Journal
CHEMBIOCHEM
Volume 14, Issue 1, Pages 115-122Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cbic.201200571
Keywords
acyl protein thioesterases; boronic acids; inhibitors; microarrays; oncogenic Ras proteins
Funding
- International Max Planck Research School (IMPRS)
- Fonds der Chemischen Industrie
- Deutsche Forschungsgemeinschaft [SFB 642]
- RIKEN-Max Planck Joint Research Center
- Grants-in-Aid for Scientific Research [20113008, 23510287, 24510320] Funding Source: KAKEN
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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 non-toxic 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.
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