The DOI matches its Crossref record; 1 of the 1 references it cites were found in a registry or an index.
Synthetic Competitive Antagonists of Corticotropin-Releasing Factor: Effect on ACTH Secretion in the Rat
Abstract
Polypeptide analogs of the known members of the corticotropin-releasing factor (CRF) family were synthesized and tested in vitro and in vivo for enhanced potency or competitive antagonism. Predictive methods and physicochemical measurements had suggested an internal secondary α-helical conformation spanning about 25 residues for at least three members of the CRF family. Maximization of α-helix-forming potential by amino acid substitutions from the native known sequences (rat/human and ovine CRF, sauvagine, and carp and sucker urotensin 1) led to the synthesis of an analog that was found to be more than twice as potent as either of the parent peptides in vitro. In contrast, certain amino-terminally shortened fragments, such as α-helical CRF or ovine CRF residues 8 to 41, 9 to 41, and 10 to 41, were found to be competitive inhibitors in vitro. Selected antagonists were examined and also found to be active in vivo.
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Citations
Cites
Swanson, L. W., Sawchenko, P. E., Rivier, J., & Vale, W. W. (2008) · Neuroendocrinology · doi:10.1159/000123454 · Cited by 1,953
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Cited by
Dunn, A. J., & Berridge, C. W. (1990) · Brain Research Reviews · doi:10.1016/0165-0173(90)90012-d · Cited by 1,352
Holsboer, F. (1999) · Journal of Psychiatric Research · doi:10.1016/s0022-3956(98)90056-5 · Cited by 654
Rivier, C., Rivier, J., & Vale, W. (1986) · Science · doi:10.1126/science.3003907 · Cited by 531
Self-citationRassnick, S., Heinrichs, S. C., Britton, K. T., & Koob, G. F. (1993) · Brain Research · doi:10.1016/0006-8993(93)91352-s · Cited by 407
Hauger, R. L., Grigoriadis, D. E., Dallman, M. F., Plotsky, P. M., Vale, W. W., & Dautzenberg, F. M. (2003) · Pharmacological Reviews · doi:10.1124/pr.55.1.3 · Cited by 365
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Metadata
- Authors
- Rivier, J., Rivier, C., & Vale, W.
- Venue
- Science
- Published
- 1984-05-25
- Volume
- 224
- Issue
- 4651
- Pages
- 889-891
- ISSN
- 0036-8075 (ISSN-L)
- 1095-9203
- OpenAlex
- W2032725109
- Cited by
- 472
- References
- 1
- FWCI
- 5.32
- Type
- journal article
- Language
- en
- Open access
- closed
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- Rivier, J., Rivier, C., & Vale, W. (1984). Synthetic Competitive Antagonists of Corticotropin-Releasing Factor: Effect on ACTH Secretion in the Rat. Science. https://doi.org/10.1126/science.6326264
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