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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]
In May 2010, the U.S. Food and Drug Administration (FDA) approved a revised label for Xenical to include new safety information about rare cases of severe liver injury that have been reported with the use of this medication. [33] A 2010 phase 2 trial found cetilistat significantly reduced weight and was better tolerated than orlistat. [34]
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.
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):
All proton pump inhibitors except for rabeprazole and pantoprazole are metabolized by the hepatic CYP450 enzyme and therefore, may interact with the metabolism of clopidogrel. Omeprazole is considered to have higher potential for drug-drug interaction than other protein pump inhibitors because it is a CYP2C19 inhibitor. [17]
1244 12780 Ensembl ENSG00000023839 ENSMUSG00000025194 UniProt Q92887 Q8VI47 RefSeq (mRNA) NM_000392 NM_013806 RefSeq (protein) NP_000383 NP_038834 Location (UCSC) Chr 10: 99.78 – 99.85 Mb Chr 19: 43.77 – 43.83 Mb PubMed search Wikidata View/Edit Human View/Edit Mouse Multidrug resistance-associated protein 2 (MRP2) also called canalicular multispecific organic anion transporter 1 (cMOAT ...
A specific inhibitor against idiopathic pulmonary fibrosis showed promising results in a phase II trial that ended in May 2018. [9] A DNA aptamer inhibitor of Autotaxin has also been described. [10] Recently, it has been shown that THC is also a partial autotaxin inhibitor, with an apparent IC50 of 407 ± 67 nM for the ATX-gamma isoform. [11]
P2Y 12 is a chemoreceptor for adenosine diphosphate (ADP) [5] [6] that belongs to the G i class of a group of G protein-coupled (GPCR) purinergic receptors. [7] This P2Y receptor family has several receptor subtypes with different pharmacological selectivity, which overlaps in some cases, for various adenosine and uridine nucleotides.