A ligand divided: antagonist, agonist and analog control.
Biochem J
; 474(18): 3087-3088, 2017 08 30.
Article
em En
| MEDLINE
| ID: mdl-28860336
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 Biochemical Journal, Zur et al. [Biochem. J. (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.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Receptor de Fator Estimulador de Colônias de Macrófagos
/
Ligantes
Limite:
Humans
Idioma:
En
Ano de publicação:
2017
Tipo de documento:
Article