RAF inhibitor LY3009120 sensitizes RAS or BRAF mutant cancer to CDK4/6 inhibition by abemaciclib via superior inhibition of phospho-RB and suppression of cyclin D1

Molecular Targeted Therapy Approaches for BRAF Wild-Type Melanoma

(2016) Romany A. N. Johnpulle et al.   Current Oncology Reports

Oncogenic BRAF Deletions That Function as Homodimers and Are Sensitive to Inhibition by RAF Dimer Inhibitor LY3009120

(2016) S.-H. Chen et al.   Cancer Discovery

Efficacy and Safety of Abemaciclib, an Inhibitor of CDK4 and CDK6, for Patients with Breast Cancer, Non-Small Cell Lung Cancer, and Other Solid Tumors

(2016) A. Patnaik et al.   Cancer Discovery

Inhibition of RAF Isoforms and Active Dimers by LY3009120 Leads to Anti-tumor Activities in RAS or BRAF Mutant Cancers

(2015) Sheng-Bin Peng et al.   CANCER CELL

Discovery of 1-(3,3-Dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a Pan-RAF Inhibitor with Minimal Paradoxical Activation and Activity against BRAF or RAS Mutant Tumor Cells

(2015) James R. Henry et al.   JOURNAL OF MEDICINAL CHEMISTRY

Co-targeting BRAF and cyclin dependent kinases 4/6 for BRAF mutant cancers

(2015) Vipin Yadav et al.   PHARMACOLOGY & THERAPEUTICS

Targeting CDK4 and CDK6: From Discovery to Therapy

(2015) C. J. Sherr et al.   Cancer Discovery

Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with gemcitabine

(2014) Lawrence M. Gelbert et al.   INVESTIGATIONAL NEW DRUGS

The CDK4/6 Inhibitor LY2835219 Overcomes Vemurafenib Resistance Resulting from MAPK Reactivation and Cyclin D1 Upregulation

(2014) V. Yadav et al.   MOLECULAR CANCER THERAPEUTICS

Drugging the undruggable RAS: Mission Possible?

(2014) Adrienne D. Cox et al.   NATURE REVIEWS DRUG DISCOVERY

BRAF Inhibitors Induce Metastasis in RAS Mutant or Inhibitor-Resistant Melanoma Cells by Reactivating MEK and ERK Signaling

(2014) B. Sanchez-Laorden et al.   Science Signaling

Dual CDK4/CDK6 Inhibition Induces Cell-Cycle Arrest and Senescence in Neuroblastoma

(2013) J. Rader et al.   CLINICAL CANCER RESEARCH

Effects of Raf Dimerization and Its Inhibition on Normal and Disease-Associated Raf Signaling

(2013) Alyson K. Freeman et al.   MOLECULAR CELL

Tumor adaptation and resistance to RAF inhibitors

(2013) Piro Lito et al.   NATURE MEDICINE

Dabrafenib; Preclinical Characterization, Increased Efficacy when Combined with Trametinib, while BRAF/MEK Tool Combination Reduced Skin Lesions

(2013) Alastair J. King et al.   PLoS One

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

(2012) Piro Lito et al.   CANCER CELL

A Landscape of Driver Mutations in Melanoma

(2012) Eran Hodis et al.   CELL

Reactivation of Mitogen-activated Protein Kinase (MAPK) Pathway by FGF Receptor 3 (FGFR3)/Ras Mediates Resistance to Vemurafenib in Human B-RAF V600E Mutant Melanoma

(2012) Vipin Yadav et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Dabrafenib in BRAF-mutated metastatic melanoma: a multicentre, open-label, phase 3 randomised controlled trial

(2012) Axel Hauschild et al.   LANCET

Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR

(2012) Anirudh Prahallad et al.   NATURE

Oncogenic NRAS signaling differentially regulates survival and proliferation in melanoma

(2012) Lawrence N Kwong et al.   NATURE MEDICINE

EGFR-Mediated Reactivation of MAPK Signaling Contributes to Insensitivity of BRAF -Mutant Colorectal Cancers to RAF Inhibition with Vemurafenib

(2012) Ryan B. Corcoran et al.   Cancer Discovery

RAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF(V600E)

(2011) Poulikos I. Poulikakos et al.   NATURE

Improved Survival with Vemurafenib in Melanoma with BRAF V600E Mutation

(2011) Paul B. Chapman et al.   NEW ENGLAND JOURNAL OF MEDICINE

A Synthetic Lethal Interaction between K-Ras Oncogenes and Cdk4 Unveils a Therapeutic Strategy for Non-small Cell Lung Carcinoma

(2010) Marta Puyol et al.   CANCER CELL

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

(2010) H. Yang et al.   CANCER RESEARCH

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

(2010) Sonja J. Heidorn et al.   CELL

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

Inhibition of Mutated, Activated BRAF in Metastatic Melanoma

(2010) Keith T. Flaherty et al.   NEW ENGLAND JOURNAL OF MEDICINE

Somatic p16INK4a loss accelerates melanomagenesis

(2010) K B Monahan et al.   ONCOGENE

Oncogenic Braf Induces Melanocyte Senescence and Melanoma in Mice

(2009) Nathalie Dhomen et al.   CANCER CELL

Melanocytic nevus-like hyperplasia and melanoma in transgenic BRAFV600E mice

(2009) V K Goel et al.   ONCOGENE

Transcriptional regulation of the cyclin D1 gene at a glance

(2008) E. A. Klein et al.   JOURNAL OF CELL SCIENCE