The DOI matches its Crossref record; 12 of the 12 references it cites were found in a registry or an index.
Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists
Open accessAbstract
3-(Acylamino)-5-phenyl-2H-1,4-benzodiazepines, antagonists of the peptide hormone cholecystokinin (CCK), are described. Developed by reasoned modification of the known anxiolytic benzodiazepines, these compounds provide highly potent, orally effective ligands selective for peripheral (CCK-A) receptors, with binding affinities approaching or equaling that of the natural ligand CCK-8. The distinction between CCK-A receptors on the one hand and CNS (CCK-B), gastrin, and central benzodiazepine receptors on the other is demonstrated by using the structure-activity profiles of the new compounds. Details of the binding of these agents to CCK-A receptors are examined, and the method of development of these compounds is discussed in terms of its relevance to the general problem of drug discovery.
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Cites
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Design of potent, orally effective, nonpeptidal antagonists of the peptide hormone cholecystokinin.
Evans, B. E., Bock, M. G., Rittle, K. E., DiPardo, R. M., Whitter, W. L., Veber, D. F., Anderson, P. S., & Freidinger, R. M. (1986) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.83.13.4918 · Cited by 327
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Benzodiazepines antagonize cholecystokinin-induced activation of rat hippocampal neurones
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The Schild regression in the process of receptor classification
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Synthesis of cholecystokinin-pancreozymin. I. C-terminal dodecapeptide
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Welsch, M. E., Snyder, S. A., & Stockwell, B. R. (2010) · Current Opinion in Chemical Biology · doi:10.1016/j.cbpa.2010.02.018 · Cited by 1,509
Nicolaou, K. C., Pfefferkorn, J. A., Roecker, A. J., Cao, G.-Q., Barluenga, S., & Mitchell, H. J. (2000) · Journal of the American Chemical Society · doi:10.1021/ja002033k · Cited by 678
Diversity-oriented synthesis: Exploring the intersections between chemistry and biology
Tan, D. S. (2005) · Nature Chemical Biology · doi:10.1038/nchembio0705-74 · Cited by 605
Chemical substructures that enrich for biological activity
Klekota, J., & Roth, F. P. (2008) · Bioinformatics · doi:10.1093/bioinformatics/btn479 · Cited by 392
Orphan G-protein-coupled receptors and natural ligand discovery
Howard, A. D., McAllister, G., Feighner, S. D., Liu, Q., Nargund, R. P., Van der Ploeg, L. H. T., & Patchett, A. A. (2001) · Trends in Pharmacological Sciences · doi:10.1016/s0165-6147(00)01636-9 · Cited by 275
Metadata
- Authors
- Evans, B. E., Rittle, K. E., Bock, M. G., DiPardo, R. M., Freidinger, R. M., Whitter, W. L., Lundell, G. F., Veber, D. F., Anderson, P. S., Chang, R. S. L., Lotti, V. J., Cerino, D. J., Chen, T. B., Kling, P. J., Kunkel, K. A., Springer, J. P., & Hirshfield, J.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 1988-12-01
- Volume
- 31
- Issue
- 12
- Pages
- 2235-2246
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2059664977
- Cited by
- 1,456
- References
- 12
- FWCI
- 5.91
- Type
- journal article
- Language
- en
- Open access
- green
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- Evans, B. E., Rittle, K. E., Bock, M. G., DiPardo, R. M., Freidinger, R. M., Whitter, W. L., Lundell, G. F., Veber, D. F., Anderson, P. S., Chang, R. S. L., Lotti, V. J., Cerino, D. J., Chen, T. B., Kling, P. J., Kunkel, K. A., Springer, J. P., & Hirshfield, J. (1988). Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists. Journal of Medicinal Chemistry. https://doi.org/10.1021/jm00120a002
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Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
