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Review

PPAR-β/δ agonists for Type 2 diabetes and dyslipidemia: an adopted orphan still looking for a home

, PhD
Pages 1465-1471 | Published online: 22 Sep 2008

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Melissa A. Davidson, Donald R. Mattison, Laurent Azoulay & Daniel Krewski. (2018) Thiazolidinedione drugs in the treatment of type 2 diabetes mellitus: past, present and future. Critical Reviews in Toxicology 48:1, pages 52-108.
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Kuan-Chung Chen, Su-Sen Chang, Hung-Jin Huang, Tu-Liang Lin, Yong-Jiang Wu & Calvin Yu-Chian Chen. (2012) Three-in-one agonists for PPAR-α, PPAR-γ, and PPAR-δ from traditional Chinese medicine. Journal of Biomolecular Structure and Dynamics 30:6, pages 662-683.
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Hung-Jin Huang, Kuei-Jen Lee, Hsin Wei Yu, Hsin-Yi Chen, Fuu-Jen Tsai & Calvin Yu-Chian Chen. (2010) A Novel Strategy for Designing the Selective PPAR Agonist by the “Sum of Activity” Model. Journal of Biomolecular Structure and Dynamics 28:2, pages 187-200.
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Binggong Zhao, Zhiqiang Xin, Ping Ren & Huijian Wu. (2022) The Role of PPARs in Breast Cancer. Cells 12:1, pages 130.
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Shivanand Pudakalakatti, Mark Titus, José S. Enriquez, Sumankalai Ramachandran, Niki M. Zacharias, Imad Shureiqi, Yi Liu, James C. Yao, Xiangsheng Zuo & Pratip K. Bhattacharya. (2022) Identifying the Metabolic Signatures of PPARD-Overexpressing Gastric Tumors. International Journal of Molecular Sciences 23:3, pages 1645.
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Donald J. AbrahamRalf Glatthar & Robert H. Arch. 2003. Burger's Medicinal Chemistry and Drug Discovery. Burger's Medicinal Chemistry and Drug Discovery 1 71 .
Donald J. AbrahamPeter T.W. Cheng, Ellen Kick & Ranjan Mukherjee. 2003. Burger's Medicinal Chemistry and Drug Discovery. Burger's Medicinal Chemistry and Drug Discovery 1 117 .
Mohammad Zarei, David Aguilar-Recarte, Xavier Palomer & Manuel Vázquez-Carrera. (2021) Revealing the role of peroxisome proliferator-activated receptor β/δ in nonalcoholic fatty liver disease. Metabolism 114, pages 154342.
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Tara Man Kadayat, Aarajana Shrestha, Yong Hyun Jeon, Hongchan An, Jina Kim, Sung Jin Cho & Jungwook Chin. (2020) Targeting Peroxisome Proliferator-Activated Receptor Delta (PPARδ): A Medicinal Chemistry Perspective. Journal of Medicinal Chemistry 63:18, pages 10109-10134.
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Dong-Su Kim, Jaehwan Lee, Ashwini M. Londhe, Tara Man Kadayat, Jeongmin Joo, Hayoung Hwang, Kyung-Hee Kim, Ae Nim Pae, Jungwook Chin, Sung Jin Cho & Heonjoong Kang. (2018) Synthesis and evaluation of an orally available “Y”-shaped biaryl peroxisome proliferator-activated receptor δ agonist. Bioorganic & Medicinal Chemistry 26:15, pages 4382-4389.
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Fan Hong, Pengfei Xu & Yonggong Zhai. (2018) The Opportunities and Challenges of Peroxisome Proliferator-Activated Receptors Ligands in Clinical Drug Discovery and Development. International Journal of Molecular Sciences 19:8, pages 2189.
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Xavier Palomer, Emma Barroso, Javier Pizarro-Delgado, Lucía Peña, Gaia Botteri, Mohammad Zarei, David Aguilar, Marta Montori-Grau & Manuel Vázquez-Carrera. (2018) PPARβ/δ: A Key Therapeutic Target in Metabolic Disorders. International Journal of Molecular Sciences 19:3, pages 913.
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Mario Thevis, Oliver Krug, Hans Geyer, Katja Walpurgis, Norbert Baume & Andreas Thomas. (2018) Analytical challenges in sports drug testing. Analytical and Bioanalytical Chemistry 410:9, pages 2275-2281.
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Fahrettin Haczeyni, Hans Wang, Vanessa Barn, Auvro R. Mridha, Matthew M. Yeh, W. Geoffrey Haigh, George N. Ioannou, Yun‐Jung Choi, Charles A. McWherter, Narcissus C.‐H. Teoh & Geoffrey C. Farrell. (2017) The selective peroxisome proliferator–activated receptor‐delta agonist seladelpar reverses nonalcoholic steatohepatitis pathology by abrogating lipotoxicity in diabetic obese mice. Hepatology Communications 1:7, pages 663-674.
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Kyeongkyu Kim, Kyungjin Boo, Young Suk Yu, Se Kyu Oh, Hyunkyung Kim, Yoon Jeon, Jinhyuk Bhin, Daehee Hwang, Keun Il Kim, Jun-Su Lee, Seung-Soon Im, Seul Gi Yoon, Il Yong Kim, Je Kyung Seong, Ho Lee, Sungsoon Fang & Sung Hee Baek. (2017) RORα controls hepatic lipid homeostasis via negative regulation of PPARγ transcriptional network. Nature Communications 8:1.
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Shogo Okazaki, Ryuta Shioi, Tomomi Noguchi-Yachide, Minoru Ishikawa, Makoto Makishima, Yuichi Hashimoto & Takao Yamaguchi. (2016) Structure–activity relationship studies of non-carboxylic acid peroxisome proliferator-activated receptor α/δ (PPARα/δ) dual agonists. Bioorganic & Medicinal Chemistry 24:21, pages 5455-5461.
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Xavier Palomer, Emma Barroso, Mohammad Zarei, Gaia Botteri & Manuel Vázquez-Carrera. (2016) PPARβ/δ and lipid metabolism in the heart. Biochimica et Biophysica Acta (BBA) - Molecular and Cell Biology of Lipids 1861:10, pages 1569-1578.
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Manuel Vázquez-Carrera. (2016) Unraveling the Effects of PPARβ/δ on Insulin Resistance and Cardiovascular Disease. Trends in Endocrinology & Metabolism 27:5, pages 319-334.
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