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Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical

Debasmita Saha1, Katie Rose Ryan2, Naga Rajiv Lakkaniga1

  • 1Department of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, Little Rock, Arkansas 72205 United States.

Journal of Medicinal Chemistry
|August 17, 2021
PubMed

Insights

Rearranged during transfection (RET) receptor tyrosine kinase signaling drives cancer growth. New RET-specific inhibitors offer targeted therapies for RET-driven malignancies, improving patient outcomes.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Rearranged during transfection (RET) is a receptor tyrosine kinase vital for tissue development.
  • Aberrant RET signaling, caused by mutations or fusions, drives cancer progression, survival, and metastasis.
  • Targeting RET is a key strategy in treating RET-driven cancers.

Purpose of the Study:

  • To provide an overview of current developments in RET precision medicine.
  • To discuss the clinical applications of RET-targeted therapies.
  • To highlight the incremental improvements in kinase inhibitors for RET-driven malignancies.

Main Methods:

  • Review of current literature on RET signaling and targeted therapies.
  • Analysis of clinical trial data for RET inhibitors.
  • Discussion of recent advancements in drug development for RET-driven cancers.

Main Results:

  • The development of RET-selective inhibitors has significantly advanced cancer treatment.
  • Pralsetinib and selpercatinib, approved in 2020, represent a breakthrough in targeting the RET oncoprotein.
  • These targeted therapies have shown efficacy in treating various RET-driven malignancies.

Conclusions:

  • RET-targeted therapies represent a significant advancement in precision medicine for RET-driven cancers.
  • Ongoing research continues to refine kinase inhibitors for improved efficacy and specificity.
  • The development of targeted therapies underscores the importance of understanding specific oncogenic drivers like RET.

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