title: Novel propeptin analog, propeptin-2, missing two amino acid residues from the propeptin C-terminus loses antibiotic potency.
abstract: A novel inhibitor of prolyl endopeptidase, the propeptin analog propeptin-2 (C105H130N24O(24)), missing two amino acid residues from the propeptin C-terminus was isolated from the fermentation broth of propeptin-producing Microbispora sp. SNA-115 grown using a large inoculum. It shows the same enzyme inhibition activity as propeptin against prolyl endopeptidase (Ki=1.5 microM), but its antimicrobial activity against Mycobacterium phlei is more than 100-fold lower.
authors.affiliation: Faculty of Agriculture, Iwate University, Morioka 020-8550, Japan. kimurak@iwate-u.ac.jp
authors.forename: Ken-ichi
authors.initials: K
authors.lastname: Kimura
authors.forename: Mai
authors.initials: M
authors.lastname: Yamazaki
authors.forename: Noriko
authors.initials: N
authors.lastname: Sasaki
authors.forename: Tetsuro
authors.initials: T
authors.lastname: Yamashita
authors.forename: Shigenori
authors.initials: S
authors.lastname: Negishi
authors.forename: Takemichi
authors.initials: T
authors.lastname: Nakamura
authors.forename: Hiroyuki
authors.initials: H
authors.lastname: Koshino
mesh_terms: D000192:Actinomycetales / Q000254:growth & development / Q000378:metabolism*; D000596:Amino Acids / Q000378:metabolism; D003470:Culture Media / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000378:metabolism* / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D009168:Mycobacterium phlei / Q000187:drug effects; D010456:Peptides, Cyclic / Q000737:chemistry* / Q000378:metabolism* / Q000494:pharmacology; D000085822:Prolyl Oligopeptidases; D012697:Serine Endopeptidases / Q000378:metabolism; D013329:Structure-Activity Relationship