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Discovery of Alogliptin: A Potent, Selective, Bioavailable, and Efficacious Inhibitor of Dipeptidyl Peptidase IV
Open accessAbstract
Alogliptin is a potent, selective inhibitor of the serine protease dipeptidyl peptidase IV (DPP-4). Herein, we describe the structure-based design and optimization of alogliptin and related quinazolinone-based DPP-4 inhibitors. Following an oral dose, these noncovalent inhibitors provide sustained reduction of plasma DPP-4 activity and a lowering of blood glucose in animal models of diabetes. Alogliptin is currently undergoing phase III trials in patients with type 2 diabetes.
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Zander, M., Madsbad, S., Madsen, J. L., & Holst, J. J. (2002) · The Lancet · doi:10.1016/s0140-6736(02)07952-7 · Cited by 1,297
Hansotia, T., Baggio, L. L., Delmeire, D., Hinke, S. A., Yamada, Y., Tsukiyama, K., Seino, Y., Holst, J. J., Schuit, F., & Drucker, D. J. (2004) · Diabetes · doi:10.2337/diabetes.53.5.1326 · Cited by 309
Cited by
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Fleming, F. F., Yao, L., Ravikumar, P. C., Funk, L., & Shook, B. C. (2010) · Journal of Medicinal Chemistry · doi:10.1021/jm100762r · Cited by 1,754
Dipeptidyl peptidase 4 inhibitors in the treatment of type 2 diabetes mellitus
Deacon, C. F. (2020) · Nature Reviews Endocrinology · doi:10.1038/s41574-020-0399-8 · Cited by 398
Nabeno, M., Akahoshi, F., Kishida, H., Miyaguchi, I., Tanaka, Y., Ishii, S., & Kadowaki, T. (2013) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2013.03.010 · Cited by 310
Ta, N. N., Schuyler, C. A., Li, Y., Lopes-Virella, M. F., & Huang, Y. (2011) · Journal of Cardiovascular Pharmacology · doi:10.1097/fjc.0b013e31821e5626 · Cited by 156
Metadata
- Authors
- Feng, J., Zhang, Z., Wallace, M. B., Stafford, J. A., Kaldor, S. W., Kassel, D. B., Navre, M., Shi, L., Skene, R. J., Asakawa, T., Takeuchi, K., Xu, R., Webb, D. R., & Gwaltney, S. L.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2007-04-19
- Volume
- 50
- Issue
- 10
- Pages
- 2297-2300
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2064780710
- Cited by
- 405
- References
- 2
- FWCI
- 16.15
- Type
- journal article
- Language
- en
- Open access
- green
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- The paper
- Feng, J., Zhang, Z., Wallace, M. B., Stafford, J. A., Kaldor, S. W., Kassel, D. B., Navre, M., Shi, L., Skene, R. J., Asakawa, T., Takeuchi, K., Xu, R., Webb, D. R., & Gwaltney, S. L. (2007). Discovery of Alogliptin: A Potent, Selective, Bioavailable, and Efficacious Inhibitor of Dipeptidyl Peptidase IV. Journal of Medicinal Chemistry. https://doi.org/10.1021/jm070104l
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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.
