The DOI matches its Crossref record.
Discovery of a Small Molecule Insulin Mimetic with Antidiabetic Activity in Mice
Abstract
Insulin elicits a spectrum of biological responses by binding to its cell surface receptor. In a screen for small molecules that activate the human insulin receptor tyrosine kinase, a nonpeptidyl fungal metabolite (L-783,281) was identified that acted as an insulin mimetic in several biochemical and cellular assays. The compound was selective for insulin receptor versus insulin-like growth factor I (IGFI) receptor and other receptor tyrosine kinases. Oral administration of L-783,281 to two mouse models of diabetes resulted in significant lowering in blood glucose levels. These results demonstrate the feasibility of discovering novel insulin receptor activators that may lead to new therapies for diabetes.
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Citations
Cited by
Hunter, T. (2000) · Cell · doi:10.1016/s0092-8674(00)81688-8 · Cited by 2,586
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Strobel, G., & Daisy, B. (2003) · Microbiology and Molecular Biology Reviews · doi:10.1128/mmbr.67.4.491-502.2003 · Cited by 2,359
Hypothalamic insulin signaling is required for inhibition of glucose production
Obici, S., Zhang, B. B., Karkanias, G., & Rossetti, L. (2002) · Nature Medicine · doi:10.1038/nm1202-798 · Cited by 904
Self-citationDistinct and Overlapping Functions of Insulin and IGF-I Receptors
Nakae, J., Kido, Y., & Accili, D. (2001) · Endocrine Reviews · doi:10.1210/edrv.22.6.0452 · Cited by 554
Management of type 2 diabetes: new and future developments in treatment
Tahrani, A. A., Bailey, C. J., Del Prato, S., & Barnett, A. H. (2011) · The Lancet · doi:10.1016/s0140-6736(11)60207-9 · Cited by 533
Metadata
- Authors
- Zhang, B., Salituro, G., Szalkowski, D., Li, Z., Zhang, Y., Royo, I., Vilella, D., Dı́ez, M. T., Pelaez, F., Ruby, C., Kendall, R. L., Mao, X., Griffin, P., Calaycay, J., Zierath, J. R., Heck, J. V., Smith, R. G., & Moller, D. E.
- Venue
- Science
- Published
- 1999-05-07
- Volume
- 284
- Issue
- 5416
- Pages
- 974-977
- ISSN
- 0036-8075 (ISSN-L)
- 1095-9203
- OpenAlex
- W2156604743
- Cited by
- 456
- References
- 0
- FWCI
- 10.66
- Type
- journal article
- Language
- en
- Open access
- closed
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- Zhang, B., Salituro, G., Szalkowski, D., Li, Z., Zhang, Y., Royo, I., Vilella, D., Dı́ez, M. T., Pelaez, F., Ruby, C., Kendall, R. L., Mao, X., Griffin, P., Calaycay, J., Zierath, J. R., Heck, J. V., Smith, R. G., & Moller, D. E. (1999). Discovery of a Small Molecule Insulin Mimetic with Antidiabetic Activity in Mice. Science. https://doi.org/10.1126/science.284.5416.974
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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.
