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Pharmacological repression of PPARγ promotes osteogenesis.
Marciano DP, Kuruvilla DS, Boregowda SV, Asteian A, Hughes TS, Garcia-Ordonez R, Corzo CA, Khan TM, Novick SJ, Park H, Kojetin DJ, Phinney DG, Bruning JB, Kamenecka TM, Griffin PR. Marciano DP, et al. Nat Commun. 2015 Jun 12;6:7443. doi: 10.1038/ncomms8443. Nat Commun. 2015. PMID: 26068133 Free PMC article.
The benzenesulfoamide T0901317 [N-(2,2,2-trifluoroethyl)-N-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-benzenesulfonamide] is a novel retinoic acid receptor-related orphan receptor-alpha/gamma inverse agonist.
Kumar N, Solt LA, Conkright JJ, Wang Y, Istrate MA, Busby SA, Garcia-Ordonez RD, Burris TP, Griffin PR. Kumar N, et al. Mol Pharmacol. 2010 Feb;77(2):228-36. doi: 10.1124/mol.109.060905. Epub 2009 Nov 3. Mol Pharmacol. 2010. PMID: 19887649 Free PMC article.
DNA binding alters coactivator interaction surfaces of the intact VDR-RXR complex.
Zhang J, Chalmers MJ, Stayrook KR, Burris LL, Wang Y, Busby SA, Pascal BD, Garcia-Ordonez RD, Bruning JB, Istrate MA, Kojetin DJ, Dodge JA, Burris TP, Griffin PR. Zhang J, et al. Nat Struct Mol Biol. 2011 May;18(5):556-63. doi: 10.1038/nsmb.2046. Epub 2011 Apr 10. Nat Struct Mol Biol. 2011. PMID: 21478866 Free PMC article.
Small molecule amides as potent ROR-γ selective modulators.
Khan PM, El-Gendy Bel-D, Kumar N, Garcia-Ordonez R, Lin L, Ruiz CH, Cameron MD, Griffin PR, Kamenecka TM. Khan PM, et al. Bioorg Med Chem Lett. 2013 Jan 15;23(2):532-6. doi: 10.1016/j.bmcl.2012.11.025. Epub 2012 Nov 22. Bioorg Med Chem Lett. 2013. PMID: 23232056 Free PMC article.
Antiobesity Effect of a Small Molecule Repressor of RORγ.
Chang MR, He Y, Khan TM, Kuruvilla DS, Garcia-Ordonez R, Corzo CA, Unger TJ, White DW, Khan S, Lin L, Cameron MD, Kamenecka TM, Griffin PR. Chang MR, et al. Mol Pharmacol. 2015 Jul;88(1):48-56. doi: 10.1124/mol.114.097485. Epub 2015 Apr 22. Mol Pharmacol. 2015. PMID: 25904554 Free PMC article.
Design, Synthesis, and Biological Evaluation of Indole Biphenylcarboxylic Acids as PPARγ Antagonists.
Asteian A, Blayo AL, He Y, Koenig M, Shin Y, Kuruvilla DS, Corzo CA, Cameron MD, Lin L, Ruiz C, Khan S, Kumar N, Busby S, Marciano DP, Garcia-Ordonez RD, Griffin PR, Kamenecka TM. Asteian A, et al. ACS Med Chem Lett. 2015 Aug 4;6(9):998-1003. doi: 10.1021/acsmedchemlett.5b00218. eCollection 2015 Sep 10. ACS Med Chem Lett. 2015. PMID: 26396687 Free PMC article.
28 results