Open AccessDesign, synthesis and crystallization of a novel glucagon analog as a therapeutic agent
Author(s) -
Li Pengyun,
Rogers Tanya,
Smiley David,
DiMarchi Richard D.,
Zhang Faming
Publication year - 2007
Publication title -
acta crystallographica section f
Language(s) - English
Resource type - Journals
ISSN - 1744-3091
DOI - 10.1107/s1744309107028655
Subject(s) - glucagon , hormone , agonist , crystallization , chemistry , peptide hormone , peptide , receptor , solubility , endocrinology , medicine , biochemistry , organic chemistry
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 Å resolution and the diffraction was consistent with space group P 23, with unit‐cell parameters a = b = c = 48.20 Å, α = β = γ = 90.0°. The crystals were suitable for a full structural determination to reveal the conformational differences between glucagon‐Cex and the native hormone.