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A ligand divided: antagonist, agonist and analog control. | LitMetric

A ligand divided: antagonist, agonist and analog control.

Biochem J

Department of Pharmacology, Yale Cancer Biology Institute, Yale University School of Medicine, West Haven, CT 06516, U.S.A.

Published: August 2017

AI Article Synopsis

Article Abstract

Inhibiting receptor tyrosine kinases has been a cornerstone of cancer therapeutics for decades. Treatment strategies largely involve small-molecule kinase inhibitors and monoclonal antibodies. For receptors activated by constitutively dimeric ligands, another potential mechanism of inhibition exists: developing monomeric ligands that prevent receptor dimerization. In a recent issue of the , Zur et al. [ (2017) 474, 2601-2617] describe the details of creating such an inhibitor directed toward the macrophage colony-stimulating factor receptor, c-FMS. In the process of teasing apart the ligand dimer, they also uncover a potential cryptic regulatory mechanism in this receptor subfamily.

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Source
http://dx.doi.org/10.1042/BCJ20170495DOI Listing

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