Zimmermann_2013_Chembiochem_14_115

Reference

Title : Boron-based inhibitors of acyl protein thioesterases 1 and 2 - Zimmermann_2013_Chembiochem_14_115
Author(s) : Zimmermann TJ , Burger M , Tashiro E , Kondoh Y , Martinez NE , Gormer K , Rosin-Steiner S , Shimizu T , Ozaki S , Mikoshiba K , Watanabe N , Hall D , Vetter IR , Osada H , Hedberg C , Waldmann H
Ref : Chembiochem , 14 :115 , 2013
Abstract : 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.
ESTHER : Zimmermann_2013_Chembiochem_14_115
PubMedSearch : Zimmermann_2013_Chembiochem_14_115
PubMedID: 23239555

Related information

Citations formats

Zimmermann TJ, Burger M, Tashiro E, Kondoh Y, Martinez NE, Gormer K, Rosin-Steiner S, Shimizu T, Ozaki S, Mikoshiba K, Watanabe N, Hall D, Vetter IR, Osada H, Hedberg C, Waldmann H (2013)
Boron-based inhibitors of acyl protein thioesterases 1 and 2
Chembiochem 14 :115

Zimmermann TJ, Burger M, Tashiro E, Kondoh Y, Martinez NE, Gormer K, Rosin-Steiner S, Shimizu T, Ozaki S, Mikoshiba K, Watanabe N, Hall D, Vetter IR, Osada H, Hedberg C, Waldmann H (2013)
Chembiochem 14 :115