Receptor tyrosine kinases and cancer: oncogenic mechanisms and therapeutic approaches

Punit Saraon1, Shivanthy Pathmanathan2,3, Jamie Snider2

  • 1Drug Discovery Program, Ontario Institute for Cancer Research, Toronto, ON, Canada.

Oncogene
|June 3, 2021
PubMed

Insights

Receptor tyrosine kinases (RTKs) drive cancer but treatments face resistance. New technologies aim to discover novel RTK inhibitors targeting both receptors and signaling pathways to overcome treatment challenges.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Receptor tyrosine kinases (RTKs) are crucial in cancer development and are key targets for cancer therapeutics.
  • Despite the success of tyrosine kinase inhibitors (TKIs), acquired resistance and tumor relapse remain significant clinical challenges.

Purpose of the Study:

  • To review the role of RTKs in cancer and the development of TKIs.
  • To highlight the challenge of acquired resistance to current RTK-targeted therapies.
  • To discuss emerging technologies for identifying novel RTK inhibitors.

Main Methods:

  • Review of existing literature on RTKs, TKIs, and cancer resistance mechanisms.
  • Analysis of recent technological advancements in drug discovery for RTK-targeted therapeutics.

Main Results:

  • RTKs are implicated in various cancers, leading to the development of numerous TKIs.
  • Acquired resistance to TKIs is a common cause of treatment failure and tumor relapse.
  • New technologies are emerging for the discovery of diverse RTK inhibitors.

Conclusions:

  • Targeting RTKs remains a critical strategy in cancer therapy.
  • Overcoming acquired resistance requires the development of novel therapeutic approaches.
  • Advancements in technology are paving the way for next-generation RTK inhibitors targeting RTKs and their signaling pathways.

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