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Open Access Green as soon as Postprint is submitted to ZB.
Controlled intramolecular antagonism as a regulator of insulin receptor maximal activity.
Peptides 100, 18-23 (2018)
In the treatment of insulin-dependent diabetes the risk of a fatal insulin overdose is a persistent fear to most patients. In order to potentially reduce the risk of overdose, we report the design, synthesis, and biochemical characterization of a set of insulin analogs designed to be fractionally reduced in maximal agonism at the insulin receptor isoforms. These analogs consist of native insulin that is site-specifically conjugated to a peptide-based insulin receptor antagonist. The structural refinement of the antagonist once conjugated to insulin provided a set of partial agonists exhibiting between 25 and 70% of the maximal agonism of native insulin at the two insulin receptor isoforms, with only slight differences in inherent potency. These rationally-designed partial agonists provide an approach to interrogate whether control of maximal activity can provide glycemic control with reduced hypoglycemic risk.
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Publication type
Article: Journal article
Document type
Scientific Article
Keywords
Antagonism ; Controlled Intramolecular ; Regulator Of Insulin Receptor Maximal Activity
ISSN (print) / ISBN
0196-9781
e-ISSN
1873-5169
Journal
Peptides
Quellenangaben
Volume: 100,
Pages: 18-23
Publisher
Elsevier
Publishing Place
New York, NY
Non-patent literature
Publications
Reviewing status
Peer reviewed
Institute(s)
Institute of Diabetes and Obesity (IDO)