Article
Structural basis for regulation of human calcium-sensing receptor by magnesium ions and an unexpected tryptophan derivative co-agonist.
Science advances - 1 May 2016
Zhang Chen, Zhang Tuo, Zou Juan, Miller Cassandra Lynn, Gorkhali Rakshya, Yang Jeong-Yeh, Schilmiller Anthony, Wang Shuo, Huang Kenneth, Brown Edward M, Moremen Kelley W, Hu Jian, Yang Jenny J
Abstract excerpt
Ca(2+)-sensing receptors (CaSRs) modulate calcium and magnesium homeostasis and many (patho)physiological processes by responding to extracellular stimuli, including divalent cations and amino acids. We report the first crystal structure of the extracellular domain (ECD) of human CaSR bound with Mg(2+) and a tryptophan derivative ligand at 2.1 Å. The structure reveals key determinants for cooperative activation...
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