title: Identification of the minimum peptide from mouse myostatin prodomain for human myostatin inhibition.
abstract: Myostatin, an endogenous negative regulator of skeletal muscle mass, is a therapeutic target for muscle atrophic disorders. Here, we identified minimum peptides 2 and 7 to effectively inhibit myostatin activity, which consist of 24 and 23 amino acids, respectively, derived from mouse myostatin prodomain. These peptides, which had the propensity to form α-helix structure, interacted to myostatin with KD values of 30-36 nM. Moreover, peptide 2 significantly increased muscle mass in Duchenne muscular dystrophy model mice.
authors.affiliation: Department of Medicinal Chemistry, ‡Laboratory of Cardiovascular Medicine, and §Department of Drug Delivery and Molecular Biopharmaceutics, Tokyo University of Pharmacy and Life Sciences , Hachioji, Tokyo192-0392, Japan.
authors.forename: Kentaro
authors.initials: K
authors.lastname: Takayama
authors.forename: Yuri
authors.initials: Y
authors.lastname: Noguchi
authors.forename: Shin
authors.initials: S
authors.lastname: Aoki
authors.forename: Shota
authors.initials: S
authors.lastname: Takayama
authors.forename: Momoko
authors.initials: M
authors.lastname: Yoshida
authors.forename: Tomo
authors.initials: T
authors.lastname: Asari
authors.forename: Fumika
authors.initials: F
authors.lastname: Yakushiji
authors.forename: Shin-ichiro
authors.initials: S
authors.lastname: Nishimatsu
authors.forename: Yutaka
authors.initials: Y
authors.lastname: Ohsawa
authors.forename: Fumiko
authors.initials: F
authors.lastname: Itoh
authors.forename: Yoichi
authors.initials: Y
authors.lastname: Negishi
authors.forename: Yoshihide
authors.initials: Y
authors.lastname: Sunada
authors.forename: Yoshio
authors.initials: Y
authors.lastname: Hayashi
mesh_terms: D000818:Animals; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D056945:Hep G2 Cells; D006801:Humans; D051379:Mice; D018101:Mice, Inbred mdx; D015394:Molecular Structure; D018482:Muscle, Skeletal / Q000737:chemistry* / Q000378:metabolism; D055435:Myostatin / Q000037:antagonists & inhibitors* / Q000378:metabolism; D010455:Peptides / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D055435:Myostatin; D010455:Peptides