ARTICLE;
CANCER REGRESSION;
CYTOTOXICITY;
DRUG EFFICACY;
DRUG SCREENING;
GENE MUTATION;
GENETIC HETEROGENEITY;
GENOTYPE;
HIGH THROUGHPUT SCREENING;
HUMAN;
MELANOMA;
NONHUMAN;
SIGNAL TRANSDUCTION;
ANIMAL;
GENETICS;
NOTE;
Exploiting the cancer genome: Strategies for the discovery and clinical development of targeted molecular therapeutics
Yap TA, Workman P. Exploiting the cancer genome: strategies for the discovery and clinical development of targeted molecular therapeutics. Annu Rev Pharmacol Toxicol 2012;52:549-573.
Genotype-selective combination therapies for melanoma identifi ed by high-throughput drug screening
Held MA, Langdon CG, Platt JT, Graham-Steed T, Liu Z, Chakraborty A, et al. Genotype-selective combination therapies for melanoma identifi ed by high-throughput drug screening. Cancer Discov 2013;3:52-67.
Improved survival with vemurafenib in melanoma with BRAF V600E mutation
Chapman PB, Hauschild A, Robert C, Haanen JB, Ascierto P, Larkin J, et al. Improved survival with vemurafenib in melanoma with BRAF V600E mutation. N Engl J Med 2011;364:2507-2516.
Targeting mutant BRAF in melanoma: Current status and future development of combination therapy strategies
Kudchadkar R, Paraiso KH, Smalley KS. Targeting mutant BRAF in melanoma: current status and future development of combination therapy strategies. Cancer J 2012;18:124-131.
The RAF inhibitor PLX4032 inhibits ERK signaling and tumor cell proliferation in a V600E BRAF-selective manner
Joseph EW, Pratilas CA, Poulikakos PI, Tadi M, Wang W, Taylor BS, et al. The RAF inhibitor PLX4032 inhibits ERK signaling and tumor cell proliferation in a V600E BRAF-selective manner. Proc Natl Acad Sci U S A. 2010;107:14903-14908.
Kinase-dead BRAF and oncogenic RAS cooperate to drive tumor progression through CRAF
Heidorn SJ, Milagre C, Whittaker S, Nourry A, Niculescu-Duvas I, Dhomen N. Kinase-dead BRAF and oncogenic RAS cooperate to drive tumor progression through CRAF. Cell 2010;151:209-221.
Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR
Prahallad A, Sun C, Huang S, Di Nicolantonio F, Salazar R, Zecchin D, Beijersbergen RL, Bardelli A, Bernards R. Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR. Nature 2012;483:100-103.
Synthetic lethal screening with small-molecule inhibitors provides a pathway to rational combination therapies for melanoma
Roller DG, Axelrod M, Capaldo BJ, Jensen K, Mackay A, Weber M Y, et al. Synthetic lethal screening with small-molecule inhibitors provides a pathway to rational combination therapies for melanoma. Mol Cancer Ther 2012;11:2505-2515.
Analysis: Objective assessment of cancer genes for drug discovery
Patel MN, Halling-Brown MD, Tym JE, Workman P, Al-Lazikani A. Analysis: Objective assessment of cancer genes for drug discovery. Nat Rev Drug Discov 2013;12:35-50.