Three-dimensional solution structure of EM703 with potent promoting activity of monocyte-to-macrophage differentiation

Hiroaki Gouda, Toshiaki Sunazuka, Kiminari Yoshida, Akihiro Sugawara, Yusuke Sakoh, Satoshi Omura, Shuichi Hirono

Research output: Contribution to journalArticlepeer-review

7 Citations (Scopus)

Abstract

EM703, which is an erythromycin derivative synthesized by our group, has a potent promoting activity of monocyte-to-macrophage differentiation in vitro. Its activity is approximately 300 times higher than that of erythromycin A (EM-A). In this study, we determined three-dimensional (3D) solution structures of EM703 and EM-A, and compared them using a superposition method, in order to investigate the 3D structure-activity relationship. We found a distinct difference between the 3D structures of these molecules, which might be an important factor in their divergent activities.

Original languageEnglish
Pages (from-to)2496-2499
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume16
Issue number9
DOIs
Publication statusPublished - 2006 May 1
Externally publishedYes

Keywords

  • Alignment
  • Erythromycin A
  • Erythromycin derivative
  • Immunomodulatory activity
  • Molecular dynamics
  • NMR
  • QSAR
  • Three-dimensional solution structure

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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