[HTML][HTML] Pathological roles of MAPK signaling pathways in human diseases

EK Kim, EJ Choi - Biochimica et Biophysica Acta (BBA)-Molecular Basis …, 2010 - Elsevier
The mammalian family of mitogen-activated protein kinases (MAPKs) includes extracellular
signal-regulated kinase (ERK), p38, and c-Jun NH2-terminal kinase (JNK), with each MAPK …

Probing the probes: fitness factors for small molecule tools

P Workman, I Collins - Chemistry & biology, 2010 - cell.com
Chemical probes for interrogating biological processes are of considerable current interest.
Cell permeable small molecule tools have a major role in facilitating the functional …

[HTML][HTML] Kinase-dead BRAF and oncogenic RAS cooperate to drive tumor progression through CRAF

SJ Heidorn, C Milagre, S Whittaker, A Nourry… - Cell, 2010 - cell.com
We describe a mechanism of tumorigenesis mediated by kinase-dead BRAF in the presence
of oncogenic RAS. We show that drugs that selectively inhibit BRAF drive RAS-dependent …

A dimerization-dependent mechanism drives RAF catalytic activation

T Rajakulendran, M Sahmi, M Lefrançois, F Sicheri… - Nature, 2009 - nature.com
The ERK (extracellular signal-regulated kinase) pathway is an evolutionarily conserved
signal transduction module that controls cellular growth, differentiation and survival …

RG7204 (PLX4032), a Selective BRAFV600E Inhibitor, Displays Potent Antitumor Activity in Preclinical Melanoma Models

H Yang, B Higgins, K Kolinsky, K Packman, Z Go… - Cancer research, 2010 - AACR
The BRAFV600E mutation is common in several human cancers, especially melanoma.
RG7204 (PLX4032) is a small-molecule inhibitor of BRAFV600E kinase activity that is in …

Antitumor activity of BRAF inhibitor vemurafenib in preclinical models of BRAF-mutant colorectal cancer

H Yang, B Higgins, K Kolinsky, K Packman… - Cancer research, 2012 - AACR
The protein kinase BRAF is a key component of the RAS–RAF signaling pathway which
plays an important role in regulating cell proliferation, differentiation, and survival. Mutations …

Integrative modelling of the influence of MAPK network on cancer cell fate decision

L Grieco, L Calzone, I Bernard-Pierrot… - PLoS computational …, 2013 - journals.plos.org
The Mitogen-Activated Protein Kinase (MAPK) network consists of tightly interconnected
signalling pathways involved in diverse cellular processes, such as cell cycle, survival …

Mechanisms of drug resistance in kinases

R Barouch-Bentov, K Sauer - Expert opinion on investigational …, 2011 - Taylor & Francis
Introduction: Because of their important roles in disease and excellent 'druggability', kinases
have become the second largest drug target family. The great success of the BCR-ABL …

Pathway-based identification of biomarkers for targeted therapeutics: personalized oncology with PI3K pathway inhibitors

JN Andersen, S Sathyanarayanan, A Di Bacco… - Science translational …, 2010 - science.org
Although we have made great progress in understanding the complex genetic alterations
that underlie human cancer, it has proven difficult to identify which molecularly targeted …

Geldanamycin and its anti-cancer activities

Y Fukuyo, CR Hunt, N Horikoshi - Cancer letters, 2010 - Elsevier
Geldanamycin is a benzoquinone ansamycin antibiotic that manifests anti-cancer activity
through the inhibition of HSP90-chaperone function. The HSP90 molecular chaperone is …