Advanced search
Publication Cover
Expert Opinion on Investigational Drugs Volume 19, 2010 - Issue 4
Submit an article Journal homepage
458
Views
49
CrossRef citations to date
0
Altmetric
Reviews

Discovery and development of selective PPARγ modulators as safe and effective antidiabetic agents

Lalit S Doshi Department of Pharmacology, Piramal Life Sciences Limited, 1 Nirlon Complex, Goregaon (E), Mumbai - 400 063, India +91 22 3081 8404; +91 22 3081 8411; [email protected]
,
Manoja Kumar Brahma Department of Pharmacology, Piramal Life Sciences Limited, 1 Nirlon Complex, Goregaon (E), Mumbai - 400 063, India +91 22 3081 8404; +91 22 3081 8411; [email protected]
,
Umakant A Bahirat Department of Pharmacology, Piramal Life Sciences Limited, 1 Nirlon Complex, Goregaon (E), Mumbai - 400 063, India +91 22 3081 8404; +91 22 3081 8411; [email protected]
,
Amol V Dixit Department of Pharmacology, Piramal Life Sciences Limited, 1 Nirlon Complex, Goregaon (E), Mumbai - 400 063, India +91 22 3081 8404; +91 22 3081 8411; [email protected]
&
Kumar VS Nemmani Department of Pharmacology, Piramal Life Sciences Limited, 1 Nirlon Complex, Goregaon (E), Mumbai - 400 063, India +91 22 3081 8404; +91 22 3081 8411; [email protected]
, PhD
Pages 489-512 | Published online: 31 Mar 2010

Citations (49)

Keep up to date with the latest research on this topic with citation updates for this article.

Subscribe to citation updates

Read on this site (2)

Jacqueline Kung & Robert R Henry. (2012) Thiazolidinedione safety. Expert Opinion on Drug Safety 11:4, pages 565-579.
Read now
Aryan, B. Babu, S. Divakar, B. Gowramma, Srikanth Jupudi, Jagdish Chand & Vishnu Malakar Kumar. Rational design of thiazolidine-4-one-gallic acid hybrid derivatives as selective partial PPARγ modulators: an in-silico approach for type 2 diabetes treatment. Journal of Biomolecular Structure and Dynamics 0:0, pages 1-15.
Read now

Articles from other publishers (47)

Liangge Li, Jiafeng Geng, Wen Yu, Feifei Zhou, Zhihuan Zheng, Kaiyue Fu, Junjie Kong & Xiujing Feng. (2023) Inhibition of PPARγ by BZ26, a GW9662 derivate, attenuated obesity-related breast cancer progression by inhibiting the reprogramming of mature adipocytes into to cancer associate adipocyte-like cells. Frontiers in Pharmacology 14.
Crossref
Lei Ma, Junyuan Tang, Guihui Cai, Fangyuan Chen, Qingmei Liu, Zhi Zhou, Silin Zhang, Xiawen Liu, Ning Hou & Wei Yi. (2022) Structure-based screening and biological validation of the anti-thrombotic drug-dicoumarol as a novel and potent PPARγ-modulating ligand. Bioorganic Chemistry 129, pages 106191.
Crossref
Sangeeta Ballav, Bini Biswas, Vishal Kumar Sahu, Amit Ranjan & Soumya Basu. (2022) PPAR-γ Partial Agonists in Disease-Fate Decision with Special Reference to Cancer. Cells 11:20, pages 3215.
Crossref
Mohammed T. QAOUD, Ihab ALMASRI & Tijen ÖNKOL. (2022) Peroxisome Proliferator-Activated Receptors as Superior Targets for Treating Diabetic Disease, Design Strategies - Review Article. Turkish Journal of Pharmaceutical Sciences 19:3, pages 353-370.
Crossref
Haowen Jiang, X. Edward Zhou, Jingjing Shi, Zhi Zhou, Guanguan Zhao, Xinwen Zhang, Yili Sun, Kelly Suino-Powell, Lei Ma, Hui Gao, Xiyong Yu, Jia Li, Jingya Li, Karsten Melcher, H. Eric Xu & Wei Yi. (2020) Identification and structural insight of an effective PPARγ modulator with improved therapeutic index for anti-diabetic drug discovery. Chemical Science 11:8, pages 2260-2268.
Crossref
Yi Shen, Hongbo Chi, Jinhu Zhou, Lifei Luo, Qian Tu, Cancan Qi & Zuhua Gao. (2018) Structure-Based Stepwise Screening of PPARγ Antagonists as Potential Competitors with NCOA1 Coactivator Peptide for PPARγ CIS Site. International Journal of Peptide Research and Therapeutics 25:4, pages 1369-1377.
Crossref
Yi Huan, Xuan Pan, Jun Peng, Chunming Jia, Sujuan Sun, Guoliang Bai, Xing Wang, Tian Zhou, Rongcui Li, Shuainan Liu, Caina Li, Quan Liu, Zhanzhu Liu & Zhufang Shen. (2019) A novel specific peroxisome proliferator‐activated receptor γ (PPARγ) modulator YR4‐42 ameliorates hyperglycaemia and dyslipidaemia and hepatic steatosis in diet‐induced obese mice. Diabetes, Obesity and Metabolism 21:11, pages 2553-2563.
Crossref
Carmen del Rio, Irene Cantarero, Belén Palomares, María Gómez-Cañas, Javier Fernández-Ruiz, Carolina Pavicic, Adela García-Martín, Maria Luz Bellido, Rafaela Ortega-Castro, Carlos Pérez-Sánchez, Chary López-Pedrera, Giovanni Appendino, Marco A Calzado & Eduardo Muñoz. (2018) VCE-004.3, a cannabidiol aminoquinone derivative, prevents bleomycin-induced skin fibrosis and inflammation through PPARγ- and CB 2 receptor-dependent pathways . British Journal of Pharmacology 175:19, pages 3813-3831.
Crossref
Jean-Charles Fruchart. (2017) Pemafibrate (K-877), a novel selective peroxisome proliferator-activated receptor alpha modulator for management of atherogenic dyslipidaemia. Cardiovascular Diabetology 16:1.
Crossref
Neelaveni Thangavel, Mohammed Al Bratty, Sadique Akhtar Javed, Waquar Ahsan & Hassan A. Alhazmi. (2017) Targeting Peroxisome Proliferator-Activated Receptors Using Thiazolidinediones: Strategy for Design of Novel Antidiabetic Drugs. International Journal of Medicinal Chemistry 2017, pages 1-20.
Crossref
E. Muñoz, F. Pollastro, O. Taglialatela-Scafati & G. Appendino. 2017. Handbook of Cannabis and Related Pathologies. Handbook of Cannabis and Related Pathologies 671 679 .
Xiujing Feng, Dan Weng, Feifei Zhou, Young D. Owen, Haohan Qin, Jingfa Zhao, WenYu, Yahong Huang, Jiajia Chen, Haijian Fu, Nanfei Yang, Dianhua Chen, Jianxin Li, Renxiang Tan & Pingping Shen. (2016) Activation of PPARγ by a Natural Flavonoid Modulator, Apigenin Ameliorates Obesity-Related Inflammation Via Regulation of Macrophage Polarization. EBioMedicine 9, pages 61-76.
Crossref
Carmen del Río, Carmen Navarrete, Juan A. Collado, M. Luz Bellido, María Gómez-Cañas, M. Ruth Pazos, Javier Fernández-Ruiz, Federica Pollastro, Giovanni Appendino, Marco A. Calzado, Irene Cantarero & Eduardo Muñoz. (2016) The cannabinoid quinol VCE-004.8 alleviates bleomycin-induced scleroderma and exerts potent antifibrotic effects through peroxisome proliferator-activated receptor-γ and CB2 pathways. Scientific Reports 6:1.
Crossref
Philip Hallenborg, Rasmus K. Petersen, Irene Kouskoumvekaki, John W. Newman, Lise Madsen & Karsten Kristiansen. (2016) The elusive endogenous adipogenic PPARγ agonists: Lining up the suspects. Progress in Lipid Research 61, pages 149-162.
Crossref
Sascha Sauer. (2015) Ligands for the Nuclear Peroxisome Proliferator-Activated Receptor Gamma. Trends in Pharmacological Sciences 36:10, pages 688-704.
Crossref
Doris T. Chan, Gerald F. Watts, Ashley B. Irish & Gursharan K. Dogra. (2015) Insulin resistance and vascular dysfunction in chronic kidney disease: mechanisms and therapeutic interventions. Nephrology Dialysis Transplantation, pages gfv326.
Crossref
Zili Zhang, Mei Guo, Shifeng Zhao, Wenxuan Xu, Jiangjuan Shao, Feng Zhang, Li Wu, Yin Lu & Shizhong Zheng. (2015) The update on transcriptional regulation of autophagy in normal and pathologic cells: A novel therapeutic target. Biomedicine & Pharmacotherapy 74, pages 17-29.
Crossref
Yuval Ramot, Arianna Mastrofrancesco, Emanuela Camera, Pierre Desreumaux, Ralf Paus & Mauro Picardo. (2015) The role of PPAR γ -mediated signalling in skin biology and pathology: new targets and opportunities for clinical dermatology . Experimental Dermatology 24:4, pages 245-251.
Crossref
Lingling Fan, Jianta Wang, Xiao Ma, Wan Xiao, Zhiyan Li, Gang Zhong, Lei Tang & Haoshu Wu. (2015) Design, synthesis and biological evaluation of GY3-based derivatives for anti-type 2 diabetes activity. Bioorganic & Medicinal Chemistry Letters 25:7, pages 1500-1505.
Crossref
Mohamed A. Helal, Khaled M. Darwish & Mohamed A. Hammad. (2014) Homology modeling and explicit membrane molecular dynamics simulation to delineate the mode of binding of thiazolidinediones into FFAR1 and the mechanism of receptor activation. Bioorganic & Medicinal Chemistry Letters 24:22, pages 5330-5336.
Crossref
Limei Wang, Birgit Waltenberger, Eva-Maria Pferschy-Wenzig, Martina Blunder, Xin Liu, Clemens Malainer, Tina Blazevic, Stefan Schwaiger, Judith M. Rollinger, Elke H. Heiss, Daniela Schuster, Brigitte Kopp, Rudolf Bauer, Hermann Stuppner, Verena M. Dirsch & Atanas G. Atanasov. (2014) Natural product agonists of peroxisome proliferator-activated receptor gamma (PPARγ): a review. Biochemical Pharmacology 92:1, pages 73-89.
Crossref
Xiujing Feng, Haohan Qin, Qian Shi, Yang Zhang, Feifei Zhou, Haochen Wu, Sen Ding, Zhiyuan Niu, Yan Lu & Pingping Shen. (2014) Chrysin attenuates inflammation by regulating M1/M2 status via activating PPARγ. Biochemical Pharmacology 89:4, pages 503-514.
Crossref
Zhanjun Jia, Ying Sun, Guangrui Yang, Aihua Zhang, Songming Huang, Kristina Marie Heiney & Yue Zhang. (2014) New Insights into the PPAR γ Agonists for the Treatment of Diabetic Nephropathy . PPAR Research 2014, pages 1-7.
Crossref
Christopher Weidner, Sylvia J. Wowro, Morten Rousseau, Anja Freiwald, Vitam Kodelja, Heba Abdel-Aziz, Olaf Kelber & Sascha Sauer. (2013) Antidiabetic Effects of Chamomile Flowers Extract in Obese Mice through Transcriptional Stimulation of Nutrient Sensors of the Peroxisome Proliferator-Activated Receptor (PPAR) Family. PLoS ONE 8:11, pages e80335.
Crossref
Dang Vu-Phan, Vladimir Grachtchouk, Jingcheng Yu, Lesley A Colby, Max S Wicha & Ronald J Koenig. (2013) The thyroid cancer PAX8–PPARG fusion protein activates Wnt/TCF-responsive cells that have a transformed phenotype. Endocrine-Related Cancer 20:5, pages 725-739.
Crossref
Madhavi Agrawal, Prashant Kharkar, Sonali Moghe, Tushar Mahajan, Vaishali Deka, Chandni Thakkar, Amrutha Nair, Chirag Mehta, Julie Bose, Asha Kulkarni-Almeida, Dilip Bhedi & Ram A. Vishwakarma. (2013) Discovery of thiazolyl-phthalazinone acetamides as potent glucose uptake activators via high-throughput screening. Bioorganic & Medicinal Chemistry Letters 23:20, pages 5740-5743.
Crossref
Muralidhara Rao Maradana, Ranjeny Thomas & Brendan J. O'Sullivan. (2013) Targeted delivery of curcumin for treating type 2 diabetes. Molecular Nutrition & Food Research 57:9, pages 1550-1556.
Crossref
Korn?l Kistam?s, Norbert Szentandr?ssy, Bence Hegyi, Ferenc Ruzsnavszky, Krisztina V?czi, L?szl? B?r?ndi, Bal?zs Horv?th, Andrea Szebeni, J?nos Magyar, Tam?s B?ny?sz, Val?ria Kecskem?ti & P?ter P. N?n?si. (2013) Effects of pioglitazone on cardiac ion currents and action potential morphology in canine ventricular myocytes. European Journal of Pharmacology 710:1-3, pages 10-19.
Crossref
Ana B. Bueno, Ana M. Castaño & Ángel Rodríguez. 2013. Drug Discovery. Drug Discovery 205 243 .
Joshua P. Taygerly, Lawrence R. McGee, Steven M. Rubenstein, Jonathan B. Houze, Timothy D. Cushing, Yang Li, Alykhan Motani, Jin-Long Chen, Walter Frankmoelle, Guosen Ye, Marc R. Learned, Juan Jaen, Shichang Miao, Pieter B. Timmermans, Martin Thoolen, Patrick Kearney, John Flygare, Holger Beckmann, Jennifer Weiszmann, Michelle Lindstrom, Nigel Walker, Jinsong Liu, Donna Biermann, Zhulun Wang, Atsushi Hagiwara, Tetsuya Iida, Hisateru Aramaki, Yuki Kitao, Hisashi Shinkai, Noboru Furukawa, Jun Nishiu & Motonao Nakamura. (2013) Discovery of INT131: A selective PPARγ modulator that enhances insulin sensitivity. Bioorganic & Medicinal Chemistry 21:4, pages 979-992.
Crossref
Hyae Gyeong Cheon. (2013) Latest research and development trends in non-insulin anti-diabetics. Archives of Pharmacal Research 36:2, pages 145-153.
Crossref
Kalina DuszkaJuliane G. Bogner-Strauss, Hubert HacklDietmar RiederClaudia Neuhold, Andreas Prokesch, Zlatko TrajanoskiAnne-M. Krogsdam. (2013) Nr4a1 Is Required for Fasting-Induced Down-Regulation of Pparγ2 in White Adipose Tissue. Molecular Endocrinology 27:1, pages 135-149.
Crossref
Jean-Charles Fruchart. (2013) Selective peroxisome proliferator-activated receptorα modulators (SPPARMα): The next generation of peroxisome proliferator-activated receptor α-agonists. Cardiovascular Diabetology 12:1, pages 82.
Crossref
Feng Zhang, Desong Kong, Yin Lu & Shizhong Zheng. (2012) Peroxisome proliferator-activated receptor-γ as a therapeutic target for hepatic fibrosis: from bench to bedside. Cellular and Molecular Life Sciences 70:2, pages 259-276.
Crossref
Dirk A. Ridder & Markus Schwaninger. (2012) In search of the neuroprotective mechanism of thiazolidinediones in Parkinson's disease. Experimental Neurology 238:2, pages 133-137.
Crossref
Steven Richards. 2012. Bioactive Heterocyclic Compound Classes. Bioactive Heterocyclic Compound Classes 327 347 .
Y. Tan, E. S. Muise, H. Dai, R. Raubertas, K. K. Wong, G. M. Thompson, H. B. Wood, P. T. Meinke, P. Y. Lum, J. R. Thompson & J. P. Berger. (2012) Novel Transcriptome Profiling Analyses Demonstrate that Selective Peroxisome Proliferator-Activated Receptor   (PPAR ) Modulators Display Attenuated and Selective Gene Regulatory Activity in Comparison with PPAR  Full Agonists. Molecular Pharmacology 82:1, pages 68-79.
Crossref
Philippe Lefebvre & Bart Staels. (2012) Naturally improving insulin resistance with amorfrutins. Proceedings of the National Academy of Sciences 109:19, pages 7136-7137.
Crossref
Christopher WeidnerJens C. de GrootAman PrasadAnja FreiwaldClaudia QuedenauMagdalena KliemAnnabell WitzkeVitam KodeljaChung-Ting HanSascha GiegoldMatthias BaumannBert KleblKarsten Siems, Lutz Müller-Kuhrt, Annette Schürmann, Rita Schüler, Andreas F. H. Pfeiffer, Frank C. SchroederKonrad BüssowSascha Sauer. (2012) Amorfrutins are potent antidiabetic dietary natural products. Proceedings of the National Academy of Sciences 109:19, pages 7257-7262.
Crossref
Mairi Sime, Amanda C. Allan, Paul Chapman, Charlotte Fieldhouse, Gerard M.P. Giblin, Mark P. Healy, Millard H. Lambert, Lisa M. Leesnitzer, Ann Lewis, Raymond V. Merrihew, Richard A. Rutter, Rosemary Sasse, Barry G. Shearer, Timothy M. Wilson, Robert X. Xu & David J. Virley. (2011) Discovery of GSK1997132B a novel centrally penetrant benzimidazole PPARγ partial agonist. Bioorganic & Medicinal Chemistry Letters 21:18, pages 5568-5572.
Crossref
Jonathan P. Whitehead. (2011) Diabetes: New conductors for the peroxisome proliferator-activated receptor γ (PPARγ) orchestra. The International Journal of Biochemistry & Cell Biology 43:8, pages 1071-1074.
Crossref
Hannah SongPeter W. ZandstraMilica Radisic. (2011) Engineered Heart Tissue Model of Diabetic Myocardium. Tissue Engineering Part A 17:13-14, pages 1869-1878.
Crossref
JC Hancox. (2011) Cardiac ion channel modulation by the hypoglycaemic agent rosiglitazone. British Journal of Pharmacology 163:3, pages 496-498.
Crossref
N Szentandrássy, G Harmati, L Bárándi, J Simkó, B Horváth, J Magyar, T Bányász, I Lőrincz, A Szebeni, V Kecskeméti & PP Nánási. (2011) Effects of rosiglitazone on the configuration of action potentials and ion currents in canine ventricular cells. British Journal of Pharmacology 163:3, pages 499-509.
Crossref
Aviva Levina & Peter A. Lay. (2011) Metal-based anti-diabetic drugs: advances and challenges. Dalton Transactions 40:44, pages 11675.
Crossref
Ebenezer A. Nyenwe, Terri W. Jerkins, Guillermo E. Umpierrez & Abbas E. Kitabchi. (2011) Management of type 2 diabetes: evolving strategies for the treatment of patients with type 2 diabetes. Metabolism 60:1, pages 1-23.
Crossref
Uwe Grether, Werner Klaus, Bernd Kuhn, Hans Peter Maerki, Peter Mohr & Matthew B. Wright. (2010) New Insights on the Mechanism of PPAR-targeted Drugs. ChemMedChem 5:12, pages 1973-1976.
Crossref

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Order Reprints Request Corporate Permissions

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

Request Academic Permissions

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.

Related research

People also read lists articles that other readers of this article have read.

Recommended articles lists articles that we recommend and is powered by our AI driven recommendation engine.

Cited by lists all citing articles based on Crossref citations.
Articles with the Crossref icon will open in a new tab.