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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):
The best-known PPAR ligands are the thiazolidinediones. After PPARδ (delta) was identified in humans in 1992, [9] it turned out to be closely related to PPARβ (beta), previously described during the same year in an amphibian, Xenopus.
Action Research is a quarterly peer-reviewed academic journal that covers the field of action research. The journal was established in 2003 and is published by SAGE Publications . The editor-in-chief is Hilary Bradbury ( AR+ Foundation ).
Stress is a bimonthly peer-reviewed medical journal covering research on stress in terms of: the mechanisms of stressful stimulation, the physiological and behavioural responses to stress, and their regulation, in both the short and long term; adaptive mechanisms, and the pathological consequences of stress. This includes research in physiology ...
Thiazolidines functionalized with carbonyls at the 2 and 4 positions, the thiazolidinediones, are drugs used in the treatment of diabetes mellitus type 2. Rhodanine is a related bioactive species, featuring one carbonyl and one thiocarbonyl. Many thiazolidines are prepared from cysteine and related aminothiols.
This is a list of notable medical and scientific journals that publish articles in pharmacology and the pharmaceutical sciences This is a dynamic list and may never be able to satisfy particular standards for completeness.
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In addition, there is continuing research and development of new γ/δ PPAR agonists for additional therapeutic indications, as well as "pan" agonists acting on all three isoforms. [10] [11] The anti-hypertension drug telmisartan is known to have PPAR γ/δ dual partial agonist activity in vivo. It also activates PPAR-α in vitro. [12]