Design, synthesis and crystallization of a novel glucagon analog as a therapeutic agent.

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Li P, Rogers T, Smiley D, DiMarchi RD, Zhang F

Design, synthesis and crystallization of a novel glucagon analog as a therapeutic agent.

Acta Crystallogr Sect F Struct Biol Cryst Commun. 2007 Jul 1;63(Pt 7):599-601. Epub 2007 Jun 15.

PubMed ID

17620721 [ View in PubMed

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Abstract

Glucagon and glucagon-like peptide 1 (GLP-1) are drugs or drug candidates for the treatment of metabolic diseases such as diabetes and obesity. The native hormones have pharmacological deficiencies such as short half-life and poor solubility. A novel glucagon receptor agonist named glucagon-Cex has been designed, synthesized and crystallized. This peptide was highly soluble under physiological conditions and crystallized readily. The crystal diffracted X-rays to 2.2 A resolution and the diffraction was consistent with space group P23, with unit-cell parameters a = b = c = 48.20 A, alpha = beta = gamma = 90.0 degrees. The crystals were suitable for a full structural determination to reveal the conformational differences between glucagon-Cex and the native hormone.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Glucagon	Glucagon receptor	Protein	Humans	Yes	Agonist	Details