The DOI matches its Crossref record; 6 of the 6 references it cites were found in a registry or an index.
Potent Derivatives of Glucagon-like Peptide-1 with Pharmacokinetic Properties Suitable for Once Daily Administration
Open accessAbstract
A series of very potent derivatives of the 30-amino acid peptide hormone glucagon-like peptide-1 (GLP-1) is described. The compounds were all derivatized with fatty acids in order to protract their action by facilitating binding to serum albumin. GLP-1 had a potency (EC(50)) of 55 pM for the cloned human GLP-1 receptor. Many of the compounds had similar or even higher potencies, despite quite large substituents. All compounds derivatized with fatty acids equal to or longer than 12 carbon atoms were very protracted compared to GLP-1 and thus seem suitable for once daily administration to type 2 diabetic patients. A structure-activity relationship was obtained. GLP-1 could be derivatized with linear fatty acids up to the length of 16 carbon atoms, sometimes longer, almost anywhere in the C-terminal part without considerable loss of potency. Derivatization with two fatty acid substituents led to a considerable loss of potency. A structure-activity relationship on derivatization of specific amino acids generally was obtained. It was found that the longer the fatty acid, the more potency was lost. Simultaneous modification of the N-terminus (in order to obtain better metabolic stability) interfered with fatty acid derivatization and led to loss of potency.
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Glucagon-like peptide 1 promotes satiety and suppresses energy intake in humans.
Flint, A., Raben, A., Astrup, A., & Holst, J. J. (1998) · Journal of Clinical Investigation · doi:10.1172/jci990 · Cited by 1,402
Kieffer, T. J., McIntosh, C. H., & Pederson, R. A. (1995) · Endocrinology · doi:10.1210/endo.136.8.7628397 · Cited by 1,124
Nauck, M. A., Kleine, N., �rskov, C., Holst, J. J., Willms, B., & Creutzfeldt, W. (1993) · Diabetologia · doi:10.1007/bf00401145 · Cited by 1,092
Truncated GLP-1 (proglucagon 78?107-amide) inhibits gastric and pancreatic functions in man
Wettergren, A., Schjoldager, B., Mortensen, P. E., Myhre, J., Christiansen, J., & Holst, J. J. (1993) · Digestive Diseases and Sciences · doi:10.1007/bf01316798 · Cited by 670
Exaggerated secretion of glucagon-like peptide-1 (GLP-1) could cause reactive hypoglycaemia
Toft-Nielsen, M., Madsbad, S., & Holst, J. J. (1998) · Diabetologia · doi:10.1007/s001250051049 · Cited by 132
Cited by
Drucker, D. J., & Nauck, M. A. (2006) · The Lancet · doi:10.1016/s0140-6736(06)69705-5 · Cited by 3,896
The Physiology of Glucagon-like Peptide 1
Holst, J. J. (2007) · Physiological Reviews · doi:10.1152/physrev.00034.2006 · Cited by 3,371
Armstrong, M. J., Gaunt, P., Aithal, G. P., Barton, D., Hull, D., Parker, R., Hazlehurst, J. M., Guo, K., Abouda, G., Aldersley, M. A., et al. (2016) · The Lancet · doi:10.1016/s0140-6736(15)00803-x · Cited by 2,203
GLP-1 receptor agonists for individualized treatment of type 2 diabetes mellitus
Meier, J. J. (2012) · Nature Reviews Endocrinology · doi:10.1038/nrendo.2012.140 · Cited by 1,311
Nauck, M., Frid, A., Hermansen, K., Shah, N. S., Tankova, T., Mitha, I. H., Zdravkovic, M., Düring, M., Matthews, D. R., & for the LEAD-2 Study Group (2009) · Diabetes Care · doi:10.2337/dc08-1355 · Cited by 1,129
Metadata
- Authors
- Knudsen, L. B., Nielsen, P. F., Huusfeldt, P. O., Johansen, N. L., Madsen, K., Pedersen, F. Z., Thøgersen, H., Wilken, M., & Agersø, H.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2000-04-18
- Volume
- 43
- Issue
- 9
- Pages
- 1664-1669
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W1986331352
- Cited by
- 700
- References
- 6
- FWCI
- 6.36
- Type
- journal article
- Language
- en
- Open access
- green
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