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Selective PPAR Modulator
A selective PPAR modulator (SPPARM) is a selective receptor modulator of the peroxisome proliferator-activated receptor (PPAR). Examples include SPPARMs of the PPARγ, BADGE, EPI-001, INT-131, MK-0533, and S26948. See also * PPAR agonist 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. Classification PPAR-alpha and PPAR-g ... References PPAR agonists {{pharmacology-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Selective Receptor Modulator
In the field of pharmacology, a selective receptor modulator or SRM is a type of drug that has different effects in different tissues. An SRM may behave as an agonist in some tissues while as an antagonist in others. Hence selective receptor modulators are sometimes referred to as tissue selective drugs or mixed agonists / antagonists. This tissue selective behavior is in contrast to many other drugs that behave either as agonists or antagonists regardless of the tissue in question. Classes Classes of selective receptor modulators include: * Selective androgen receptor modulator (SARM) * Selective estrogen receptor modulator (SERM) * Selective glucocorticoid receptor modulator (SEGRM) * Selective progesterone receptor modulator (SPRM) * Selective PPAR modulator (SPPARM) including SPPARMγ (affecting the PPARγ) and SPPARMα ( PPARα) See also * Agonist–antagonist * Selective glucocorticoid receptor agonist Selective glucocorticoid receptor modulators (SEGRMs) and s ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Peroxisome Proliferator-activated Receptor
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 gene expression. PPARs play essential roles in regulating cell differentiation, cellular differentiation, developmental biology, development, and metabolism (carbohydrate metabolism, carbohydrate, lipid metabolism, lipid, protein metabolism, protein), and tumorigenesis Nomenclature and tissue distribution Three types of PPARs have been identified: alpha, PPARG, gamma, and delta (beta): * Peroxisome proliferator-activated receptor alpha, α (alpha) - expressed in liver, kidney, heart, muscle, adipose tissue, and others * Peroxisome proliferator-activated receptor delta, β/δ (beta/delta) - expressed in many tissues, especially in brain, adipose tissue, and skin * Peroxisome proliferator-activated receptor gamma, γ (gamma) - although transcribed by the same gene, this PPAR, by way of alternativ ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
PPARγ
Peroxisome proliferator-activated receptor gamma (PPAR-γ or PPARG), also known as the glitazone reverse insulin resistance receptor, or NR1C3 (nuclear receptor subfamily 1, group C, member 3) is a type II nuclear receptor functioning as a transcription factor that in humans is encoded by the ''PPARG'' gene. Tissue distribution PPARG is mainly present in adipose tissue, colon and macrophages. Two isoforms of PPARG are detected in the human and in the mouse: PPAR-γ1 (found in nearly all tissues except muscle) and PPAR-γ2 (mostly found in adipose tissue and the intestine). Gene expression This gene encodes a member of the peroxisome proliferator-activated receptor (PPAR) subfamily of nuclear receptors. PPARs form heterodimers with retinoid X receptors (RXRs) and these heterodimers regulate transcription of various genes. 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 dif ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bisphenol A Diglycidyl Ether
Bisphenol A diglycidyl ether (commonly abbreviated BADGE or DGEBA) is an organic compound and is a liquid epoxy resin. The compound is a colorless viscous liquid (commercial samples can appear pale straw-coloured). It is a key component of many epoxy resin formulations. Addition of further Bisphenol A and a catalyst and heat can produce Bisphenol A glycidyl ether epoxy resins of higher molecular weight that are solid. Preparation and reactions It is prepared by O-alkylation of bisphenol A with epichlorohydrin. This reaction mainly affords bisphenol A diglycidyl ether, as well as some oligomer. The degree of polymerization may be as low as 0.1. The epoxide content of such epoxy resins is of interest. This parameter is commonly expressed as the epoxide number, which is the number of epoxide equivalents in 1 kg of resin (Eq./kg), or as the equivalent weight, which is the weight in grams of resin containing 1 mole equivalent of epoxide (g/mol). Since unsymmetrical epoxides ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
EPI-001
EPI-001 is the first inhibitor of the androgen receptor amino-terminal domain. The single stereoisomer of EPI-001, EPI-002, is a first-in-class drug that the USAN council assigned a new stem class "-aniten" and the generic name "ralaniten". This distinguishes the anitens novel molecular mechanism from anti androgens that bind the C-terminus ligand-binding domain and have the stem class "lutamide" (such as flutamide, nilutamide, bicalutamide, enzalutamide, etc.). EPI-001 and its stereoisomers and analogues were discovered by Marianne Sadar and Raymond Andersen, who co-founded the pharmaceutical company ESSA Pharma Inc (Vancouver, Canada) for the clinical development of anitens for the treatment of castration-resistant prostate cancer (CRPC). EPI-001 is an receptor antagonist, antagonist of the androgen receptor (AR) that acts by binding covalently to the N-terminal domain (NTD) of the AR and blocking protein-protein interactions required for gene transcription, transcriptional act ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
S26948
S, or s, is the nineteenth letter of the Latin alphabet, used in the English alphabet, the alphabets of other western European languages and other latin alphabets worldwide. Its name in English is ''ess'' (pronounced ), plural ''esses''. History Northwest Semitic šîn represented a voiceless postalveolar fricative (as in 'ip'). It originated most likely as a pictogram of a tooth () and represented the phoneme via the acrophonic principle. Ancient Greek did not have a "sh" phoneme, so the derived Greek letter Sigma () came to represent the voiceless alveolar sibilant . While the letter shape Σ continues Phoenician ''šîn'', its name ''sigma'' is taken from the letter ''Samekh'', while the shape and position of ''samekh'' but name of ''šîn'' is continued in the '' xi''. Within Greek, the name of ''sigma'' was influenced by its association with the Greek word (earlier ), "to hiss". The original name of the letter "Sigma" may have been ''san'', but due to the earl ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
PPAR Agonist
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. Classification PPAR-alpha and PPAR-gamma are the molecular targets of a number of marketed drugs. The main classes of PPAR agonists are: PPAR-alpha agonists An endogenous compound, 7(S)-Hydroxydocosahexaenoic Acid (7(S)-HDHA), which is a Docosanoid derivative of the omega-3 fatty acid DHA was isolated as an endogenous high affinity ligand for PPAR-alpha in the rat and mouse brain. The 7(S) enantiomer bound with micromolar affity to PPAR alpha with 10 fold higher affinity compared to the (R) enantiomer and could trigger dendritic activation. PPARα (alpha) is the main target of fibrate drugs, a class of amphipathic carboxylic acids ( clofibrate, gemfibrozil, ciprofibrate, bezafibrate, and fenofibrate). They were originally indicated for dyslipidemia of cholesterol and more ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
