Mechanism-based design of prolactin receptor antagonists.
作者： G. Fuh , P. Colosi , W.I. Wood , J.A. Wells
DOI: 10.1016/S0021-9258(18)53332-9
关键词:
摘要: The mechanism of action two forms the prolactin (PRL) receptor was studied using analogs human growth hormone (hGH). At low concentrations (approximately 1 pM), hGH binds and stimulates proliferation Nb2 cells containing 391-residue PRL as well murine lymphoid FDC-P1 transfected with 591-residue hPRL receptor. However, at high 70 microM) inhibits both these cell lines. Such a "bell-shaped" response curve observed for stimulation (Fuh, G., Cunningham, B.C., Fukunaga, R., Nagata, S., Goeddel, D. V., Wells, J.A. (1992) Science 256, 1677-1680) is consistent sequential formation an active hormone-(receptor)2 complex in which through first site (Site 1) to then second 2) By analogy activation receptor, we find that variants are mutated Site or 2 greatly reduced agonists. Similarly, only mutants potent antagonists either stimulated proliferation. These other data support notion activate by dimerization provide rational basis design
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