Identification of SR1078, a synthetic agonist for the orphan nuclear receptors RORα and RORγ

ACS Chemical Biology

Volumn 5, Issue 11, 2010, Pages 1029-1034

  Wang, Yongjun ^a   Kumar, Naresh ^a   Nuhant, Philippe ^a   Cameron, Michael D ^a   Istrate, Monica A ^a   Roush, William R ^a   Griffin, Patrick R ^a   Burris, Thomas P ^a  

^a SCRIPPS RESEARCH INSTITUTE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

FIBROBLAST GROWTH FACTOR 21; GLUCOSE 6 PHOSPHATASE; LIGAND; ORPHAN NUCLEAR RECEPTOR; RECEPTOR RELATED ORPHAN RECEPTOR ALPHA; RECEPTOR RELATED ORPHAN RECEPTOR GAMMA; SR 1078; UNCLASSIFIED DRUG;

AGONIST; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; CELL STRAIN HEPG2; CHEMICAL ANALYSIS; CONFORMATIONAL TRANSITION; CONTROLLED STUDY; DOSE RESPONSE; DRUG IDENTIFICATION; DRUG MECHANISM; GENE EXPRESSION; GENE TARGETING; GENETIC TRANSFECTION; HUMAN; HUMAN CELL; IN VIVO STUDY; LIVER; MOLECULAR PROBE; MOUSE; NONHUMAN; PLASMA CONCENTRATION-TIME CURVE; PRIORITY JOURNAL; PROMOTER REGION; STIMULATION; TRANSCRIPTION INITIATION;

ANIMALS; BENZAMIDES; HEK293 CELLS; HUMANS; LIGANDS; MICE; NUCLEAR RECEPTOR SUBFAMILY 1, GROUP F, MEMBER 1; NUCLEAR RECEPTOR SUBFAMILY 1, GROUP F, MEMBER 3;

MUS;

EID: 78649685719     PISSN: 15548929     EISSN: 15548937     Source Type: Journal    
DOI: 10.1021/cb100223d     Document Type: Article

References (23)

1. Jetten, A. M. (2009) Retinoid-related orphan receptors (RORs): critical roles in development, immunity, circadian rhythm, and cellular metabolism Nucl. Recept. Signaling 7 e003
2. Solt, L. A., Griffin, P. R., and Burris, T. P. ((•••• )) Ligand regulation of retinoic acid receptor-related orphan receptors: implications for development of novel therapeutics Curr. Opin. Lipidol. 21, 204-211
3. Kallen, J., Schlaeppi, J. M., Bitsch, F., Delhon, I., and Fournier, B. (2004) Crystal structure of the human ROR alpha ligand binding domain in complex with cholesterol sulfate at 2.2 angstrom J. Biol. Chem. 279, 14033-14038
4. Kallen, J. A., Schlaeppi, J. M., Bitsch, F., Geisse, S., Geiser, M., Delhon, I., and Fournier, B. (2002) X-ray structure of the hROR alpha LBD at 1.63 angstrom: Structural and functional data that cholesterol or a cholesterol derivative is the natural ligand of ROR alpha Structure 10, 1697-1707
5. Wang, Y., Kumar, N., Solt, L. A., Richardson, T. I., Helvering, L. M., Crumbley, C., Garcia-Ordonez, R. A., Stayrook, K. R., Zhang, X., Novick, S., Chalmers, M. J., Griffin, P. R., and Burris, T. P. (2010) Modulation of RORalpha and RORgamma activity by 7-oxygenated sterol ligands J. Biol. Chem. 285, 5013-5025
6. Wang, Y., Kumar, N., Crumbley, C., Griffin, P. R., and Burris, T. P. (2010) A second class of nuclear receptors for oxysterols: Regulation of RORalpha and RORgamma activity by 24S-hydroxycholesterol (cerebrosterol) Biochim. Biophys. Acta 1801, 917-923
7. Jin, L. H., Martynowski, D., Zheng, S. Y., Wada, T., Xie, W., and Li, Y. Structural basis for hydroxycholesterols as natural ligands of orphan nuclear receptor ROR gamma Mol. Endocrinol. 24, 923-929
8. Lau, P., Fitzsimmons, R. L., Raichur, S., Wang, S. C. M., Lechtken, A., and Muscat, G. E. O. (2008) The orphan nuclear receptor, ROR alpha, regulates gene expression that controls lipid metabolism-Staggerer (sg/sg) mice are resistant to diet-induced obesity J. Biol. Chem. 283, 18411-18421
9. Yang, X. X. O., Pappu, B. P., Nurieva, R., Akimzhanov, A., Kang, H. S., Chung, Y., Ma, L., Shah, B., Panopoulos, A. D., Schluns, K. S., Watowich, S. S., Tian, Q., Jetten, A. M., and Dong, C. (2008) T helper 17 lineage differentiation is programmed by orphan nuclear receptors ROR alpha and ROR gamma Immunity 28, 29-39
10. Ivanov, I. I., McKenzie, B. S., Zhou, L., Tadokoro, C. E., Lepelley, A., Lafaille, J. J., Cua, D. J., and Littman, D. R. (2006) The orphan nuclear receptor RORgammat directs the differentiation program of proinflammatory IL-17(+) T helper cells Cell 126, 1121-1133
11. Meyer, T., Kneissel, M., Mariani, J., and Fournier, B. (2000) In vitro and in vivo evidence for orphan nuclear receptor ROR alpha function in bone metabolism Proc. Natl. Acad. Sci. U.S.A. 97, 9197-9202
12. Kumar, N., Solt, L. A., Conkright, J. J., Wang, Y., Istrate, M. A., Busby, S. A., Garcia-Ordonez, R., Burris, T. P., and Griffin, P. R. (2010) The benzenesulfonamide T0901317 is a novel ROR{alpha}/{gamma} inverse agonist Mol. Pharmacol. 77, 228-236
13. Schultz, J. R., Tu, H., Luk, A., Repa, J. J., Medina, J. C., Li, L. P., Schwendner, S., Wang, S., Thoolen, M., Mangelsdorf, D. J., Lustig, K. D., and Shan, B. (2000) Role of LXRs in control of lipogenesis Genes Dev. 14, 2831-2838
14. Houck, K. A., Borchert, K. M., Hepler, C. D., Thomas, J. S., Bramlett, K. S., Michael, L. F., and Burris, T. P. (2004) T0901317 is a dual LXR/FXR agonist Mol. Genet. Metab. 83, 184-187
15. Farah, B. S., Gilbert, E. E., and Sibilia, J. P. (1965) Perhalo ketones.V. Reaction of perhaloacetones with aromatic hydrocarbons J. Org. Chem. 30, 998-1001
16. Wang, Y. J., Solt, L. A., and Burris, T. P. (2010) Regulation of FGF21 expression and secretion by retinoic acid receptor-related orphan receptor alpha J. Biol. Chem. 285, 15668-15673
17. Chopra, A. R., Louet, J. F., Saha, P., An, J., DeMayo, F., Xu, J. M., York, B., Karpen, S., Finegold, M., Moore, D., Chan, L., Newgard, C. B., and OMalley, B. W. (2008) Absence of the SRC-2 coactivator results in a glycogenopathy resembling Von Gierkes disease Science 322, 1395-1399
18. Raghuram, S., Stayrook, K. R., Huang, P., Rogers, P. M., Nosie, A. K., McClure, D. B., Burris, L. L., Khorasanizadeh, S., Burris, T. P., and Rastinejad, F. (2007) Identification of heme as the ligand for the orphan nuclear receptors REV-ERBalpha and REV-ERBbeta Nat. Struct. Mol. Biol. 14, 1207-1213
19. Yin, L., Wu, N., Curtin, J. C., Qatanani, M., Szwergold, N. R., Reid, R. A., Waitt, G. M., Parks, D. J., Pearce, K. H., Wisely, G. B., and Lazar, M. A. (2007) Rev-erb{alpha}, a heme sensor that coordinates metabolic and circadian pathways Science 318, 1786-1789
20. Kumar, N., Solt, L. A., Wang, Y., Rogers, P. M., Bhattacharyya, G., Kamenecka, T. M., Stayrook, K. R., Crumbley, C., Floyd, Z. E., Gimble, J. M., Griffin, P. R., and Burris, T. P. (2010) Regulation of adipogenesis by natural and synthetic REV-ERB ligands Endocrinology 151, 3015-3025
21. Bettoun, D. J., Burris, T. P., Houck, K. A., Buck, D. W., Stayrook, K. R., Khalifa, B., Lu, J. F., Chin, W. W., and Nagpal, S. (2003) Retinoid X receptor is a nonsilent major contributor to vitamin D receptor-mediated transcriptional activation Mol. Endocrinol. 17, 2320-2328
22. Houck, K. A., Borchert, K. M., Hepler, C. D., Thomas, J. S., Bramlett, K. S., Michael, L. F., and Burris, T. P. (2004) T0901317 is a dual LXR/FXR agonist Mol. Genet. Metab. 83, 184-187
23. Bramlett, K. S., Houck, K. A., Borchert, K. M., Dowless, M. S., Kulanthaivel, P., Zhang, Y., Beyer, T. P., Schmidt, R., Thomas, J. S., Michael, L. F., Barr, R., Montrose, C., Eacho, P. I., Cao, G., and Burris, T. P. (2003) A natural product ligand of the oxysterol receptor, liver X receptor J. Pharmacol. Exp. Ther. 307, 291-296