Ligand bias in receptor tyrosine kinase signaling

Kelly Karl, Michael D. Paul, Elena B. Pasquale, Kalina Hristova

Research output: Contribution to journalArticlepeer-review

Abstract

Ligand bias is the ability of ligands to differentially activate certain receptor signaling responses compared with others. It reflects differences in the responses of a receptor to specific ligands and has implications for the development of highly specific therapeutics. Whereas ligand bias has been studied primarily for G protein–coupled receptors (GPCRs), there are also reports of ligand bias for receptor tyrosine kinases (RTKs). However, the understanding of RTK ligand bias is lagging behind the knowledge of GPCR ligand bias. In this review, we highlight how protocols that were developed to study GPCR signaling can be used to identify and quantify RTK ligand bias. We also introduce an operational model that can provide insights into the biophysical basis of RTK activation and ligand bias. Finally, we discuss possible mechanisms underpinning RTK ligand bias. Thus, this review serves as a primer for researchers interested in investigating ligand bias in RTK signaling.

Original languageEnglish (US)
Pages (from-to)18494-18507
Number of pages14
JournalJournal of Biological Chemistry
Volume295
Issue number52
DOIs
StatePublished - Dec 25 2020

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Cell Biology

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