Boron-Based Inhibitors of Acyl Protein Thioesterases 1 and 2

Tobias J. Zimmermann, Marco Bürger, Etsu Tashiro, Yasumitsu Kondoh, Nancy E. Martinez, Kristina Görmer, Sigrid Rosin-Steiner, Takeshi Shimizu, Shoichiro Ozaki, Katsuhiko Mikoshiba, Nobumoto Watanabe, Dennis Hall, Ingrid R. Vetter, Hiroyuki Osada, Christian Hedberg, Herbert Waldmann

研究成果: Article査読

26 被引用数 (Scopus)

抄録

Ras proteins are of importance in cell proliferation, and hence their mutated forms play causative roles in many kinds of cancer in different tissues. Inhibition of the Ras-depalmitoylating enzyme acyl protein thioesterases APT1 and -2 is a new approach to modulating the Ras cycle. Here we present boronic and borinic acid derivatives as a new class of potent and nontoxic APT inhibitors. These compounds were detected by extensive library screening using chemical arrays and turned out to inhibit human APT1 and -2 in a competitive mode. Furthermore, one of the molecules was demonstrated to inhibit Erk1/2 phosphorylation significantly.

本文言語English
ページ(範囲)115-122
ページ数8
ジャーナルChemBioChem
14
1
DOI
出版ステータスPublished - 2013 1

ASJC Scopus subject areas

  • 生化学
  • 分子医療
  • 分子生物学
  • 有機化学

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