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PPAR -alpha and -gamma pathways. In the field of molecular biology, the peroxisome proliferator–activated receptors (PPARs) are a group of nuclear receptor proteins that function as transcription factors regulating the expression of genes. [1]
PPAR-alpha is activated under conditions of energy deprivation and is necessary for the process of ketogenesis, a key adaptive response to prolonged fasting. [ 8 ] [ 9 ] Activation of PPAR-alpha promotes uptake, utilization, and catabolism of fatty acids by upregulation of genes involved in fatty acid transport, fatty acid binding and ...
PPAR-alpha and -gamma pathways PPAR agonists are drugs which act upon the peroxisome proliferator-activated receptor . They are used for the treatment of symptoms of the metabolic syndrome , mainly for lowering triglycerides and blood sugar .
Three subtypes of PPARs are known: PPAR-alpha, PPAR-delta, and PPAR-gamma. 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 ...
Peroxisome proliferator-activated receptor gamma coactivator 1-alpha (PGC-1α) is a protein that in humans is encoded by the PPARGC1A gene. [4] PPARGC1A is also known as human accelerated region 20 . It may, therefore, have played a key role in differentiating humans from apes. [5] PGC-1α is the master regulator of mitochondrial biogenesis.
It is a first in class drug which acts as a dual PPAR agonist at the subtypes α (alpha) and γ (gamma) of the peroxisome proliferator-activated receptor (PPAR). Agonist action on PPARα lowers high blood triglycerides, and agonist action on PPARγ improves insulin resistance and consequently lowers blood sugar. [2]
Nuclear receptors are specific to metazoans (animals) and are not found in protists, algae, fungi, or plants. [8] Amongst the early-branching animal lineages with sequenced genomes, two have been reported from the sponge Amphimedon queenslandica, two from the comb jelly Mnemiopsis leidyi [9] four from the placozoan Trichoplax adhaerens and 17 from the cnidarian Nematostella vectensis. [10]
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):