Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: UMLS:C0018799 (
heart disease
)
34,133
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
Posttranslational arginylation mediated by arginyltransferase (
ATE1
) is an emerging major regulator of embryogenesis and cell physiology. Impairments of
ATE1
are implicated in congenital heart defects, obesity, cancer, and neurodegeneration making this enzyme an important therapeutic target, whose potential has been virtually unexplored. Here we report the development of a biochemical assay for identification of small molecule inhibitors of
ATE1
and application of this assay to screen a library of 3280 compounds. Our screen identified two compounds which specifically affect
ATE1
-regulated processes in vivo, including tannic acid, which has been previously shown to inhibit protein degradation and angiogenesis and to act as a therapeutic agent in
heart disease
and cancer. Our data suggest that these actions of tannic acid are mediated by its direct effect on
ATE1
, which regulates protein degradation and angiogenesis in vivo.
...
PMID:Small molecule inhibitors of arginyltransferase regulate arginylation-dependent protein degradation, cell motility, and angiogenesis. 2228 Aug 15
