title: Isolation and characterisation of an antifungal antibiotic (GR135402) with protein synthesis inhibition.
abstract: A novel antifungal antibiotic GR135402 has been isolated from a fermentation broth of Graphium putredinis which inhibited protein synthesis in Candida albicans but not rabbit reticulocytes. The spectrum of activity included C. albicans and Cryptococcus neoformans but not some other Candida species or Aspergillus species. Therapeutic efficacy in a mouse model of systemic candidosis was attained following parenteral dosing.
authors.affiliation: Glaxo Wellcome Research and Development, Hertfordshire, UK.
authors.forename: O S
authors.initials: OS
authors.lastname: Kinsman
authors.forename: P A
authors.initials: PA
authors.lastname: Chalk
authors.forename: H C
authors.initials: HC
authors.lastname: Jackson
authors.forename: R F
authors.initials: RF
authors.lastname: Middleton
authors.forename: A
authors.initials: A
authors.lastname: Shuttleworth
authors.forename: B A
authors.initials: BA
authors.lastname: Rudd
authors.forename: C A
authors.initials: CA
authors.lastname: Jones
authors.forename: H M
authors.initials: HM
authors.lastname: Noble
authors.forename: H G
authors.initials: HG
authors.lastname: Wildman
authors.forename: M J
authors.initials: MJ
authors.lastname: Dawson
authors.forename: C
authors.initials: C
authors.lastname: Stylli
authors.forename: P J
authors.initials: PJ
authors.lastname: Sidebottom
authors.forename: B
authors.initials: B
authors.lastname: Lamont
authors.forename: S
authors.initials: S
authors.lastname: Lynn
authors.forename: M V
authors.initials: MV
authors.lastname: Hayes
mesh_terms: D000818:Animals; D000935:Antifungal Agents / Q000737:chemistry* / Q000302:isolation & purification* / Q000494:pharmacology; D001230:Aspergillus / Q000187:drug effects; D002176:Candida albicans / Q000187:drug effects; D005285:Fermentation; D051379:Mice; D008826:Microbial Sensitivity Tests; D003904:Mitosporic Fungi / Q000737:chemistry* / Q000145:classification; D011083:Polycyclic Compounds / Q000737:chemistry* / Q000302:isolation & purification* / Q000494:pharmacology; D011500:Protein Synthesis Inhibitors / Q000737:chemistry* / Q000302:isolation & purification* / Q000494:pharmacology
chemical_list: D000935:Antifungal Agents; C111326:GR135402; D011083:Polycyclic Compounds; D011500:Protein Synthesis Inhibitors