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Open Access Green möglich sobald Postprint bei der ZB eingereicht worden ist.
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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Publikationstyp
Artikel: Journalartikel
Dokumenttyp
Wissenschaftlicher Artikel
Schlagwörter
Antagonism ; Controlled Intramolecular ; Regulator Of Insulin Receptor Maximal Activity
Sprache
Veröffentlichungsjahr
2018
HGF-Berichtsjahr
2018
ISSN (print) / ISBN
0196-9781
e-ISSN
1873-5169
Zeitschrift
Peptides
Quellenangaben
Band: 100,
Seiten: 18-23
Verlag
Elsevier
Verlagsort
New York, NY
Begutachtungsstatus
Peer reviewed
Institut(e)
Institute of Diabetes and Obesity (IDO)
POF Topic(s)
30201 - Metabolic Health
Forschungsfeld(er)
Helmholtz Diabetes Center
PSP-Element(e)
G-502200-001
Scopus ID
85041464862
PubMed ID
29412818
Erfassungsdatum
2018-05-18