Article

Identification of selective inhibitors of RET and comparison with current clinical candidates through development and validation of a robust screening cascade

2016-08-23

Abstract excerpt

RET (REarranged during Transfection) is a receptor tyrosine kinase, which plays pivotal roles in regulating cell survival, differentiation, proliferation, migration and chemotaxis. Activation of RET is a mechanism of oncogenesis in medullary thyroid carcinomas where both germline and sporadic activating somatic mutations are prevalent. At present, there are no known specific RET inhibitors in clinical development,...

Topics

Open a Topic to create a Post that cites this publication.

Identifiers and source

Literature Corpus work: 800c8dc4-095a-5556-a869-83f8128f342c
DOI: 10.12688/f1000research.8724.2

Open publication

Related research

Semantic proximity does not establish scientific evidence.

Click a neighbor to travelStep 1 · 12 closest

Identification of selective inhibitors of RET and comparison with current clinical candidates through development and validation of a robust screening cascadeDOI 10.12688/f1000research.8724.2Read

RET kinase inhibitors: a review of recent patents (2012–2015)Semantic proximity Read

Discovery of wt RET and V804M RET Inhibitors: From Hit to Lead.Semantic proximity Read

Discovery of 4-methyl-N-(4-((4-methylpiperazin- 1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((6-(pyridin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl)-oxy)benzamide as a potent inhibitor of RET and its gatekeeper mutant.Semantic proximity Read

Discovery of 4-chloro-3-(5-(pyridin-3-yl)-1,2,4-oxadiazole-3-yl)benzamides as novel RET kinase inhibitors.Semantic proximity Read

Targeting RET alterations in cancer: Recent progress and future directions.Semantic proximity Read

State-of-the-Art Strategies for Targeting RET -Dependent CancersSemantic proximity Read

Precision Targeted Therapy with BLU-667 for RET-Driven Cancers.Semantic proximity Read

Identification of a novel 5-amino-3-(5-cyclopropylisoxazol-3-yl)-1-isopropyl-1H-pyrazole-4-carboxamide as a specific RET kinase inhibitor.Semantic proximity Read

Discovery of CN-3 as a Next-Generation RET Inhibitor Potently Overcoming Multiple Mutations.Semantic proximity Read

Discovery of N-Trisubstituted Pyrimidine Derivatives as Type I RET and RET Gatekeeper Mutant Inhibitors with a Novel Kinase Binding Pose.Semantic proximity Read

A Pyrazolo[3,4-d]pyrimidin-4-amine Derivative Containing an Isoxazole Moiety Is a Selective and Potent Inhibitor of RET Gatekeeper Mutants.Semantic proximity Read

RET Inhibitors in RET Fusion-Positive Lung Cancers: Past, Present, and Future.Semantic proximity Read