Peroxisome proliferator-activated receptor translational research and clinical experience.
- Authors
- Cheatham, Wayman Wendell
- Year
- 2010
- Journal
- The American journal of clinical nutrition
- PMID
- 19923366
- DOI
- 10.3945/ajcn.2009.28449D
Since the early 1970s, pharmaceutical biochemists have sought to exploit the scientific findings that were uncovered when they studied the basis for the function and mode of action of fibric acid derivatives. In the early 1970s, little was known of peroxisome proliferator-activated receptors (PPARs), even in concept. Since then, however, the development of bioactive small molecules in medicinal science has resulted in tools developed to be inserted into the PPAR-binding domain, which has resulted in the recognition of literally thousands of possible biological effects of binding configurations. In diabetes care, the first of the marketed agents from these discoveries and developments was introduced in 1996. It was potent and did its job well. However, the use of this early form of thiazolidinedione sometimes, although rarely, led to fulminant liver failure, and ultimately the drug was removed from the market. Subsequent thiazolidinediones have been developed, and 2 have been relatively successful. However, they are not without their problems. This article describes the history of the development of these drugs, identifies the valuable attributes that they possess, and gives a clear rationale as to why a quest for a "safer" PPAR agonist is still being sought.
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In this knowledge base
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|---|---|---|
| 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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| History of current non-insulin medications for diabetes mellitus. | Quianzon CC et al. | β | 2012 | β |
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| Emerging options in the treatment of dyslipidemias: a bright future? | Florentin M et al. | β | 2011 | β |
| Improving glucose metabolism with resveratrol in a swine model of metabolic syndrome through alteration of signaling pathways in the liver and skeletal muscle. | Burgess TA et al. | β | 2011 | β |
| Pharmacophore-driven identification of PPARΞ³ agonists from natural sources. | Petersen RK et al. | β | 2011 | β |
| Targeting the peroxisome proliferator-activated receptors (PPARs) in spinal cord injury. | Esposito E et al. | β | 2011 | β |
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