Novel selective small molecule agonists for peroxisome proliferator-activated receptor delta (PPARdelta)--synthesis and biological activity.
paper
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- Authors
- Sznaidman, Marcos L; Haffner, Curt D; Maloney, Patrick R; Fivush, Adam; Chao, Esther; Goreham, Donna; Sierra, Michael L; LeGrumelec, Christelle; Xu, H Eric; Montana, Valerie G; Lambert, Millard H; Willson, Timothy M; Oliver, William R; Sternbach, Daniel D
- Year
- 2003
- Journal
- Bioorganic & medicinal chemistry letters
- PMID
- 12699745
- DOI
- 10.1016/s0960-894x(03)00207-5
We report the synthesis and biological activity of a new series of small molecule agonists of the human Peroxisome Proliferator-Activated Receptor delta (PPARdelta). Several hits were identified from our original libraries containing lipophilic carboxylic acids. Optimization of these hits by structure-guided design led to 7k (GW501516) and 7l (GW0742), which shows an EC(50) of 1.1 nM against PPARdelta with 1000-fold selectivity over the other human subtypes.
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| Title | Year | PMID |
|---|---|---|
| Peroxisome proliferator-activated receptors Ξ± and Ξ³ are linked with alcohol consumption in mice and withdrawal and dependence in humans. | 2015 | 25516156 |
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| Ligand activation of peroxisome proliferator-activated receptor-beta/delta inhibits cell proliferation in human HaCaT keratinocytes. | Borland MG et al. | β | 2008 | β |
| Ligand activation of peroxisome proliferator-activated receptor beta/delta (PPAR beta/delta) inhibits chemically induced skin tumorigenesis. | Bility MT et al. | β | 2008 | β |
| Peroxisome proliferator-activated receptor beta/delta activation improves angiotensin II-induced cardiac hypertrophy in vitro. | Sheng L et al. | β | 2008 | β |
| Peroxisome proliferator-activated receptor beta/delta expression and activation in lung cancer. | Pedchenko TV et al. | β | 2008 | β |
| Peroxisome proliferator-activated receptor-beta/delta (PPARbeta/delta) ligands inhibit growth of UACC903 and MCF7 human cancer cell lines. | Girroir EE et al. | β | 2008 | β |
| Peroxisome proliferator-activated receptor-delta agonist enhances vasculogenesis by regulating endothelial progenitor cells through genomic and nongenomic activations of the phosphatidylinositol 3-kinase/Akt pathway. | Han JK et al. | β | 2008 | β |
| Peroxisome proliferator-activated receptor gamma and lung cancer biology: implications for therapy. | Roman J | β | 2008 | β |
| PPAR alpha, more than PPAR delta, mediates the hepatic and skeletal muscle alterations induced by the PPAR agonist GW0742. | Faiola B et al. | β | 2008 | β |
| PPAR-delta in Vascular Pathophysiology. | Wang N | β | 2008 | β |
| PPARdelta regulates multiple proinflammatory pathways to suppress atherosclerosis. | Barish GD et al. | β | 2008 | β |
| Role of cyclooxygenase isoforms in prostacyclin biosynthesis and murine prehepatic portal hypertension. | Skill NJ et al. | β | 2008 | β |
| Role of nitric oxide and prostacyclin as vasoactive hormones released by the endothelium. | Mitchell JA et al. | β | 2008 | β |
| Role of peroxisome-proliferator-activated receptor beta/delta (PPARbeta/delta) in gastrointestinal tract function and disease. | Peters JM et al. | β | 2008 | β |
| SAR-oriented discovery of peroxisome proliferator-activated receptor pan agonist with a 4-adamantylphenyl group as a hydrophobic tail. | Kasuga J et al. | β | 2008 | β |
| Structural Development Studies of Subtype-Selective Ligands for Peroxisome Proliferator-Activated Receptors (PPARs) Based on the 3,4-Disubstituted Phenylpropanoic Acid Scaffold as a Versatile Template. | Miyachi H et al. | β | 2008 | β |
| A widely used retinoic acid receptor antagonist induces peroxisome proliferator-activated receptor-gamma activity. | Schupp M et al. | β | 2007 | β |
| Design, synthesis, and evaluation of potent, structurally novel peroxisome proliferator-activated receptor (PPAR) delta-selective agonists. | Kasuga J et al. | β | 2007 | β |
| Discovery of para-alkylthiophenoxyacetic acids as a novel series of potent and selective PPARdelta agonists. | Zhang R et al. | β | 2007 | β |
| Fenofibrate represses interleukin-17 and interferon-gamma expression and improves colitis in interleukin-10-deficient mice. | Lee JW et al. | β | 2007 | β |
| Lipids, lipoproteins, and peroxisome proliferator activated receptor-delta. | Sprecher DL | β | 2007 | β |
| Metabolic Functions of Peroxisome Proliferator-Activated Receptor beta/delta in Skeletal Muscle. | Gaudel C et al. | β | 2007 | β |
| Novel selective PPARdelta agonists: optimization of activity by modification of alkynylallylic moiety. | Havranek M et al. | β | 2007 | β |
| Peroxisome proliferator-activated receptor-beta/delta (PPARbeta/delta) ligands do not potentiate growth of human cancer cell lines. | Hollingshead HE et al. | β | 2007 | β |
| Peroxisome proliferator-activated receptor-delta, a regulator of oxidative capacity, fuel switching and cholesterol transport. | FΓΌrnsinn C et al. | β | 2007 | β |
| Peroxisome proliferator-activated receptor-delta upregulates 14-3-3 epsilon in human endothelial cells via CCAAT/enhancer binding protein-beta. | Brunelli L et al. | β | 2007 | β |
| Peroxisome proliferator-activated receptors in lung cancer. | Keshamouni VG et al. | β | 2007 | β |
| PPAR agonists: multimodal drugs for the treatment of type-2 diabetes. | Gross B et al. | β | 2007 | β |
| PPARbeta/delta activation inhibits angiotensin II-induced collagen type I expression in rat cardiac fibroblasts. | Zhang H et al. | β | 2007 | β |
| PPARdelta agonism induces a change in fuel metabolism and activation of an atrophy programme, but does not impair mitochondrial function in rat skeletal muscle. | Constantin D et al. | β | 2007 | β |
| PPAR delta agonists and metabolic diseases. | Kang K et al. | β | 2007 | β |
| Role of AMP kinase and PPARdelta in the regulation of lipid and glucose metabolism in human skeletal muscle. | KrΓ€mer DK et al. | β | 2007 | β |
| Synthesis and identification of [1,2,4]thiadiazole derivatives as a new series of potent and orally active dual agonists of peroxisome proliferator-activated receptors alpha and delta. | Shen L et al. | β | 2007 | β |
| The Effect of PPARalpha, PPARdelta, PPARgamma, and PPARpan Agonists on Body Weight, Body Mass, and Serum Lipid Profiles in Diet-Induced Obese AKR/J Mice. | Harrington WW et al. | β | 2007 | β |
| The PPARdelta agonist, GW501516, promotes fatty acid oxidation but has no direct effect on glucose utilisation or insulin sensitivity in rat L6 skeletal muscle cells. | Dimopoulos N et al. | β | 2007 | β |
| Triglyceride:high-density lipoprotein cholesterol effects in healthy subjects administered a peroxisome proliferator activated receptor delta agonist. | Sprecher DL et al. | β | 2007 | β |
| 1,3,5-Trisubstituted aryls as highly selective PPARdelta agonists. | Epple R et al. | β | 2006 | β |
| 3,4,5-Trisubstituted isoxazoles as novel PPARdelta agonists: Part 1. | Epple R et al. | β | 2006 | β |
| Concise and efficient asymmetric synthesis of (S)-2-ethylphenylpropanoic acid derivatives: dual agonists for human peroxisome proliferator-activated receptor alpha and delta. | Kasuga J et al. | β | 2006 | β |
| Cross-talk between peroxisome proliferator-activated receptor delta and cytosolic phospholipase A(2)alpha/cyclooxygenase-2/prostaglandin E(2) signaling pathways in human hepatocellular carcinoma cells. | Xu L et al. | β | 2006 | β |
| Design and synthesis of substituted phenylpropanoic acid derivatives as human peroxisome proliferator-activated receptor alpha/delta dual agonists. | Kasuga J et al. | β | 2006 | β |
| Design, synthesis, and evaluation of a novel series of alpha-substituted phenylpropanoic acid derivatives as human peroxisome proliferator-activated receptor (PPAR) alpha/delta dual agonists for the treatment of metabolic syndrome. | Kasuga J et al. | β | 2006 | β |
| Identification of novel PPARalpha ligands by the structural modification of a PPARgamma ligand. | Usui S et al. | β | 2006 | β |
| Ligand activation of peroxisome proliferator-activated receptor beta inhibits colon carcinogenesis. | Marin HE et al. | β | 2006 | β |
| Mono(2-ethylhexyl)phthalate and mono-n-butyl phthalate activation of peroxisome proliferator activated-receptors alpha and gamma in breast. | Venkata NG et al. | β | 2006 | β |
| PPARbeta/delta selectively induces differentiation and inhibits cell proliferation. | Kim DJ et al. | β | 2006 | β |
| Regulation of inflammation by PPARs: a future approach to treat lung inflammatory diseases? | Becker J et al. | β | 2006 | β |
| Retracted: A novel positive feedback loop between peroxisome proliferator-activated receptor-delta and prostaglandin E2 signaling pathways for human cholangiocarcinoma cell growth. | Xu L et al. | β | 2006 | β |
| Short-term activation of peroxysome proliferator-activated receptor beta/delta increases fatty acid oxidation but does not restore insulin action in muscle cells from type 2 diabetic patients. | Debard C et al. | β | 2006 | β |
| Studies towards the conception of new selective PPARbeta/delta ligands. | BassΓ©ne CE et al. | β | 2006 | β |
| Synthesis of the PPARbeta/delta-selective agonist GW501516 and C4-thiazole-substituted analogs. | Pereira R et al. | β | 2006 | β |
| The toxicology of ligands for peroxisome proliferator-activated receptors (PPAR). | Peraza MA et al. | β | 2006 | β |
| Chemoselective arylamidine cyclizations: mild formation of 2-arylimidazole-4-carboxylic acids. | Yoburn JC et al. | β | 2005 | β |
| Differential responses of PPARalpha, PPARdelta, and PPARgamma reporter cell lines to selective PPAR synthetic ligands. | Seimandi M et al. | β | 2005 | β |
| Direct activation of glucose transport in primary human myotubes after activation of peroxisome proliferator-activated receptor delta. | KrΓ€mer DK et al. | β | 2005 | β |
| Expression and regulation of sterol 27-hydroxylase (CYP27A1) in human macrophages: a role for RXR and PPARgamma ligands. | Quinn CM et al. | β | 2005 | β |
| Minor structural modifications convert a selective PPARalpha agonist into a potent, highly selective PPARdelta agonist. | Weigand S et al. | β | 2005 | β |
| Peroxisome proliferator-activated receptor beta/delta as a therapeutic target for metabolic diseases. | Bedu E et al. | β | 2005 | β |
| Peroxisome proliferator-activated receptors and their ligands: entry into the post-glucocorticoid era of skin treatment? | Weindl G et al. | β | 2005 | β |
| Protective effects of a peroxisome proliferator-activated receptor-beta/delta agonist in experimental autoimmune encephalomyelitis. | Polak PE et al. | β | 2005 | β |
| Recent applications of protein crystallography and structure-guided drug design. | Williams SP et al. | β | 2005 | β |
| Reduced cholesterol absorption upon PPARdelta activation coincides with decreased intestinal expression of NPC1L1. | van der Veen JN et al. | β | 2005 | β |
| Roles of PPAR delta in lipid absorption and metabolism: a new target for the treatment of type 2 diabetes. | Luquet S et al. | β | 2005 | β |
| Rosiglitazone induces interleukin-1 receptor antagonist in interleukin-1beta-stimulated rat synovial fibroblasts via a peroxisome proliferator-activated receptor beta/delta-dependent mechanism. | Moulin D et al. | β | 2005 | β |
| Differential inhibition of macrophage foam-cell formation and atherosclerosis in mice by PPARalpha, beta/delta, and gamma. | Li AC et al. | β | 2004 | β |
| Effect of the peroxisome proliferator-activated receptor beta activator GW0742 in rat cultured cerebellar granule neurons. | Smith SA et al. | β | 2004 | β |
| Polyunsaturated fatty acids including docosahexaenoic and arachidonic acid bind to the retinoid X receptor alpha ligand-binding domain. | Lengqvist J et al. | β | 2004 | β |
| Roles of peroxisome proliferator-activated receptor delta in skeletal muscle function and adaptation. | Fredenrich A et al. | β | 2004 | β |
| A short and efficient synthesis of the pharmacological research tool GW501516 for the peroxisome proliferator-activated receptor delta. | Wei ZL et al. | β | 2003 | β |