsible for the high selectivity of MPH-220.^[1]

Drug development status

MPH-220 is in preclinical phase of drug-development. Planned to enter clinical phase 1 soon sponsored by Motorpharma Ltd. ^[2]

References

^ ^a ^b Gyimesi, Máté; Horváth, Ádám I.; Túrós, Demeter; Suthar, Sharad Kumar; Pénzes, Máté; Kurdi, Csilla; Canon, Louise; Kikuti, Carlos; Ruppel, Kathleen M.; Trivedi, Darshan V.; Spudich, James A. (2020-10-15). "Single Residue Variation in Skeletal Muscle Myosin Enables Direct and Selective Drug Targeting for Spasticity and Muscle Stiffness". Cell. 183 (2): 335–346.e13. doi:10.1016/j.cell.2020.08.050. ISSN 1097-4172. PMC 7596007. PMID 33035452.
^ "Motorpharma website".{{cite web}}: CS1 maint: url-status (link)

External links

www.motorpharma.com

[:0-1] Gyimesi, Máté; Horváth, Ádám I.; Túrós, Demeter; Suthar, Sharad Kumar; Pénzes, Máté; Kurdi, Csilla; Canon, Louise; Kikuti, Carlos; Ruppel, Kathleen M.; Trivedi, Darshan V.; Spudich, James A. (2020-10-15). "Single Residue Variation in Skeletal Muscle Myosin Enables Direct and Selective Drug Targeting for Spasticity and Muscle Stiffness". Cell. 183 (2): 335–346.e13. doi:10.1016/j.cell.2020.08.050. ISSN 1097-4172. PMC 7596007. PMID 33035452.

[2] "Motorpharma website".{{cite web}}: CS1 maint: url-status (link)

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