Identification of farnesoid X receptor modulators by a fluorescence polarization-based interaction assay

Analytical Biochemistry

Volumn 398, Issue 2, 2010, Pages 185-190

  Han, Ki Cheol ^a,b   Kim, Jung Hwan ^a   Kim, Kook Han ^a   Kim, Eunice EunKyeong ^a   Seo, Jin Ho ^b   Yang, Eun Gyeong ^a  

^a Korea Institute of Science and Technology   (South Korea)

^b Seoul National University   (South Korea)

Author keywords

Agonist; Antagonist; Chenodeoxycholic acid; Farnesoid X receptor; Fluorescence polarization; Reporter assay

Indexed keywords

AMINO ACIDS; POLARIZATION;

AGONIST; ANTAGONIST; CHENODEOXYCHOLIC ACID; FARNESOID X RECEPTORS; FLUORESCENCE POLARIZATION; REPORTER ASSAY;

FLUORESCENCE;

BILE SALT; CHENODEOXYCHOLIC ACID; FARNESOID X RECEPTOR; PROTEIN INHIBITOR; TRYPTOPHAN;

ARTICLE; BINDING ASSAY; CHEMICAL ANALYSIS; CHEMICAL LABELING; CONTROLLED STUDY; FLUORESCENCE; FLUORESCENCE POLARIZATION; HUMAN; LIGAND BINDING; PRIORITY JOURNAL; RECEPTOR BINDING; TRANSACTIVATION;

EID: 77649192410     PISSN: 00032697     EISSN: 10960309     Source Type: Journal    
DOI: 10.1016/j.ab.2009.11.008     Document Type: Article

References (22)

1. Makishima M., Okamoto A.Y., Repa J.J., Tu H., Learned R.M., Luk A., Hull M.V., Lustig K.D., Mangelsdorf D.J., Shan B. Identification of a nuclear receptor for bile acids. Science 1999, 284:1362-1365.
2. Parks D.J., Blanchard S.G., Bledsoe R.K., Chandra G., Consler T.G., Kliewer S.A., Stimmel J.B., Willson T.M., Zavacki A.M., Moore D.D., Lehmann J.M. Bile acids: Natural ligands for an orphan nuclear receptor. Science 1999, 284:1365-1368.
3. Laffitte B.A., Kast H.R., Nguyen C.M., Zavacki A.M., Moore D.D., Edwards P.A. Identification of the DNA binding specificity and potential target genes for the farnesoid X-activated receptor. J. Biol. Chem. 2000, 275:10638-10647.
4. Goodwin B., Gauthier K.C., Umetani M., Watson M.A., Lochansky M.I., Collins J.L., Leitersdorf E., Mangelsdorf D.J., Kliewer S.A., Repa J.J. Identification of bile acid precursors as endogenous ligands for the nuclear xenobiotic pregnane X receptor. Proc. Natl. Acad. Sci. USA 2003, 100:223-228.
5. Malerød L., Sporstøl M., Juvet L.K., Mousavi S.A., Gjøen T., Berg T., Roos N., Eskild W. Bile acids reduce SR-BI expression in hepatocytes by a pathway involving FXR/RXR, SHP, and LRH-1. Biochem. Biophys. Res. Commun. 2005, 336:1096-1105.
6. Grober J., Zaghini I., Fujii H., Jonesi S.A., Klieweri S.A., Willson T.M., Ono T., Besnard P. Identification of a bile acid-responsive element in the human ileal bile acid-binding protein gene. J. Biol. Chem. 1999, 274:29749-29754.
7. Urizar N.L., Dowhan D.H., Moore D.D. The farnesoid X-activated receptor mediates bile acid activation of phospholipid transfer protein gene expression. J. Biol. Chem. 2000, 275:39313-39317.
8. Ananthanarayanan M., Balasubramanian N., Makishima M., Mangelsdorf D.J., Suchy F.J. Human bile salt export pump promoter is transactivated by the farnesoid X receptor/bile acid receptor. J. Biol. Chem. 2001, 276:28857-28865.
9. Berger J., Bailey P., Biswas C., Cullinan C.A., Doebber T.W., Hayes N.S., Saperstein R., Smith R.G., Leibowitz M.D. Thiazolidinediones produce a conformational change in peroxisomal proliferator-activated receptor-gamma: Binding and activation correlate with antidiabetic actions in db/db mice. Endocrinology 1996, 137:4189-4195.
10. Willson T.M., Cobb J.E., Cowan D.J., Wiethe R.W., Correa I.D., Prakash S.R., Beck K.D., Moore L.B., Kliewer S.A., Lehmann J.M. The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones. J. Med. Chem. 1996, 39:665-668.
11. Krey G., Braissant O., L'Horset F., Kalkhoven E., Perroud M., Parker M.G., Wahli W. Fatty acids, eicosanoids, and hypolipidemic agents identified as ligands of peroxisome proliferator-activated receptors by coactivator-dependent receptor ligand assay. Mol. Endocrinol. 1997, 11:779-791.
12. Wang H., Chen J., Hollister K., Sowers L.C., Forman B.M. Endogenous bile acids are ligands for the nuclear receptor FXR/BAR. Mol. Cell 1999, 3:543-553.
13. Bramlett K.S., Yao S., Burris T.P. Correlation of farnesoid X receptor coactivator recruitment and cholesterol 7α-hydroxylase gene expression by bile acids. Mol. Genet. Metab. 2000, 71:609-615.
14. Fujino T., Sato Y., Une M., Kanayasu-Toyoda T., Yamaguchi T., Shudo K., Inoue K., Nishimaki-Mogami T. In vitro farnesoid X receptor ligand sensor assay using surface plasmon resonance and based on ligand-induced coactivator association. J. Steroid Biochem. Mol. Biol. 2003, 87:247-252.
15. Drake K.A., Zhang J.H., Harrison R.K., McGeehan G.M. Development of a homogeneous, fluorescence resonance energy transfer-based in vitro recruitment assay for peroxisome proliferator-activated receptor delta via selection of active LXXLL coactivator peptides. Anal. Biochem. 2002, 304:63-69.
16. Ou J., Tu H., Shan B., Luk A., DeBose-Boyd R.A., Bashmakov Y., Goldstein J.L., Brown M.S. Unsaturated fatty acids inhibit transcription of the sterol regulatory element-binding protein-1c (SREBP-1c) gene by antagonizing ligand-dependent activation of the LXR. Proc. Natl. Acad. Sci. USA 2001, 98:6027-6032.
17. Cui J., Huang L., Zhao A., Lew J.L., Yu J., Sahoo S., Meinke P.T., Royo I., Pelaez F., Wright S.D. Guggulsterone is a farnesoid X receptor antagonist in coactivator association assays but acts to enhance transcription of bile salt export pump. J. Biol. Chem. 2003, 278:10214-10220.
18. Kanaya E., Shiraki T., Jingami H. The nuclear bile acid receptor FXR is activated by PGC-1α in a ligand-dependent manner. Biochem. J. 2004, 382:913-921.
19. Kimbrough R.D. Review of recent evidence of toxic effects of hexachlorophene. Pediatrics 1973, 51:391-394.
20. De Jesus P.V., Pleasure D.E. Hexachlorophene neuropathy. Arch. Neurol. 1973, 29:180-182.
21. Mavier P., Stengel D., Hanoune J. Inhibition of adenylate cyclase and ATPase activities from rat liver plasma membrane by hexachlorophene. Biochem. Pharmacol. 1976, 25:305-359.
22. Matsumura H., Matsuoka M., Igisu H., Ikeda M. Cooperative inhibition of acetylcholinesterase activities by hexachlorophene in human erythrocytes. Arch. Toxicol. 1997, 71:151-156.