Related Experiment Video

Updated: Jun 16, 2026

Identification of Mediators of T-cell Receptor Signaling via the Screening of Chemical Inhibitor Libraries
08:49

Identification of Mediators of T-cell Receptor Signaling via the Screening of Chemical Inhibitor Libraries

Published on: January 22, 2019

Current review of small molecule Ret kinase inhibitors

W J Zuercher1, B J Turunen, K E Lackey

  • 1GlaxoSmithKline, Research Triangle Park, North Carolina 27709, USA.

Mini Reviews in Medicinal Chemistry
|January 29, 2010
PubMed

Insights

Researchers are developing novel small molecule inhibitors targeting Ret kinase, crucial in various cancers. This review summarizes discovery efforts and clinical outcomes of advanced Ret kinase inhibitors.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • Aberrant Ret kinase signaling is a key driver in numerous carcinomas and other disorders.
  • Identifying effective Ret kinase inhibitors is critical for therapeutic intervention.
  • Existing strategies focus on developing targeted therapies against Ret kinase.

Purpose of the Study:

  • To review current strategies for discovering novel small molecule Ret kinase inhibitors.
  • To compile a comprehensive list of known Ret kinase inhibitors.
  • To summarize the clinical progress of advanced Ret kinase inhibitor drug candidates.

Main Methods:

  • Literature review of scientific publications and clinical trial data.
  • Systematic compilation of small molecule Ret kinase inhibitors.
  • Analysis of clinical outcomes for drugs targeting Ret kinase.

Main Results:

  • Detailed overview of diverse approaches in small molecule Ret kinase inhibitor discovery.
  • A curated list of identified Ret kinase inhibitors.
  • Summary of clinical efficacy and safety data for advanced therapeutic agents.

Conclusions:

  • Small molecule inhibitors targeting Ret kinase represent a promising therapeutic avenue for various cancers.
  • Continued research is essential for optimizing inhibitor design and clinical application.
  • Clinical evaluation of advanced Ret kinase inhibitors shows potential for patient benefit.

More Related Videos

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays13:22

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays

Published on: October 23, 2019

Related Concept Videos

Inhibition of Cdk Activity02:34

Inhibition of Cdk Activity

The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
Receptor Tyrosine Kinases01:26

Receptor Tyrosine Kinases

Receptor tyrosine kinases or RTKs are membrane-bound receptors that phosphorylate specific tyrosine on protein substrates. RTKs regulate cellular growth, differentiation, survival, and migration. They contain an extracellular ligand binding domain, a transmembrane domain, and a cytosolic tail with intrinsic kinase activity. Several extracellular signaling molecules activate RTKs in one or more ways and relay the signal downstream. Ligands such as platelet-derived growth factor (PDGF) or...
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against specific...
M-Cdk Drives Transition Into Mitosis02:15

M-Cdk Drives Transition Into Mitosis

Checkpoints throughout the cell cycle serve as safeguards and gatekeepers, allowing the cell cycle to progress in favorable conditions and slow or halt it in problematic ones. This regulation is known as the cell cycle control system.
Cyclin-dependent kinases, or Cdks, work in concert with cyclins to control cell cycle transitions. M-Cdk, a complex of Cdk1 bound to M cyclin, is a well-known example of this coordinated control that drives the transition from the G2 to the M phase.
M cyclin...
Treatment for Pulmonary Arterial Hypertension: Receptor Tyrosine Kinase Inhibitors and Calcium Channel Blockers01:26

Treatment for Pulmonary Arterial Hypertension: Receptor Tyrosine Kinase Inhibitors and Calcium Channel Blockers

Receptor tyrosine kinase inhibitors (TKIs) and calcium channel blockers (CCBs) are two critical categories of drugs employed in the treatment of pulmonary artery hypertension (PAH). PAH is a disease that causes high blood pressure in the pulmonary arteries, resulting in chest pain, fatigue, and shortness of breath.
TKIs, such as imatinib (Gleevec), are particularly effective in tackling the growth and mitogenic factors that become upregulated in PAH patients. These factors contribute to the...