Intrinsic and acquired resistance to MEK1/2 inhibitors in cancer

Disruption of CRAF-Mediated MEK Activation Is Required for Effective MEK Inhibition in KRAS Mutant Tumors

(2014) Piro Lito et al.   CANCER CELL

That which does not kill me makes me stronger; combining ERK1/2 pathway inhibitors and BH3 mimetics to kill tumour cells and prevent acquired resistance

(2013) Matthew J Sale et al.   BRITISH JOURNAL OF PHARMACOLOGY

Enhanced Inhibition of ERK Signaling by a Novel Allosteric MEK Inhibitor, CH5126766, That Suppresses Feedback Reactivation of RAF Activity

(2013) Nobuya Ishii et al.   CANCER RESEARCH

Melanoma adapts to RAF/MEK inhibitors through FOXD3-mediated upregulation of ERBB3

(2013) Ethan V. Abel et al.   JOURNAL OF CLINICAL INVESTIGATION

Subtype-Specific MEK-PI3 Kinase Feedback as a Therapeutic Target in Pancreatic Adenocarcinoma

(2013) O. K. Mirzoeva et al.   MOLECULAR CANCER THERAPEUTICS

Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers

(2013) Georgia Hatzivassiliou et al.   NATURE

BCL2A1is a lineage-specific antiapoptotic melanoma oncogene that confers resistance to BRAF inhibition

(2013) Rizwan Haq et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

TORC1 Suppression Predicts Responsiveness to RAF and MEK Inhibition in BRAF-Mutant Melanoma

(2013) R. B. Corcoran et al.   Science Translational Medicine

MAP Kinase Pathway Alterations in BRAF-Mutant Melanoma Patients with Acquired Resistance to Combined RAF/MEK Inhibition

(2013) N. Wagle et al.   Cancer Discovery

Discovery of a Novel ERK Inhibitor with Activity in Models of Acquired Resistance to BRAF and MEK Inhibitors

(2013) E. J. Morris et al.   Cancer Discovery

Relief of Feedback Inhibition of HER3 Transcription by RAF and MEK Inhibitors Attenuates Their Antitumor Effects in BRAF -Mutant Thyroid Carcinomas

(2013) Cristina Montero-Conde et al.   Cancer Discovery

Concurrent MEK2 Mutation and BRAF Amplification Confer Resistance to BRAF and MEK Inhibitors in Melanoma

(2013) Jessie Villanueva et al.   Cell Reports

The BH3 mimetic ABT-263 synergizes with the MEK1/2 inhibitor selumetinib/AZD6244 to promote BIM-dependent tumour cell death and inhibit acquired resistance

(2012) Matthew J. Sale et al.   BIOCHEMICAL JOURNAL

Intrinsic resistance to selumetinib, a selective inhibitor of MEK1/2, by cAMP-dependent protein kinase A activation in human lung and colorectal cancer cells

(2012) T Troiani et al.   BRITISH JOURNAL OF CANCER

Cutaneous manifestations of dabrafenib (GSK2118436): a selective inhibitor of mutant BRAF in patients with metastatic melanoma

(2012) R.M. Anforth et al.   BRITISH JOURNAL OF DERMATOLOGY

Relief of Profound Feedback Inhibition of Mitogenic Signaling by RAF Inhibitors Attenuates Their Activity in BRAFV600E Melanomas

(2012) Piro Lito et al.   CANCER CELL

Synthetic Lethal Interaction of Combined BCL-XL and MEK Inhibition Promotes Tumor Regressions in KRAS Mutant Cancer Models

(2012) Ryan B. Corcoran et al.   CANCER CELL

ERK Inhibition Overcomes Acquired Resistance to MEK Inhibitors

(2012) G. Hatzivassiliou et al.   MOLECULAR CANCER THERAPEUTICS

Progression of RAS-Mutant Leukemia during RAF Inhibitor Treatment

(2012) Margaret K. Callahan et al.   NEW ENGLAND JOURNAL OF MEDICINE

Combined BRAF and MEK Inhibition in Melanoma with BRAF V600 Mutations

(2012) Keith T. Flaherty et al.   NEW ENGLAND JOURNAL OF MEDICINE

RASMutations in Cutaneous Squamous-Cell Carcinomas in Patients Treated with BRAF Inhibitors

(2012) Fei Su et al.   NEW ENGLAND JOURNAL OF MEDICINE

Mechanisms of acquired resistance to ERK1/2 pathway inhibitors

(2012) A S Little et al.   ONCOGENE

Fully Activated MEK1 Exhibits Compromised Affinity for Binding of Allosteric Inhibitors U0126 and PD0325901

(2011) Payal R. Sheth et al.   BIOCHEMISTRY

Identification of the MEK1(F129L) Activating Mutation as a Potential Mechanism of Acquired Resistance to MEK Inhibition in Human Cancers Carrying the B-RafV600E Mutation

(2011) H. Wang et al.   CANCER RESEARCH

STAT3 Mediates Resistance to MEK Inhibitor through MicroRNA miR-17

(2011) B. Dai et al.   CANCER RESEARCH

PTEN Loss Confers BRAF Inhibitor Resistance to Melanoma Cells through the Suppression of BIM Expression

(2011) K. H. T. Paraiso et al.   CANCER RESEARCH

GSK1120212 (JTP-74057) Is an Inhibitor of MEK Activity and Activation with Favorable Pharmacokinetic Properties for Sustained In Vivo Pathway Inhibition

(2011) A. G. Gilmartin et al.   CLINICAL CANCER RESEARCH

Adaptive upregulation of FOXD3 and resistance to PLX4032/4720-induced cell death in mutant B-RAF melanoma cells

(2011) K J Basile et al.   ONCOGENE

Amplification of the Driving Oncogene, KRAS or BRAF, Underpins Acquired Resistance to MEK1/2 Inhibitors in Colorectal Cancer Cells

(2011) A. S. Little et al.   Science Signaling

High level of AKT activity is associated with resistance to MEK inhibitor AZD6244 (ARRY-142886)

(2010) Jieru Meng et al.   CANCER BIOLOGY & THERAPY

Kinase-Dead BRAF and Oncogenic RAS Cooperate to Drive Tumor Progression through CRAF

(2010) Sonja J. Heidorn et al.   CELL

Identification of Predictive Markers of Response to the MEK1/2 Inhibitor Selumetinib (AZD6244) in K-ras-Mutated Colorectal Cancer

(2010) J. J. Tentler et al.   MOLECULAR CANCER THERAPEUTICS

RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF

(2010) Poulikos I. Poulikakos et al.   NATURE

RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth

(2010) Georgia Hatzivassiliou et al.   NATURE

Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma

(2010) Gideon Bollag et al.   NATURE

BRAF Gene Amplification Can Promote Acquired Resistance to MEK Inhibitors in Cancer Cells Harboring the BRAF V600E Mutation

(2010) R. B. Corcoran et al.   Science Signaling

PI3K Pathway Activation Mediates Resistance to MEK Inhibitors in KRAS Mutant Cancers

(2009) S. Wee et al.   CANCER RESEARCH

Intrinsic resistance to the MEK1/2 inhibitor AZD6244 (ARRY-142886) is associated with weak ERK1/2 signalling and/or strong PI3K signalling in colorectal cancer cell lines

(2009) Kathryn Balmanno et al.   INTERNATIONAL JOURNAL OF CANCER

Oncogenic Activating Mutations Are Associated with Local Copy Gain

(2009) B. Modrek et al.   MOLECULAR CANCER RESEARCH

Oncogene Mutations, Copy Number Gains and Mutant Allele Specific Imbalance (MASI) Frequently Occur Together in Tumor Cells

(2009) Junichi Soh et al.   PLoS One

MEK1 mutations confer resistance to MEK and B-RAF inhibition

(2009) C. M. Emery et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

V600EBRAF is associated with disabled feedback inhibition of RAF-MEK signaling and elevated transcriptional output of the pathway

(2009) C. A. Pratilas et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

BRAF V600E Disrupts AZD6244-Induced Abrogation of Negative Feedback Pathways between Extracellular Signal-Regulated Kinase and Raf Proteins

(2008) B. B. Friday et al.   CANCER RESEARCH

Tumour cell survival signalling by the ERK1/2 pathway

(2008) K Balmanno et al.   CELL DEATH AND DIFFERENTIATION

The regulation of extracellular signal-regulated kinase (ERK) in mammalian cells

(2008) Joe W. Ramos   INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY

Increased cyclin D1 expression can mediate BRAF inhibitor resistance in BRAF V600E-mutated melanomas

(2008) K. S.M. Smalley et al.   MOLECULAR CANCER THERAPEUTICS