KS-501 and KS-502, new inhibitors of Ca2+ and calmodulin-dependent cyclic-nucleotide phosphodiesterase from Sporothrix sp

J Antibiot (Tokyo). 1989 Jul;42(7):1049-55. doi: 10.7164/antibiotics.42.1049.

Abstract

New inhibitors of Ca2+ and calmodulin-dependent cyclic-nucleotide phosphodiesterase, KS-501 and KS-502 were isolated from a fungus, Sporothrix sp. KAC-1985. Inhibitory concentration causing 50% inhibition (IC50) values of KS-501 and KS-502 for bovine brain enzyme were 1.8 and 4.3 microM, respectively. The compounds exhibited no or weak inhibition for calmodulin-independent cyclic-nucleotide phosphodiesterases and protein kinase C.

MeSH terms

  • 2',3'-Cyclic-Nucleotide Phosphodiesterases / antagonists & inhibitors*
  • Calcium / metabolism*
  • Calmodulin / metabolism
  • Chromatography, Gel
  • Chromatography, Thin Layer
  • Fermentation
  • Hydroxybenzoates / biosynthesis*
  • Hydroxybenzoates / isolation & purification
  • Hydroxybenzoates / pharmacology
  • Molecular Structure
  • Sporothrix / metabolism*

Substances

  • Calmodulin
  • Hydroxybenzoates
  • KS 502
  • KS 501
  • 2',3'-Cyclic-Nucleotide Phosphodiesterases
  • Calcium