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Items: 1 to 20 of 99

1.

Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization.

Shinozuka T, Tsukada T, Fujii K, Tokumaru E, Shimada K, Onishi Y, Matsui Y, Wakimoto S, Kuroha M, Ogata T, Araki K, Ohsumi J, Sawamura R, Watanabe N, Yamamoto H, Fujimoto K, Tani Y, Mori M, Tanaka J.

Bioorg Med Chem. 2018 Oct 1;26(18):5099-5117. doi: 10.1016/j.bmc.2018.09.005. Epub 2018 Sep 8.

PMID:
30220602
2.

Discovery of DS-6930, a potent selective PPARγ modulator. Part I: Lead identification.

Shinozuka T, Tsukada T, Fujii K, Tokumaru E, Shimada K, Onishi Y, Matsui Y, Wakimoto S, Kuroha M, Ogata T, Araki K, Ohsumi J, Sawamura R, Watanabe N, Yamamoto H, Fujimoto K, Tani Y, Mori M, Tanaka J.

Bioorg Med Chem. 2018 Oct 1;26(18):5079-5098. doi: 10.1016/j.bmc.2018.09.006. Epub 2018 Sep 8.

PMID:
30241907
3.

Potent Anti-Diabetic Actions of a Novel Non-Agonist PPARγ Ligand that Blocks Cdk5-Mediated Phosphorylation.

Kamenecka TM, Busby SA, Kumar N, Choi JH, Banks AS, Vidovic D, Cameron MD, Schurer SC, Mercer BA, Hodder P, Spiegelman BM, Griffin PR.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2011 Jul 5 [updated 2013 Mar 7].

4.

Characterization of telmisartan-derived PPARγ agonists: importance of moiety shift from position 6 to 5 on potency, efficacy and cofactor recruitment.

Herbst L, Goebel M, Bandholtz S, Gust R, Kintscher U.

ChemMedChem. 2012 Nov;7(11):1935-42. doi: 10.1002/cmdc.201200337.

PMID:
24155042
5.

The Development of INT131 as a Selective PPARgamma Modulator: Approach to a Safer Insulin Sensitizer.

Higgins LS, Mantzoros CS.

PPAR Res. 2008;2008:936906. doi: 10.1155/2008/936906.

6.

Selective targeting of PPARγ by the natural product chelerythrine with a unique binding mode and improved antidiabetic potency.

Zheng W, Qiu L, Wang R, Feng X, Han Y, Zhu Y, Chen D, Liu Y, Jin L, Li Y.

Sci Rep. 2015 Jul 17;5:12222. doi: 10.1038/srep12222.

7.

L312, a novel PPARγ ligand with potent anti-diabetic activity by selective regulation.

Xie X, Zhou X, Chen W, Long L, Li W, Yang X, Li S, Wang L.

Biochim Biophys Acta. 2015 Jan;1850(1):62-72. doi: 10.1016/j.bbagen.2014.09.027. Epub 2014 Oct 12.

PMID:
25305559
8.

A unique PPARgamma ligand with potent insulin-sensitizing yet weak adipogenic activity.

Rocchi S, Picard F, Vamecq J, Gelman L, Potier N, Zeyer D, Dubuquoy L, Bac P, Champy MF, Plunket KD, Leesnitzer LM, Blanchard SG, Desreumaux P, Moras D, Renaud JP, Auwerx J.

Mol Cell. 2001 Oct;8(4):737-47.

9.

PAT5A: a partial agonist of peroxisome proliferator-activated receptor gamma is a potent antidiabetic thiazolidinedione yet weakly adipogenic.

Misra P, Chakrabarti R, Vikramadithyan RK, Bolusu G, Juluri S, Hiriyan J, Gershome C, Rajjak A, Kashireddy P, Yu S, Surapureddi S, Qi C, Zhu YJ, Rao MS, Reddy JK, Ramanujam R.

J Pharmacol Exp Ther. 2003 Aug;306(2):763-71. Epub 2003 May 2.

10.

PPAR(gamma) and glucose homeostasis.

Picard F, Auwerx J.

Annu Rev Nutr. 2002;22:167-97. Epub 2002 Jan 4. Review.

PMID:
12055342
11.

Distinct properties and advantages of a novel peroxisome proliferator-activated protein [gamma] selective modulator.

Berger JP, Petro AE, Macnaul KL, Kelly LJ, Zhang BB, Richards K, Elbrecht A, Johnson BA, Zhou G, Doebber TW, Biswas C, Parikh M, Sharma N, Tanen MR, Thompson GM, Ventre J, Adams AD, Mosley R, Surwit RS, Moller DE.

Mol Endocrinol. 2003 Apr;17(4):662-76. Epub 2003 Jan 16.

PMID:
12554792
12.

A novel partial agonist of peroxisome proliferator-activated receptor-gamma (PPARgamma) recruits PPARgamma-coactivator-1alpha, prevents triglyceride accumulation, and potentiates insulin signaling in vitro.

Burgermeister E, Schnoebelen A, Flament A, Benz J, Stihle M, Gsell B, Rufer A, Ruf A, Kuhn B, Märki HP, Mizrahi J, Sebokova E, Niesor E, Meyer M.

Mol Endocrinol. 2006 Apr;20(4):809-30. Epub 2005 Dec 22.

PMID:
16373399
13.

PAM-1616, a selective peroxisome proliferator-activated receptor γ modulator with preserved anti-diabetic efficacy and reduced adverse effects.

Kim MK, Chae YN, Choi SH, Moon HS, Son MH, Bae MH, Choi HH, Hur Y, Kim E, Park YH, Park CS, Kim JG, Lim JI, Shin CY.

Eur J Pharmacol. 2011 Jan 15;650(2-3):673-81. doi: 10.1016/j.ejphar.2010.10.044. Epub 2010 Oct 23.

PMID:
20974124
14.

A novel selective peroxisome proliferator-activator receptor-gamma modulator-SPPARgammaM5 improves insulin sensitivity with diminished adverse cardiovascular effects.

Chang CH, McNamara LA, Wu MS, Muise ES, Tan Y, Wood HB, Meinke PT, Thompson JR, Doebber TW, Berger JP, McCann ME.

Eur J Pharmacol. 2008 Apr 14;584(1):192-201. doi: 10.1016/j.ejphar.2007.12.036. Epub 2008 Feb 14.

PMID:
18346728
15.

Discovery of a novel selective PPARgamma modulator from (-)-Cercosporamide derivatives.

Furukawa A, Arita T, Satoh S, Wakabayashi K, Hayashi S, Matsui Y, Araki K, Kuroha M, Ohsumi J.

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2095-8. doi: 10.1016/j.bmcl.2010.02.073. Epub 2010 Feb 20.

PMID:
20219371
16.

Sulfonylthiadiazoles with an unusual binding mode as partial dual peroxisome proliferator-activated receptor (PPAR) γ/δ agonists with high potency and in vivo efficacy.

Keil S, Matter H, Schönafinger K, Glien M, Mathieu M, Marquette JP, Michot N, Haag-Diergarten S, Urmann M, Wendler W.

ChemMedChem. 2011 Apr 4;6(4):633-53. doi: 10.1002/cmdc.201100047. Epub 2011 Mar 11.

PMID:
21400663
17.

FK614, a novel peroxisome proliferator-activated receptor gamma modulator, induces differential transactivation through a unique ligand-specific interaction with transcriptional coactivators.

Fujimura T, Sakuma H, Konishi S, Oe T, Hosogai N, Kimura C, Aramori I, Mutoh S.

J Pharmacol Sci. 2005 Dec;99(4):342-52. Epub 2005 Nov 26.

18.

Selective Tissue Distribution Mediates Tissue-Dependent PPARγ Activation and Insulin Sensitization by INT131, a Selective PPARγ Modulator.

Xie X, Chen W, Zhang N, Yuan M, Xu C, Zheng Z, Li H, Wang L.

Front Pharmacol. 2017 May 30;8:317. doi: 10.3389/fphar.2017.00317. eCollection 2017.

19.

Amorfrutin B is an efficient natural peroxisome proliferator-activated receptor gamma (PPARγ) agonist with potent glucose-lowering properties.

Weidner C, Wowro SJ, Freiwald A, Kawamoto K, Witzke A, Kliem M, Siems K, Müller-Kuhrt L, Schroeder FC, Sauer S.

Diabetologia. 2013 Aug;56(8):1802-12. doi: 10.1007/s00125-013-2920-2. Epub 2013 May 18.

PMID:
23680913
20.

Discovery of INT131: a selective PPARγ modulator that enhances insulin sensitivity.

Taygerly JP, McGee LR, Rubenstein SM, Houze JB, Cushing TD, Li Y, Motani A, Chen JL, Frankmoelle W, Ye G, Learned MR, Jaen J, Miao S, Timmermans PB, Thoolen M, Kearney P, Flygare J, Beckmann H, Weiszmann J, Lindstrom M, Walker N, Liu J, Biermann D, Wang Z, Hagiwara A, Iida T, Aramaki H, Kitao Y, Shinkai H, Furukawa N, Nishiu J, Nakamura M.

Bioorg Med Chem. 2013 Feb 15;21(4):979-92. doi: 10.1016/j.bmc.2012.11.058. Epub 2012 Dec 10.

PMID:
23294830

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