Pegvisomant, a growth hormone-specific antagonist, undergoes cellular internalization

Journal of Clinical Endocrinology and Metabolism

Volumn 89, Issue 9, 2004, Pages 4532-4537

  Maamra, M ^a   Kopchick, J J ^a   Strasburger, C J ^b   Ross, R J M ^a,c  

^a OHIO UNIVERSITY   (United States)

^b CHARITÉ UNIVERSITÄTSMEDIZIN BERLIN   (Germany)

^c UNIVERSITY OF SHEFFIELD   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

GROWTH HORMONE; GROWTH HORMONE RECEPTOR; HORMONE RECEPTOR BLOCKING AGENT; MACROGOL; PEGVISOMANT;

ACROMEGALY; AMINO ACID SUBSTITUTION; ARTICLE; CELL TRANSPORT; CIRCULATION; CONFORMATIONAL TRANSITION; DIMERIZATION; DRUG CLEARANCE; DRUG EFFICACY; DRUG METABOLISM; DRUG UPTAKE; HORMONE RECEPTOR INTERACTION; HUMAN; HUMAN CELL; KIDNEY CLEARANCE; PLASMA HALF LIFE; PRIORITY JOURNAL; PROTEIN EXPRESSION; SIGNAL TRANSDUCTION;

EID: 4544273108     PISSN: 0021972X     EISSN: None     Source Type: Journal    
DOI: 10.1210/jc.2003-031781     Document Type: Article

References (21)

1. Trainer PJ, Drake WM, Katznelson L, Freda PU, Herman-Bonert V, van der Lely AJ, Dimaraki EV, Stewart PM, Friend KE, Vance ML, Besser M, Scarlett JAA 2000 Treatment of acromegaly with the growth hormone-receptor antagonist pegvisomant. N Engl J Med 342:1171-1177
2. van der Lely AJ, Hutson RK, Trainer PJ, Besser GM, Barkan AL, Katznelson L, Klibanski A, Herman-Bonert V, Melmed S, Vance ML, Freda PU, Stewart PM, Friend KE, Clemmons DR, Johannsson G, Stavrou S, Cook DM, Phillips LS, Strasburger CJ, Hackett S, Zib KA, Davis RJ, Scarlett JA, Thorner MO 2001 Long-term treatment of acromegaly with pegvisomant, a growth hormone receptor antagonist. Lancet 358:1754-1759
3. Chen WY, Wight DC, Wagner TE, Kopchick JJ 1990 Expression of a mutated bovine growth hormone gene suppresses growth of transgenic mice. Proc Natl Acad Sci USA 87:5061-5065
4. Chen WY, Wight DC, Chen NY, Coleman TA, Wagner TE, Kopchick JJ 1991 Mutations in the third α-helix of bovine growth hormone dramatically affect its intracellular distribution in vitro and growth enhancement in transgenic mice. J Biol Chem 266:2252-2258
5. Chen WY, Wight DC, Mehta BV, Wagner TE, Kopchick JJ 1991 Glycine 119 of bovine growth hormone is critical for growth-promoting activity. Mol Endocrinol 5:1845-1852
6. Gent J, van Kerkhof P, Roza M, Bu G, Strous GJ 2002 Ligand-independent growth hormone receptor dimerization occurs in the endoplasmic reticulum and is required for ubiquitin system-dependent endocytosis. Proc Natl Acad Sci USA 99:9858-9863
7. Ross RJM, Leung KC, Maamra M, Bennett W, Doyle n, Waters MJ, Ho KKY 2001 Binding and functional studies with the growth hormone receptor antagonist, B2036-PEG (pegvisomant), reveal effects of pegylation and evidence that it binds to a receptor dimer. J Clin Endocrinol Metab 86:1716-1723
8. Remy I, Wilson IA, Michnick SW 1999 Erythropoietin receptor activation by a ligand-induced conformation change. Science 283:990-993
9. Livnah O, Stura EA, Middleton SA, Johnson DL, Jolliffe LK, Wilson IA 1999 Crystallographic evidence for preformed dimers of erythropoietin receptor before ligand activation. Science 283:987-990
10. Harding PA, Wang X, Okada S, Chen WY, Wan W, Kopchick JJ 1996 Growth hormone (GH) and a GH antagonist promote GH receptor dimerization and internalization. J Biol Chem 271:6708-6712
11. Johnson V, Maack T 1977 Renal extraction, filtration, absorption, and catabolism of growth hormone. Am J Physiol 233:F185-F196
12. Haffner D, Schaefer F, Girard J, Ritz E, Mehls O 1994 Metabolic clearance of recombinant human growth hormone in health and chronic renal failure. J Clin Invest 93:1163-1171
13. Veldhuis JD, Bidlingmaier M, Anderson SM, Evans WS, Wu Z, Strasburger CJ 2002 Impact of experimental blockade of peripheral growth hormone (GH) receptors on the kinetics of endogenous and exogenous GH removal in healthy women and men. J Clin Endocrinol Metab 87:5737-5745
14. Thorner MO, Strasburger CJ, Wu Z, Straume M, Bidlingmaier M, Pezzoli S, Zib K, Scarlett JC, Bennett WF 1999 Growth hormone (GH) receptor blockade with a PEG-modified GH (B2036-PEG) lowers serum insulin-like growth factor-I but does not acutely stimulate serum GH. J Clin Endocrinol Metab 84:2098-2103
15. Maamra M, Finidori J, Von Laue S, Simon S, Justice S, Webster J, Dower S, Ross R 1999 Studies with a growth hormone antagonist and dual-fluorescent confocal microscopy demonstrate that the full-length human growth hormone receptor, but not the truncated isoform, is very rapidly internalized independent of Jak2-Stat5 signaling. J Biol Chem 274:14791-14798
16. Clark R, Olson K, Fuh G, Marian M, Mortensen D, Teshima G, Chang S, Chu H, Mukku V, Canova-Davis E, Somers T, Cronin M, Winkler M, Wells JA 1996 Long-acting growth hormones produced by conjugation with polyethylene glycol. J Biol Chem 271:21969-21977
17. Baumann G 1991 Growth hormone heterogeneity: genes, isohormones, variants, and binding proteins. Endocr Rev 12:424-449
18. Roupas P, Herington AC 1988 Intracellular processing of growth hormone receptors by adipocytes in primary culture. Mol Cell Endocrinol 57:93-99
19. Allevato G, Billestrup N, Goujon L, Galsgaard ED, Norstedt G, Postel-Vinay MC, Kelly PA, Nielsen JH 1995 Identification of phenylalanine 346 in the rat growth hormone receptor as being critical for ligand-mediated internalization and down-regulation. J Biol Chem 270:17210-17214
20. Hopkins CR, Trowbridge IS 1983 Internalization and processing of transferrin and the transferrin receptor in human carcinoma A431 cells. J Cell Biol 97:508-521
21. Roupas P, Herington AC 1987 Receptor-mediated endocytosis and degradative processing of growth hormone by rat adipocytes in primary culture. Endocrinology 120:2158-2165