Dual structure-activity relationship of osteoclastogenesis inhibitor methyl gerfelin based on teg scanning

Naoki Kanoh, Takahiro Suzuki, Makoto Kawatani, Yasuhiro Katou, Hiroyuki Osada, Yoshiharu Iwabuchi

Research output: Contribution to journalArticle

8 Citations (Scopus)

Abstract

Methyl gerfelin derivatives, each having an amine-terminated tri(ethylene glycol) linker at the peripheral position, were designed and systematically synthesized. These "TEGylated" derivatives were then subjected to a structure-activity relationship (SAR) study to examine their glyoxalase 1-inhibition activity and binding affinity toward the three binding proteins identified. Among the derivatives synthesized, that with a NH2-TEG linker at the C6-methyl group showed the most potent glyoxalase 1-inhibiting activity and glyoxalase 1 selectivity. These results indicated that derivatization at the C6-methyl group would be suitable for the further development of selective glyoxalase 1 inhibitors.

Original languageEnglish
Pages (from-to)44-52
Number of pages9
JournalBioconjugate Chemistry
Volume24
Issue number1
DOIs
Publication statusPublished - 2013 Jan 16

ASJC Scopus subject areas

  • Biotechnology
  • Bioengineering
  • Biomedical Engineering
  • Pharmacology
  • Pharmaceutical Science
  • Organic Chemistry

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