IMR Press / FBL / Volume 7 / Issue 4 / DOI: 10.2741/A778

Frontiers in Bioscience-Landmark (FBL) is published by IMR Press from Volume 26 Issue 5 (2021). Previous articles were published by another publisher on a subscription basis, and they are hosted by IMR Press on as a courtesy and upon agreement with Frontiers in Bioscience.

Autoinhibitory mechanisms in receptor tyrosine kinases
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1 Skirball Institute of Biomolecular Medicine and Department of Pharmacology, New York University School of Medicine, New York, NY 10016, USA
Front. Biosci. (Landmark Ed) 2002, 7(4), 330–340;
Published: 1 February 2002

Receptor tyrosine kinases (RTKs) are single-pass transmembrane receptors that possess intrinsic tyrosine kinase catalytic activity in their cytoplasmic domains. RTKs are critical components in signal transduction pathways involved in cellular proliferation, differentiation, migration, and metabolism. This large protein family includes the receptors for many growth factors and for insulin. Ligand binding to the extracellular portion of these receptors results in receptor dimerization, which facilitates trans-autophosphorylation of specific tyrosine residues in the cytoplasmic portion. The phosphotyrosine residues enhance receptor catalytic activity and/or provide docking sites for downstream signaling proteins. Because of the critical roles played by RTKs in cellular signaling processes, their catalytic activity is normally under tight control by intrinsic regulatory mechanisms as well as by protein tyrosine phosphatases. This review will focus on the autoinhibitory mechanisms that modulate RTK catalytic activity.

Receptor Tyrosine Kinase
Tyrosine Phosphorylation
Signal Transduction
Growth Factor Receptor
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