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Updated: May 5, 2026

Assessment of Resistance to Tyrosine Kinase Inhibitors by an Interrogation of Signal Transduction Pathways by Antibody Arrays
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Assessment of Resistance to Tyrosine Kinase Inhibitors by an Interrogation of Signal Transduction Pathways by Antibody Arrays

Published on: September 19, 2018

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Targeting receptor tyrosine kinase MET in cancer: small molecule inhibitors and clinical progress

J Jean Cui1

  • 1TP Therapeutics, Inc. , 6150 Lusk Boulevard, Suite B100, San Diego, California 92121, United States.

Journal of Medicinal Chemistry
|December 11, 2013
PubMed

Insights

The HGF/MET pathway is vital for normal functions but drives cancer growth and treatment resistance. Inhibiting this pathway, particularly with small molecule MET inhibitors, shows therapeutic promise in clinical studies.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • The hepatocyte growth factor (HGF)/mesenchymal-epithelial transition (MET) signaling pathway regulates crucial physiological processes.
  • Aberrant HGF/MET activation is implicated in various human cancers, contributing to tumor progression and therapeutic resistance.
  • Targeting the HGF/MET pathway presents a significant therapeutic opportunity for cancer treatment.

Purpose of the Study:

  • To provide an overview of the HGF/MET signaling pathway in the context of cancer.
  • To review the development and clinical progress of small molecule MET inhibitors.
  • To discuss the therapeutic potential of HGF/MET pathway inhibition in oncology.

Main Methods:

  • Review of existing literature on the HGF/MET signaling pathway in cancer.
  • Analysis of current clinical studies involving HGF/MET pathway inhibitors.
  • Focus on the development and application of small molecule MET inhibitors.

Main Results:

  • The HGF/MET pathway plays a dual role in normal physiology and cancer development.
  • Aberrant pathway activation occurs through various mechanisms including overexpression and mutation.
  • Preliminary clinical benefits have been observed with HGF or MET inhibition.

Conclusions:

  • Inhibition of the HGF/MET signaling pathway is a promising strategy for cancer therapy.
  • Small molecule MET inhibitors are a key focus in ongoing clinical development.
  • Modulating HGF/MET signaling offers potential to overcome cancer treatment resistance.

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