Allosteric activation of the Follicle-stimulating Hormone (FSH) receptor by selective, nonpeptide agonists

Journal of Biological Chemistry

Volumn 281, Issue 19, 2006, Pages 13226-13233

  Yanofsky, Stephen D ^a,c   Shen, Emily S ^b   Holden, Frank ^a   Whitehorn, Erik ^a   Aguilar, Barbara ^a   Tate, Emily ^a   Holmes, Christopher P ^a   Scheuerman, Randall ^a   MacLean, Derek ^a   Wu, May M ^b   Frail, Donald E ^b   López, Francisco J ^b   Winneker, Richard ^b   Arey, Brian J ^b   Barrett, Ronald W ^a  

^a AFFYMAX RESEARCH INSTITUTE   (United States)

^b PFIZER INC   (United States)

^c NONE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ACTIVATION ANALYSIS; AMINO ACIDS; ENZYMES; HORMONES; OPTIMIZATION; PHYSIOLOGICAL MODELS;

GLYCOPROTEIN HORMONES; GRANULOSA CELLS; HORMONE BINDING; THYROID-STIMULATING HORMONE (TSH) RECEPTOR;

CELLS;

CYCLIC AMP; FOLLITROPIN RECEPTOR BINDING INHIBITOR;

ANIMAL CELL; ARTICLE; BINDING SITE; CONTROLLED STUDY; FERTILIZATION IN VITRO; GENETIC TRANSFECTION; GRANULOSA CELL; HORMONE BINDING; IN VIVO STUDY; NONHUMAN; PRIORITY JOURNAL; PROTEIN ANALYSIS; PROTEIN STRUCTURE;

ALLOSTERIC REGULATION; ANIMALS; CELL LINE; COMBINATORIAL CHEMISTRY TECHNIQUES; CRICETINAE; ESTRADIOL; FEMALE; FOLLICLE STIMULATING HORMONE; GRANULOSA CELLS; HUMANS; MICE; MOLECULAR STRUCTURE; PROGESTERONE; RATS; RECEPTORS, FSH; STRUCTURE-ACTIVITY RELATIONSHIP; THIAZOLIDINEDIONES;

EID: 33744964702     PISSN: 00219258     EISSN: 1083351X     Source Type: Journal    
DOI: 10.1074/jbc.M600601200     Document Type: Article

References (39)

1. Braun, T., Schofield, P.R., and Sprengel, R. (1991) EMBO J. 10, 1885-1890
2. Christophe, S., Robert, P., Maugain, S., Bellet, D., Koman, A., and Bidart, J.-M. (1993) Biochem. Biophys. Res. Commun. 196, 402-408
3. Johnson, G. L., and Dhanasekaran, N. (1989) Endocr. Rev. 10, 317-331
4. Albanese, C., Cristin-Maitre, S., Sluss, P. M. Crowley, W. F., and Jameson, J. L. (1994) Mol. Cell. Endocrinol. 101, 211-219
5. George, S. E., Bungay, P. J., and Naylor, L. H. (1998) Biochem. Pharmacol. 56, 25-30
6. George, S.E., Bungay, P.J., and Naylor, L.H. (1997) J. Neurochem. 69, 1278-1285
7. Aittomaki, K., Lucena, J. L. D., Pakarinen, P., Sistonen, P., Tapanainen, J., Gromoll, J., Kaskikari, R., Sankila, E. M., Lehvaslaiho, H., Engel, A.R., Nieschlag, E., Huhtaniemi, L., and de la Chapelle, A. (1995) Cell 82, 959-968
8. Kumar, T. R., Wang, Y., Lu, N., and Matzuk, M. M. (1997) Nat. Genet. 15, 201-204
9. Dierich, A., Sairam, M. R., Monaco, L., Fimia, G. M., Gansmuller, A., LeMeur, M., and Sassone-Corsi, P. (1998) Proc. Natl. Acad. Sci. U. S. A. 95, 13612-13617
10. Koller, K. J., Whitehorn, E. A., Tate, E., Ries, T., Aguilar, B., Chernov-Rogan, T., Davis, A.M., Dobbs, A., Yen, M., and Barrett, R. W. (1997) Anal. Biochem. 250, 51-60
11. McDonnell, J., Latif, M. L., Rees, E. S., Bevan, N. J., and Hill S. J. (1998) Br. J. Pharmacol. 125, 717-726
12. Arey, B. J., Deecher, D. C., Shen, E. S., Stevis, P. E., Meade, E. H., Jr., Wrobel, J., Frail, D. E., and Lopez, F. J. (2002) Endocrinology 143, 3822-3829
13. Holmes, C. P., Chinn, J. P., Look, G. C., Gordon, E. M., and Gallop, M. A. (1995) J. Org. Chem. 60, 7328-7333
14. Gordon, E. M. (1995) Curr. Opin. Biotechnol. 6, 624-631
15. Gordon, E. M., Barrett, R. W., Dower, W. J., Fodor, S. P., and Gallop, M. A. (1994) J. Med. Chem. 37, 1385-1401
16. Holmes, C. P., and Jones, D. G. (1995) J. Org. Chem. 60, 2318-2319
17. MacLean, D., Holden, F., Davis, A. M., Scheuerman, R. A., Yanofsky, S., Holmes, C. P., Fitch, W. L., Tsutsui, K., Barrett, R. W., and Gallop, M. A. (2004) J. Comb. Chem. 6, 196-206
18. Ni, Z. J., Maclean, D., Holmes, C. P., Murphy, M. M., Ruhland, B., Jacobs, J. W., Gordon, E. M., and Gallop, M. A. (1996) J. Med. Chem. 39, 1601-1608
19. Hsueh, A. J., Bicsak, T. A., Jia, X. C., Dahl, K. D., Fauser, B. C., Galway, A. B., Czekala, N., Pavlou, S. N., Papkoff, H., Keene, J., and Boime, A. (1989) Recent Prog. Horm. Res. 45, 209-277
20. Arey, B. J., Stevis, P. E., Deecher, D. C., Shen, E. S., Frail, D. E., Negro-Vilar, A., and Lopez, F. J. (1997) Mol. Endocrinol. 11, 517-526
21. Grossmann, M., Szkudlinski, M. W., Wong, R., Dias, J. A., Ji, T. H., and Weintraub, B. D. (1997) J. Biol. Chem. 272, 15532-15540
22. Nagayama, Y., Wadsworth, H. L., Chazenbalk, G. D., Russo, D., Seto, P., and Rapoport, B. (1991) Proc. Natl. Acad. Sci. 88, 902-905
23. Nagayama, Y., Russo, D., Chazenbalk, G. D., Wadsworth, H. L., and Rapoport, B. (1990) Biochem. Biophys. Res. Commun. 173, 1150-1156
24. Vassart, G., Parmentier, M., Libert, F., and Dumont, J. E. (1991) Trends Endocrinol. Metab. 2, 151-156
25. Zhang, B., Salituro, G., Szalkowski, D., Li, Z., Zhang, Y., Royo, I., Vilella, D., Diez, M. T., Pelaez, F., Ruby, C., Kendall, R. L., Mao, X., Griffin, P., Calaycay, J., Zierath, J. R., Heck, J. V., Smith, R. G., and Moller, D. E. (1999) Science 284, 974-977
26. Tian, S. S., Lamb, P., King, A. G., Miller, S. G., Kessler, L., Luengo, J. I., Averill, L., Johnson, R. K., Gleason, J. G., Pelus, L. M., Dillon, S. B., and Rosen, J. (1998) Science 281, 257-259
27. Guo, T., Adang, A. E., Dolle, R. E., Dong, G., Fitzpatrick, D., Geng, P., Ho, K. K., Kultgen, S. G., Liu, R., McDonald, E., McGuinness, B. F., Saionz, K. W., Valenzano, K. J., van Straten, N. C., Xie, D., and Webb, M. L. (2004) Bioorg. Med. Chem. Lett. 14, 1713-1716
28. Guo, T., Adang, A. E., Dong, G., Fitzpatrick, D., Geng, P., Ho, K. K., Jibilian, C. H., Kultgen, S. G., Liu, R., McDonald, E., Saionz, K. W., Valenzano, K. J., van Straten, N. C., Xie, D., and Webb, M. L. (2004) Bioorg. Med. Chem. Lett. 14, 1717-1720
29. Sohn, J., Ryu, K., Sievert, G., Jeoung, M., Ji, I., and Ji, T. H. (2002) J. Biol. Chem. 277, 50165-50175
30. Ji, I., and Ji, T. H. (1995) J. Biol. Chem. 270, 15970-15973
31. Ji, I., and Ji, T. H. (1991) Endocrinology 128, 2648-2650
32. May, L. T., and Christopoulos, A. (2003) Curr. Opin. Pharmacol. 3, 551-556
33. Christopoulos, A., and Kenakin, T. (2002) Pharmacol. Rev. 54, 323-374
34. Arey, B. J., Seethala, R., Ma, Z., Fura, A., Morin, J., Swartz, J., Vyas, V., Yang, W., Dickson, J. K., Jr., and Feyen, J. H. (2005) Endocrinology 146, 2015-2022
35. Fan, Q. R., and Hendrickson, W. A. (2005) Nature 433, 269-277
36. Lerner, D. J., Chen, M., Tram, T., and Coughlin, S. R. (1996) J. Biol. Chem. 271, 13943-13947
37. Chappel, S., Buckler, D., Kelton C., and Tayar, N. E. (June 13, 1998) Hum. Reprod. (Oxf.) Suppl. 3, 18-35 and 47-51
38. Stevis, P. E., Deecher, D. C., Lopez, F. J. amd Frail, D. E. (1999) Endocrine 10, 153-160
39. Vassart, G., Pardo, L., and Costagliola, S. (2004) Trends. Biochem. Sci. 29, 119-126