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

Research output: Contribution to journalArticlepeer-review

28 Citations (Scopus)


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.

Original languageEnglish
Pages (from-to)115-122
Number of pages8
Issue number1
Publication statusPublished - 2013 Jan
Externally publishedYes


  • Acyl protein thioesterases
  • Boronic acids
  • Inhibitors
  • Microarrays
  • Oncogenic Ras proteins

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Organic Chemistry


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