Structural requirements for the activation of the human growth hormone secretagogue receptor by peptide and nonpeptide secretagogues

Molecular Endocrinology

Volumn 12, Issue 1, 1998, Pages 137-145

  Feighner, Scott D ^a   Howard, Andrew D ^a   Prendergast, Kristine ^a   Palyha, Oksana C ^a   Hreniuk, Donna L ^a   Nargund, Ravi ^a   Underwood, Dennis ^a   Tata, James R ^a   Dean, Dennis C ^a   Tan, Carina P ^a   McKee, Karen Kulju ^a   Woods, John W ^a   Patchett, Arthur A ^a   Smith, Roy G ^a   Van Der Ploeg, Lex H T ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

PEPTIDE HORMONE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BINDING SITE; CALCIUM TRANSPORT; CONTROLLED STUDY; DRUG RECEPTOR BINDING; GENE MAPPING; GENETIC COMPLEMENTATION; GROWTH HORMONE RELEASE; HORMONAL REGULATION; HORMONE RELEASE; LIGAND BINDING; MOLECULAR MODEL; NONHUMAN; PEPTIDE SYNTHESIS; PRIORITY JOURNAL; RAT;

AMINO ACID SEQUENCE; ANIMALS; GTP-BINDING PROTEINS; HUMAN GROWTH HORMONE; HUMANS; MOLECULAR SEQUENCE DATA; MUTAGENESIS, SITE-DIRECTED; PEPTIDES; RATS; RECEPTORS, CELL SURFACE; RECEPTORS, G-PROTEIN-COUPLED; SWINE;

ANIMALIA;

EID: 15444361604     PISSN: 08888809     EISSN: None     Source Type: Journal    
DOI: 10.1210/me.12.1.137     Document Type: Article

References (29)

1. Bowers CY, Sartor RA, Reynolds GA 1991 On the actions of the growth hormone-releasing hexapeptide GHRP. Endocrinology 128:2027-2035
2. Smith RA, Cheng K, Schoen WR, Pong S-S, Hickey G, Jacks T, Butler B, Chan WW, Chaung L-YP, Judith F, Taylor J, Wyvratt MJ, Fisher M-H 1993 A nonpeptidyl growth hormone secretagogue. Science 260:1640-1643
3. Patchett AA, Nargund RA, Tata JR, Chen M-M, Barakat KJ, Johnston DBR, Cheng K, Chan WW-S, Butler B, Hickey G, Jacks T, Scheim K, Pong S-S, Chaung L-YP, Chen HY, Frazer E, Leung KH, Chiu S-HL, Smith RG 1995 Design and biological activities of L-163, 191 (MK-0677): a potent and orally active growth hormone secretagogue. Proc Natl Acad Sci USA 92:7001-7005
4. Pong S-S, Chaung L-YP, Dean DC, Nargund RP, Patchett AA, Smith RG 1996 Identification of a new G protein-linked receptor for growth hormone secretagogues. Mol Endocrinol 10:57-61
5. Howard AD, Feighner SD, Cully DF, Arena JP, Liberator PL, Rosenblum CI, Hamelin M, Hreniuk DL, Palyha OC, Anderson J, Paress PS, Diaz C, Chou M, Liu KK, McKee K-K, Pong S-S, Chaung L-Y, Elbrecht A, Dashkevicz M, Heavens R, Rigby M, Sirinathsinghji D, Dean DC, Melillo DG, Patchett AA, Nargund R, Griffin PR, DeMartino JA, Gupta SK, Schaeffer JA, Smith RG, Van der Ploeg LHT 1996 A receptor in pituitary and hypothalamus that functions in growth hormone release. Science 273:974-977
6. McKee K-K, Palyha OC, Feighner SD, Hreniuk DL, Tan C, Phillips M, Smith RG, Van der Ploeg LHT, Howard AD 1997 Molecular analysis of rat pituitary and hypothalamic growth hormone secretagogue receptors. Mol Endocrinol 11:415-423
7. Laron Z 1995 Growth hormone secretagogues: clinical experience and therapeutic potential. Drugs 50:595-601
8. Henderson R, Baldwin J, Ceska T, Zemlin F, Beckmann E, Downing K 1990 Model for the structure of bacteriorhodopsin based on high-resolution electron cryo-microscopy. J Mol Biol 213:899-929
9. Probst WC, Snyder LA, Schuster DI 1992 Sequence alignment of the G-protein coupled receptor superfamily. DNA Cell Biol 11:1-20
10. Schertler G, Villa C, Henderson R 1993 Projection structure of rhodopsin. Nature 362:770-772
11. Pittel Z, Wess J 1994 Intramolecular interactions in muscarinic acetylcholine-receptors studied with chimeric m2/m5 receptors. Mol Pharmacol 45:61-64
12. Fong TM, Yu H, Cascieri MA, Underwood D, Swain CJ, Strader CD 1994 The role of histidine-265 in antagonist binding to the neurokinin-1 receptor. J Biol Chem 269:2728-2732
13. Schoen WR, Pisano JM, Prendergast K, Wyvratt MJ, Fisher MH, Cheng K, Chan WW-S, Butler B, Smith RG, Ball RG 1994 A novel 3-substituted benzazepinone growth hormone secretagogue (L-692, 429). J Med Chem 37:897-906
14. 1 subtype, G protein-coupled receptor. Curr Biol 1:211-221
15. Bednarek MA, Arison B, Baum MW, Cheng K, Butler B, Chan WW-S, Ren EN, Wu T-J, Prendergast K 1996 NMR and Structure-Function Studies on Growth Hormone Releasing Peptides, GHRP-6 and GHRP-2. Springer-Verlag, Edinburgh
16. Momany FA, Bowers CY, Reynolds GA, Hong A, Newlander K 1984 Conformational energy studies and in vitro and in vivo activity data on growth hormone-releasing peptides. Endocrinology 114:1531-1536
17. McDowell RS, Elias KA, Stanley MS, Burdick DJ, Burnier JP, Chan KS, Fairbrother WJ, Hammonds RG, Ingle GS, Jacobsen NE 1995 Growth hormone secretagogues: characterization, efficacy, and minimal bioactive conformation. Proc Natl Acad Sci USA 92:11165-11169
18. Schwartz TW 1994 Locating ligand-binding sites in 7TM receptors by protein engineering. Curr Opin Biotechnol 5:434-444
19. Fong TM 1996 Mechanistic hypotheses for the activation of G protein-coupled receptors. Cell Signal 8:217-224
20. Schwartz TW, Rosenkilde MM 1996 Is there a lock for all agonist keys in 7TM receptors? Trends Pharmacol Sci 17:213-216
21. Strader CD, Candelore MR, Hill WS, Dixon RAF, Sigal IS 1989 A single amino acid subsitution in the beta-adrenergic receptor promotes partial agonist activity from antagonists. J Biol Chem 264:16470-16477
22. Cheng K, Chan WWS, Butler B, Barrato A, Smith RA 1991 Evidence for a role of protein kinase-C in His-D-Trp-Ala-D-Phe-Lys-amide induced growth hormone release from rat primary pituitary cells. Endocrinology 129:3337-3342
23. Bresson-Bepoldun L, Odessa MF, Dufy-Barbe L 1994 GHRP-6 stimulates calcium increase and growth hormone release in human somatotrophs in vitro. Endocr J 2:793-803
24. Lei T, Buchfelder M, Fahlbusch R, Adams EF 1995 Growth hormone releasing peptide (GHRP-6) stimulates phosphatidylinositol (PI) turnover in human pituitary somatotroph cells. J Mol Endocrinol 14:135-138
25. 2+ mobilization. Cell Calcium 14:663-671
26. Hein L, Ishii K, Coughlin SR, Kobilka BK 1994 Intracellular targeting and trafficking of thrombin receptors. J Biol Chem 269:27719-27726
27. Kunkel TA 1985 Rapid and efficient site-specific mutagenesis without phenotypic selection. Proc Natl Acad Sci USA 82:488
28. van Rhee AM, Jacobson KA 1996 Molecular architecture of G protein-coupled receptors. Drug Dev Res 37:1-38
29. Brooks BB, Bruccoleri RE, Olafson BD, States DJ, Swaminathan S, Karplus M 1983 CHARMm: a program for macromolecular energy, minimization, and dynamics calculations. J Comput Chem 4:187-217