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aP2 (adipocyte Protein 2) [5] is a carrier protein for fatty acids that is primarily expressed in adipocytes and macrophages. aP2 is also called fatty acid binding protein 4 (FABP4). Blocking this protein either through genetic engineering or drugs [6] has the possibility of treating heart disease and the metabolic syndrome. [7]
Unlike other HIV protease inhibitors on the market, tipranavir was developed from a nonpeptidic coumarin template and its antiprotease activity was discovered by high-throughput screening. [23] This sulfonamide containing 5,6-dihydro-4-hydroxy-2-pyrone had emerged from screenings of 3-substituted coumarins and dihydropyrones. [24]
The protein encoded by this gene is PPAR-gamma and is a regulator of adipocyte differentiation. Alternatively spliced transcript variants that encode different isoforms have been described. [10] The activity of PPARG can be regulated via phosphorylation through the MEK/ERK pathway.
The adipokines, or adipocytokines (Greek adipo-, fat; cytos-, cell; and -kinos, movement) are cytokines (cell signaling proteins) secreted by adipose tissue.Some contribute to an obesity-related low-grade state of inflammation or to the development of metabolic syndrome, a constellation of diseases including, but not limited to, type 2 diabetes, cardiovascular disease and atherosclerosis. [1]
Forkhead box protein O1 (FOXO1), also known as forkhead in rhabdomyosarcoma (FKHR), is a protein that in humans is encoded by the FOXO1 gene. [5] FOXO1 is a transcription factor that plays important roles in regulation of gluconeogenesis and glycogenolysis by insulin signaling , and is also central to the decision for a pre adipocyte to commit ...
Adipocyte FABP (A-FABP): Located in adipose tissue, A-FABP plays a crucial role in lipid metabolism, including the storage and release of fatty acids in adipocytes. Intestinal FABP (I-FABP): Found in the intestine, I-FABP is essential for the absorption and transport of dietary fatty acids.
These phosphinate MMP inhibitors contain phenyl segments that are thought to be responsible for the selectivity to MMP-13. The phosphinic group of those inhibitors (R 1 R 2 (O)OH) binds as a zinc ligand. R 1 and R 2 substituents affect the inhibition potency. [7] Phosphinate inhibitors have been developed that showed high selectivity for MMP-11.
Thiazolidinedione ligand dependent transactivation is responsible for the majority of anti-diabetic effects. The activated PPAR/RXR heterodimer binds to peroxisome proliferator hormone response elements upstream of target genes in complex with a number of coactivators such as nuclear receptor coactivator 1 and CREB binding protein, this causes upregulation of genes (for a full list see PPARγ):