Mutational analysis of the endothelin type A receptor (ETA): Interactions and model of the selective ETA antagonist BMS-182874 with the putative ETA receptor binding cavity

Biochemistry

Volumn 35, Issue 8, 1996, Pages 2548-2556

  Webb, Maria L ^a   Patel, Pramathesh S ^a   Rose, Patricia M ^a   Liu, Eddie C K ^a   Stein, Philip D ^a   Barrish, Joel ^a   Lach, David A ^a   Stouch, Terry ^a   Fisher, Susan M ^a   Hadjilambris, Ophelia ^a   Lee, Helen ^a   Skwish, Stephen ^a   Dickinson, Kenneth E J ^a   Krystek Jr , Stanley R ^a  

^a BRISTOL MYERS SQUIBB   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 (2 CARBOXYMETHOXY 4 METHOXYPHENYL) 1 (3,4 METHYLENEDIOXYPHENYL) 5 PROPOXY 2 INDANCARBOXYLIC ACID; 5 DIMETHYLAMINO N (3,4 DIMETHYL 5 ISOXAZOLYL) 1 NAPHTHALENESULFONAMIDE; BOSENTAN; CYCLO(DEXTRO TRYPTOPHYL DEXTRO ASPARTYLPROLYL DEXTRO VALYLLEUCYL); ENDOTHELIN 1; ENDOTHELIN 3; ENDOTHELIN A RECEPTOR; ENDOTHELIN RECEPTOR ANTAGONIST;

ARTICLE; BINDING SITE; DRUG RECEPTOR BINDING; HUMAN; PRIORITY JOURNAL; PROTEIN DOMAIN; SITE DIRECTED MUTAGENESIS; STRUCTURE ACTIVITY RELATION;

AMINO ACID SEQUENCE; ANIMALS; BINDING SITES; CELL LINE; DANSYL COMPOUNDS; ENDOTHELINS; HUMANS; HYDROGEN BONDING; MODELS, MOLECULAR; MOLECULAR SEQUENCE DATA; MUTAGENESIS, SITE-DIRECTED; PROTEIN CONFORMATION; RECEPTOR, ENDOTHELIN A; RECEPTORS, ENDOTHELIN;

EID: 0029988633     PISSN: 00062960     EISSN: None     Source Type: Journal    
DOI: 10.1021/bi951836v     Document Type: Article

References (57)

1. Adachi, M., Yang, Y.-Y., Trzeciak, A., Furuichi, Y., & Miyamoto, C. (1992) FEBS Lett. 311, 179-183.
2. Adachi, M., Furuichi, Y., & Miyamoto, C. (1994) Eur. J. Biochem. 220, 37-43.
3. Arai, H., Hori, S., Aramori, I., Ohkubo, H., & Nakanishi, S. (1990) Nature 348, 730-732.
4. Baldwin, J. M. (1993) EMBO J. 12, 1693-1703.
5. Beinborn, M., Lee, Y. M., McBride, E. W., Quinn, S. M., & Kopin, A. S. (1993) Nature 362, 348-350.
6. Berridge, M. J. (1983) Biochem. J. 212, 849-858.
7. Bond, R. A., Leff, P., Johnson, T. D., Milano, C. A., Rockman, H. A., McMinn, T. R., Apparsundaram, S., Hyek, M. F., Kenakin, T. P., Allen, L. F., & Lefkowitz, R. J. (1995) Nature 374, 272-276.
8. Bousso, D., Bdolah, A., & Sokolovsky, M. (1992) Neurosci. Lett. 140, 247-250.
9. Burley, S. K., & Petsko, G. A. (1985) Science 229, 23-28.
10. Clozel, M., Breu, V., Burri, K., Cassal, J.-M., Fischli, W., Gray, G. A., Hirth, G., Loffler, B.-M., Muller, M., Neidhart, W., & Ramuz, H. (1993) Nature 365, 759-761.
11. Clozel, M., Breu, V., Gray, G. A., Kalina, B., Loffler, B.-M., Burri, K., Cassal, J.-M., Hirth, G., Muller, M., Neidhart, W., & Ramuz, H. (1994) J. Pharmacol. Exp. Ther. 270, 228-235.
12. Deng, W. P., & Nickoloff, J. A. (1992) Anal. Biochem. 200, 81-88.
13. Doherty, A. M., Patt, W. C., Edmunds, J. J., Berryman, K. A., Reisdorph, B. R., Plummer, M. S., Shahripour, A., Lee, C., Cheng, X.-M., Walker, D. M., Haleen, S. J., Keiser, J. A., Flynn, M. A., Welch, K. M., Hallak, H., Taylor, D. G., & Reynolds, E. E. (1995) J. Med. Chem. 38, 1259-1263.
14. Elliott, J. D., Lago, A., Cousins, R. D., Goa, A., Leber, J. D., Erhard, K. F., Nambi, P., Elshourbagy, N. A., Kumar, C., Lee, J. A., Bean, J. W., DeBrosse, C. W., Eggleston, D. S., Brooks, D. P., Feuerstein, G., Ruffolo, R. R., Jr., Weinstock, J., Gleason, J. G., Peishoff, C. E., & Ohlstein, E. H. (1994) J. Med. Chem. 37, 1553-1557.
15. Fong, T. M., Huang, R. R. C., & Strader, C. D. (1992) J. Biol. Chem. 267, 25664-25667.
16. Fong, T. M., Cascieri, M. A., Yu, H., Bansal, A., Swain, C., & Strader, C. D. (1993) Nature 362, 350-353.
17. Fujimoto, M., Mihara, S.-I., Nakajima, S., Ueda, M., Nakmura, M., & Sakurai, K.-S. (1992) FEBS Lett. 305, 41-44.
18. Gether, J., Johansen, T. E., Snider, R. M., Lowe, J. A., Nakanishi, S., & Schwartz, T. W. (1993a) Nature 362, 345-348.
19. Gether, J., Yokota, Y., Emonds-Alt, X., Breliere, J.-C., Lowe, J., III, Snider, R. M., Nakanishi, S., & Schwartz, T. W. (1993b) Proc. Natl. Acad. Sci. U.S.A. 90, 6194-6198.
20. Guan, X., Peroutka, S. J., & Kobilka, B. K. (1992) Mol. Pharmacol. 41, 695-698.
21. Hebert, C. A., Chuntharapai, A., Smith, M., Colby, T., Kim, J., & Horuk, R. (1993) J. Biol. Chem. 268, 18549-18553.
22. Henderson, R., Baldwin, J. M., Ceska, T. A., Zemlin, F., Beckmann, E., & Downing, K. H. (1990) J. Mol. Biol. 213, 899-929.
23. Hjorth, S. A., Schambye, H. T., Greenlee, W. J., & Schwartz, T. W. (1994) J. Biol. Chem. 269, 30953-30959.
24. Huggins, J. P., Trumpp-Kallmeyer, S., Hibert, M. F., Hoflack, J. M., Fanger, B. O., & Jones, C. R. (1993) Eur. J. Pharmacol. Mol. Pharmacol. 245, 203-214.
25. Ihara, M., Noguchi, K., Saeki, T., Fukuroda, T., Tsuchida, S., Kimura, S., Takehiro, F., Ishikawa, K., Nishikibe, M., & Yano, M. (1992) Life Sci. 50, 247-255.
26. Ji, H., Leung, M., Zhang, Y., Catt, K. J., & Sandberg, K. (1994) J. Biol. Chem. 269, 16533-16536.
27. Krystek, S. R., Patel, P. S., Rose, P. M., Fisher, S. M., Kienzle, B. K., Lach, D. A., Liu, E. C.-K., Lynch, J. S., Novotny, J., & Webb, M. L. (1994) J. Biol. Chem. 269, 12383-12386.
28. Krystek, S. R., Hunt, J. T., Stein, P. D., & Stouch, T. R. (1995) J. Med. Chem. 38, 659-668.
29. Lee, J. A., Elliott, J. D., Sutiphong, J. A., Friesen, W. J., Ohlstein, E. H., Stadel, J. M., Gleason, J. G., & Peishoff, C. E. (1994a) Proc. Natl. Acad. Sci. U.S.A. 91, 7164-7168.
30. Lee, J. A., Brinkmann, J. A., Longton, E. D., Peishoff, C. E., Amparo Lago, M., Leber, J. D., Cousins, R. D., Gao, A., Stadel, J. M., Kumar, C. S., Ohlstein, E. H., Gleason, J. G., & Elliott, J. D. (1994b) Biochemistry 33, 14543-14549.
31. Mauzy, C., Wu, L. H., Egloff, A. M., Mirzadegan, T., & Chung, F. Z. (1992) J. Cardiovasc. Pharmacol. 12, S5-S7.
32. Mihara, S.-I., Nakajima, S., Matumura, S., Kohnoike, T., & Fujimoto, M. (1994) J. Pharmacol. Exp. Ther. 268, 1122-1128.
33. Ohashi, H., Akiyama, H., Nishikori, K., & Mochizuki, J.-I. (1992) J. Antibiot. 45, 1684-1685.
34. Oksenberg, D., Marsters, S. A., O'Dowd, B. F., Jin, H., Havlik, S., Peroutka, S. J., & Ashkenazi, A. (1992) Nature 360, 161-163.
35. Owicki, J. C., Parce, J. W., Kerso, K. M., Sigal, G. B., Muir, V. C., Venter, J. C., Fraser, C. M., & McConnell, H. M. (1990) Proc. Natl. Acad. Sci. U.S.A. 87, 4007-4011.
36. Perlman, J. H., Thaw, C. M., Laakkonen, L., Bowers, C. Y., Osman, R., & Gershengorn, M. C. (1994a) J. Biol. Chem. 269, 1610-1613.
37. Perlman, J. H., Laakkonen, L., Osman, R., & Gershengorn, M. C. (1994b) J. Biol. Chem. 269, 23383-23386.
38. Ponder, J. W., & Richards, F. M. (1987) J. Mol. Biol. 193, 775-791.
39. Rose, P. M., Krystek, S. R., Jr., Patel, P. S., Lach, D. A., Liu, E. C. K., Lynch, J. S., Lach, D. A., Fisher, S. M., & Webb, M. L. (1995) FEBS Lett. 361, 243-249.
40. Sachais, B. S., Snider, R. M., Lowe, J. A., III, & Krause, J. E. (1993) J. Biol. Chem. 268, 2319-2323.
41. Sakamoto, A., Yanagisawa, M., Sawamura, T., Enoki, T., Ohtani, T., Sakurai, T., Nakao, K., Toyo-oka, T., & Masaki, T. (1993) J. Biol. Chem. 268, 8547-8553.
42. Sakurai, T., Yanagisawa, M., Takuwa, Y., Miyazaki, H., Kimura, S., Goto, K., & Masaki, T. (1990) Nature 348, 732-735.
43. Sakurai, Y., & Goto, K. (1993) Drugs 46, 795-804.
44. Sanger, F., Nicklen, S., & Coulson, A. R. (1977) Proc. Natl. Acad. Sci. U.S.A. 74, 5463-5467.
45. Schertler, G. F. X., Villa, C., & Henderson, R. (1993) Nature 362, 770-772.
46. Sogabe, K., Nirei, H., Shoubo, M., Nomoto, A., Ao, S., Notsu, Y., & Takaharu, O. (1993) J. Pharmacol. Exp. Ther. 264, 1040-1046.
47. Stein, P. D., Hunt, J. T., Floyd, D. M., Moreland, S., Dickenson, K. E. J., Mitchell, C., Liu, E. C.-K., Webb, M. L., Murugesan, N., Dickey, J., McMullen, D., Zhang, R., Lee, V. G., Serafino, R., Delaney, C., Schaeffer, T. R., & Kozlowski, M. (1994) J. Med. Chem. 37, 329-331.
48. Strader, C. D., Sigal, I. S., Register, R. B., Candelore, M. R., Rands, E., & Dixon, R. A. (1987) Proc. Natl. Acad. Sci. U.S.A. 84, 4384-4388.
49. Strader, C. D., Sigal, I. S., Candelore, M. R., Rands, E., Hill, W. S., & Dixon, R. A. (1988) J. Biol. Chem. 263, 10267-10271.
50. Suryanarayana, S., Daunt, D. A., Zastrow, M. V., & Kobilka, B. K. (1991) J. Biol. Chem. 266, 15488-15492.
51. Takuwa, Y. (1993) Endocrine J. 40, 489-506.
52. Tota, M. R., & Strader, C. D. (1990) J. Biol. Chem. 265, 16891-16897.
53. Wadsworth, H. L., Chazenbalk, G. D., Nagayama, Y., Russo, D., & Rapoport, B. (1990) Science 249, 1423-1425.
54. Webb, M. L., Liu, E. C.-K., Monshizadegan, H., Chao, C.-C., Lynch, J., Fisher, S. M., & Rose, P. M. (1993) Mol. Pharmacol 44, 959-965.
55. Webb, M. L., Bird, J. E., Liu, E. C.-K., Rose, P. M., Serafino, R., Stein, P. D., & Moreland, S. (1995) J. Pharmacol Exp. Ther. 272, 1124-1134.
56. Zhu, G., Wu, L.-H., Mauzy, C., Egloff, A. M., Mirzadegan, T., & Chung, F.-Z. (1992) J. Cell. Biochem. 50, 159-164.
57. Zoffmann, S., Gether, U., & Schwartz, T. W. (1993) FEBS Lett. 336, 506-510.