title: AS1387392, a novel immunosuppressive cyclic tetrapeptide compound with inhibitory activity against mammalian histone deacetylase.
abstract: The novel immunosuppressant AS1387392 has been isolated from Acremonium sp. No. 27082. This compound showed a strong inhibitory effect against mammalian histone deacetylase and T-cell proliferation. Further, AS1387392 showed a good oral absorption, and its plasma concentration was higher than that of FR235222, an analog of AS1387392 that inhibited histone deacetylase previously reported. Given these findings, AS1387392 may represent an important new lead in developing immunosuppressant.
authors.affiliation: Pharmacology Research Laboratories, Astellas Pharma Inc., Tsukuba-shi, Ibaraki, Japan. satoshi.sasamura@jp.astellas.com
authors.forename: Satoshi
authors.initials: S
authors.lastname: Sasamura
authors.forename: Kazutoshi
authors.initials: K
authors.lastname: Sakamoto
authors.forename: Shoji
authors.initials: S
authors.lastname: Takagaki
authors.forename: Toshiko
authors.initials: T
authors.lastname: Yamada
authors.forename: Shigehiro
authors.initials: S
authors.lastname: Takase
authors.forename: Hiroaki
authors.initials: H
authors.lastname: Mori
authors.forename: Takashi
authors.initials: T
authors.lastname: Fujii
authors.forename: Motohiro
authors.initials: M
authors.lastname: Hino
authors.forename: Michizane
authors.initials: M
authors.lastname: Hashimoto
mesh_terms: D000164:Acremonium / Q000737:chemistry*; D000818:Animals; D049109:Cell Proliferation / Q000187:drug effects; D005260:Female; D005285:Fermentation; D056572:Histone Deacetylase Inhibitors / Q000302:isolation & purification / Q000493:pharmacokinetics / Q000494:pharmacology*; D006655:Histone Deacetylases / Q000187:drug effects* / Q000378:metabolism; D006801:Humans; D007166:Immunosuppressive Agents / Q000302:isolation & purification / Q000494:pharmacology*; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D010456:Peptides, Cyclic / Q000302:isolation & purification / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats; D011917:Rats, Inbred Lew; D013601:T-Lymphocytes / Q000187:drug effects / Q000378:metabolism
chemical_list: C554554:AS 1387392; C474179:FR 235222; D056572:Histone Deacetylase Inhibitors; D007166:Immunosuppressive Agents; D010456:Peptides, Cyclic; D006655:Histone Deacetylases