title: Synthesis of tripeptide chloromethyl ketones and examination of their inhibitory effects on plasmin and plasma kallikrein.
abstract: With the aim of obtaining selective synthetic inhibitors of plasmin and plasma kallikrein, D-Ile-Phe-Lys-CH2Cl, Ile-Phe-Lys-CH2Cl, D-Ile-Phe-Arg-CH2Cl and Ile-Phe-Arg-CH2Cl were synthesized and their inhibitory activity against plasmin, plasma kallikrein and other trypsin-like serine proteinases was examined. Among them, D-Ile-Phe-Arg-CH2Cl exhibited a highly selective inhibitory activity against plasma kallikrein, yet D-Ile-Phe-Lys-CH2Cl exhibited nearly the same order of inhibitory activity against plasmin as well as plasma kallikrein.
authors.forename: Y
authors.initials: Y
authors.lastname: Tsuda
authors.forename: N
authors.initials: N
authors.lastname: Teno
authors.forename: Y
authors.initials: Y
authors.lastname: Okada
authors.forename: K
authors.initials: K
authors.lastname: Wanaka
authors.forename: M
authors.initials: M
authors.lastname: Bohgaki
authors.forename: A
authors.initials: A
authors.lastname: Hijikata-Okunomiya
authors.forename: U
authors.initials: U
authors.lastname: Okamoto
authors.forename: T
authors.initials: T
authors.lastname: Naito
authors.forename: S
authors.initials: S
authors.lastname: Okamoto
mesh_terms: D000590:Amino Acid Chloromethyl Ketones / Q000138:chemical synthesis*; D000595:Amino Acid Sequence; D055598:Chemical Phenomena; D002621:Chemistry; D003864:Depression, Chemical; D005341:Fibrinolysin / Q000037:antagonists & inhibitors / Q000378:metabolism*; D007610:Kallikreins / Q000037:antagonists & inhibitors / Q000097:blood*; D008969:Molecular Sequence Data
chemical_list: D000590:Amino Acid Chloromethyl Ketones; C063352:isoleucyl-phenylalanyl-arginine chloromethyl ketone; C063351:isoleucyl-phenylalanyl-lysine chloromethyl ketone; D007610:Kallikreins; D005341:Fibrinolysin