Unknown

Dataset Information

0

Design and synthesis of small molecule glycerol 3-phosphate acyltransferase inhibitors.


ABSTRACT: The incidence of obesity and other diseases associated with an increased triacylglycerol mass is growing rapidly, particularly in the United States. Glycerol 3-phosphate acyltransferase (GPAT) catalyzes the rate-limiting step of glycerolipid biosynthesis, the acylation of glycerol 3-phosphate with saturated long-chain acyl-CoAs. In an effort to produce small molecule inhibitors of this enzyme, a series of benzoic and phosphonic acids was designed and synthesized. In vitro testing of this series has led to the identification of several compounds, in particular 2-(nonylsulfonamido)benzoic acid (15g), possessing moderate GPAT inhibitory activity in an intact mitochondrial assay.

SUBMITTER: Wydysh EA 

PROVIDER: S-EPMC3184552 | biostudies-literature | 2009 May

REPOSITORIES: biostudies-literature

altmetric image

Publications

Design and synthesis of small molecule glycerol 3-phosphate acyltransferase inhibitors.

Wydysh Edward A EA   Medghalchi Susan M SM   Vadlamudi Aravinda A   Townsend Craig A CA  

Journal of medicinal chemistry 20090501 10


The incidence of obesity and other diseases associated with an increased triacylglycerol mass is growing rapidly, particularly in the United States. Glycerol 3-phosphate acyltransferase (GPAT) catalyzes the rate-limiting step of glycerolipid biosynthesis, the acylation of glycerol 3-phosphate with saturated long-chain acyl-CoAs. In an effort to produce small molecule inhibitors of this enzyme, a series of benzoic and phosphonic acids was designed and synthesized. In vitro testing of this series  ...[more]

Similar Datasets

| S-EPMC3184547 | biostudies-literature
| S-EPMC4109893 | biostudies-literature
| S-EPMC7432870 | biostudies-literature
| S-EPMC2442282 | biostudies-literature
| S-EPMC10823475 | biostudies-literature
| S-EPMC5070603 | biostudies-literature
| S-EPMC9463491 | biostudies-literature
| S-EPMC4993694 | biostudies-literature
| S-EPMC1702318 | biostudies-literature
| S-EPMC4373408 | biostudies-literature