Boron-based inhibitors of acyl protein thioesterases 1 and 2.
Chembiochem
; 14(1): 115-22, 2013 Jan 02.
Article
de En
| MEDLINE
| ID: mdl-23239555
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.
Texte intégral:
1
Collection:
01-internacional
Base de données:
MEDLINE
Sujet principal:
Thiolester hydrolases
/
Bore
/
Antienzymes
Limites:
Animals
/
Humans
Langue:
En
Journal:
Chembiochem
Sujet du journal:
BIOQUIMICA
Année:
2013
Type de document:
Article
Pays d'affiliation:
Allemagne