Isolation and structural elucidation of glucoside congeners of platencin from Streptomyces platensis sb12600

Zhiguo Yu, Mostafa E. Rateb, Michael J. Smanksi, Ryan M. Peterson, Ben Shen

Research output: Contribution to journalArticle

11 Citations (Scopus)

Abstract

Platensimycin (PTM, 1)1, 2 and platencin (PTN, 2)3, 4 are recently discovered natural products, which are potent and selective inhibitors of bacterial and mammalian fatty acid synthases (Figure 1a). They have emerged as promising drug leads for both antibacterial and antidiabetic therapies. Although the efficacy of PTM and PTN has been demonstrated in mouse models, they suffer from poor pharmacokinetic properties, mainly a high rate of clearance, thereby requiring continuous infusion to ensure adequate exposure, a delivery method that is not desirable to most patients. Consequently, significant effort has been undertaken to prepare PTM and PTN analogues by organic synthesis,8, 9 and to isolate PTM and PTN congeners by fermentation optimization. Although these analogues have helped define the structure–activity relationship of PTM and PTN, none of them however can be argued to have significantly improved therapeutic properties.
Original languageEnglish
Pages (from-to)291-294
Number of pages4
JournalThe Journal of Antibiotics
Volume66
Issue number5
DOIs
Publication statusPublished - May 2013
Externally publishedYes

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Keywords

  • antibacterial
  • Antidiabetes
  • Fatty acid synthase inhibitor
  • Glucoside
  • Pathway regulation
  • Platencin
  • Platensimycin

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