Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885.

doi:10.1158/0008-5472.CAN-06-2554

Loading publication...

Noodle always counts identifier-free feature events for service operation. With your permission, Google Analytics can also estimate audience and engagement. Search text, publication identifiers, cookies, IP addresses and browser fingerprints are never included in Noodle's first-party event counters.

Privacy details

Community

Back to search

Article

Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885.

Cancer research - 1 Dec 2006

King Alastair J, Patrick Denis R, Batorsky Roberta S, Ho Maureen L, Do Hieu T, Zhang Shu Yun, Kumar Rakesh, Rusnak David W, Takle Andrew K, Wilson David M, Hugger Erin, Wang Lifu, Karreth Florian, Lougheed Julie C, Lee Jae, Chau David, Stout Thomas J, May Earl W, Rominger Cynthia M, Schaber Michael D, Luo Lusong, Lakdawala Ami S, Adams Jerry L, Contractor Rooja G, Smalley Keiran S M, Herlyn Meenhard, Morrissey Michael M, Tuveson David A, Huang Pearl S

Abstract excerpt

Oncogenic BRAF alleles are both necessary and sufficient for cellular transformation, suggesting that chemical inhibition of the activated mutant protein kinase may reverse the tumor phenotype. Here, we report the characterization of SB-590885, a novel triarylimidazole that selectively inhibits Raf kinases with more potency towards B-Raf than c-Raf. Crystallographic analysis revealed that SB-590885 stabilizes the...

Read the complete abstract on PubMed

Topics

Share this publication in a Topic to start or enrich a Post.

Share to Crystallization

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to Crystallography, X-Ray

Share to Extracellular Signal-Regulated MAP Kinases

Share to HT29 Cells

Share to Imidazoles

Share to Mice, Nude

Share to Molecular Structure

Share to Xenograft Model Antitumor Assays

Source

Open in PubMed

Identifiers

PMID: 17145850
DOI: 10.1158/0008-5472.CAN-06-2554

Genes

BRAF

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

Related research

Semantic proximity does not establish scientific evidence.

Research trail→

Click a neighbor to travelStep 1 · 12 closest

Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885.PMID 17145850Read ↗

Molecular Pathways and Mechanisms of BRAF in Cancer Therapy.Semantic proximity Read ↗

Current Insights of BRAF Inhibitors in Cancer.Semantic proximity Read ↗

Mutant B-Raf Kinase Inhibitors as Anticancer Agents.Semantic proximity Read ↗

B-Raf Inhibition in the Clinic: Present and FutureSemantic proximity Read ↗

Therapeutic strategies for inhibiting oncogenic BRAF signaling.Semantic proximity Read ↗

Targeting oncogenic Raf protein-serine/threonine kinases in human cancers.Semantic proximity Read ↗

The genesis of Zelboraf: targeting mutant B-Raf in melanoma.Semantic proximity Read ↗

Antitumor Properties of RAF709, a Highly Selective and Potent Inhibitor of RAF Kinase Dimers, in Tumors Driven by Mutant RAS or BRAF.Semantic proximity Read ↗

BRAF - a tumour-agnostic drug target with lineage-specific dependencies.Semantic proximity Read ↗

Recent advances in B-RAF inhibitors as anticancer agents.Semantic proximity Read ↗

Raf proteins and cancer: B-Raf is identified as a mutational target.Semantic proximity Read ↗

C-RAF mutations confer resistance to RAF inhibitors.Semantic proximity Read ↗

⌁Select a neighboring publication to make it the new centre.