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Optical Control of Insulin Secretion Using an Incretin Switch.

ABSTRACT: Incretin mimetics are set to become a mainstay of type?2 diabetes treatment. By acting on the pancreas and brain, they potentiate insulin secretion and induce weight loss to preserve normoglycemia. Despite this, incretin therapy has been associated with off-target effects, including nausea and gastrointestinal disturbance. A novel photoswitchable incretin mimetic based upon the specific glucagon-like peptide-1 receptor (GLP-1R) agonist liraglutide was designed, synthesized, and tested. This peptidic compound, termed LirAzo, possesses an azobenzene photoresponsive element, affording isomer-biased GLP-1R signaling as a result of differential activation of second messenger pathways in response to light. While the trans isomer primarily engages calcium influx, the cis isomer favors cAMP generation. LirAzo thus allows optical control of insulin secretion and cell survival.

SUBMITTER: Broichhagen J 

PROVIDER: S-EPMC4736448 | biostudies-literature | 2015 Dec

REPOSITORIES: biostudies-literature

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Optical Control of Insulin Secretion Using an Incretin Switch.

Broichhagen Johannes J   Podewin Tom T   Meyer-Berg Helena H   von Ohlen Yorrick Y   Johnston Natalie R NR   Jones Ben J BJ   Bloom Stephen R SR   Rutter Guy A GA   Hoffmann-Röder Anja A   Hodson David J DJ   Trauner Dirk D  

Angewandte Chemie (International ed. in English) 20151102 51

Incretin mimetics are set to become a mainstay of type 2 diabetes treatment. By acting on the pancreas and brain, they potentiate insulin secretion and induce weight loss to preserve normoglycemia. Despite this, incretin therapy has been associated with off-target effects, including nausea and gastrointestinal disturbance. A novel photoswitchable incretin mimetic based upon the specific glucagon-like peptide-1 receptor (GLP-1R) agonist liraglutide was designed, synthesized, and tested. This pept  ...[more]

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