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By Luciano Martini

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In the brain, POMC generates a range of bioactive peptides, including ACTH, b-endorphin, and a-, b-, and g-MSH. b-Lipotropin, a fragment with 91 amino acids, which contains b-MSH (41-58), g-LPH (1-58), and b-endorphin, is secreted in equimolar quantities with ACTH. The endogenous opioid peptides a-, b-, and g-endorphin are derived from POMC and are composed of amino acids 61–76, 61–91, and 61–77 of b-LPH, respectively. The biological effects of POMC-derived peptides are diverse and are largely mediated through melanocortin (MC) receptors (R), five of which have been described.

8, 714, Elsevier. G Proteins p0035 The activity of all transmembrane ACs is stimulated by Gsa combined with GTP. The structure–activity analysis of the AC catalytic core by various methods has identified the site of interaction with GTP–Gsa (Fig. 2) in the cytosolic C2a domain. The binding of GTP–Gsa to C2a is thought to facilitate the association of C1 and C2. The activity of some but not all ACs is inhibited by Gia (Table I), thereby opposing the stimulation by Gsa. In addition to G protein alpha subunits, Gßg subunits have a direct influence on the activity of some ACs.

USA 88, 5428–5432. Miller, W. , and Tyrell, J. B. (1995). The adrenal cortex. In ‘‘Endocrinology and Metabolism’’ (P. Felig, J. D. Baxter, and L. A. ), International Edition, pp. 555–680. McGraw Hill, New York. Smith, A. , and Funder, J. W. (1988). Proopiomelanocortin processing in the pituitary, central nervous system, and peripheral tissues. Endocr. Rev 9, 159–179. , Nicholson, W. , and Orth, D. N. (1978). The nature of the immunoreactive lipotropins in human plasma and tissue extracts. J. Clin.

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