Vemurafenib: the first drug approved for BRAF-mutant cancer
G Bollag, J Tsai, J Zhang, C Zhang, P Ibrahim… - Nature reviews Drug …, 2012 - nature.com
The identification of driver oncogenes has provided important targets for drugs that can
change the landscape of cancer therapies. One such example is the BRAF oncogene, which …
change the landscape of cancer therapies. One such example is the BRAF oncogene, which …
A brief history of melanoma: from mummies to mutations
VW Rebecca, VK Sondak, KSM Smalley - Melanoma research, 2012 - journals.lww.com
In recent years, melanoma research has undergone a renaissance. What was once viewed,
at least in the metastatic setting, as an intractable and untreatable disease is now revealing …
at least in the metastatic setting, as an intractable and untreatable disease is now revealing …
High-throughput screening using patient-derived tumor xenografts to predict clinical trial drug response
H Gao, JM Korn, S Ferretti, JE Monahan, Y Wang… - Nature medicine, 2015 - nature.com
Profiling candidate therapeutics with limited cancer models during preclinical development
hinders predictions of clinical efficacy and identifying factors that underlie heterogeneous …
hinders predictions of clinical efficacy and identifying factors that underlie heterogeneous …
The activation of MAPK in melanoma cells resistant to BRAF inhibition promotes PD-L1 expression that is reversible by MEK and PI3K inhibition
X Jiang, J Zhou, A Giobbie-Hurder, J Wargo… - Clinical cancer …, 2013 - AACR
Abstract Purpose: Selective BRAF inhibition (BRAFi) provides a paradigm shift for
melanoma treatment. The duration of benefit is typically limited before resistance develops …
melanoma treatment. The duration of benefit is typically limited before resistance develops …
Combinations of BRAF, MEK, and PI3K/mTOR Inhibitors Overcome Acquired Resistance to the BRAF Inhibitor GSK2118436 Dabrafenib, Mediated by NRAS or MEK …
JG Greger, SD Eastman, V Zhang, MR Bleam… - Molecular cancer …, 2012 - AACR
Recent results from clinical trials with the BRAF inhibitors GSK2118436 (dabrafenib) and
PLX4032 (vemurafenib) have shown encouraging response rates; however, the duration of …
PLX4032 (vemurafenib) have shown encouraging response rates; however, the duration of …
Intra- and Inter-Tumor Heterogeneity of BRAFV600EMutations in Primary and Metastatic Melanoma
M Yancovitz, A Litterman, J Yoon, E Ng, RL Shapiro… - PloS one, 2012 - journals.plos.org
The rationale for using small molecule inhibitors of oncogenic proteins as cancer therapies
depends, at least in part, on the assumption that metastatic tumors are primarily clonal with …
depends, at least in part, on the assumption that metastatic tumors are primarily clonal with …
Paradoxical oncogenesis—the long-term effects of BRAF inhibition in melanoma
GT Gibney, JL Messina, IV Fedorenko… - Nature reviews Clinical …, 2013 - nature.com
The clinical benefits of BRAF inhibition in patients with advanced-stage BRAF-mutant
melanoma are now well established. Although the emergence of cutaneous squamous-cell …
melanoma are now well established. Although the emergence of cutaneous squamous-cell …
NRAS mutant melanoma: biological behavior and future strategies for therapeutic management
IV Fedorenko, GT Gibney, KSM Smalley - Oncogene, 2013 - nature.com
The recent years have seen a significant shift in the expectations for the therapeutic
management of disseminated melanoma. The clinical success of BRAF targeted therapy …
management of disseminated melanoma. The clinical success of BRAF targeted therapy …
Resistance to BRAF inhibitors: unraveling mechanisms and future treatment options
J Villanueva, A Vultur, M Herlyn - Cancer research, 2011 - AACR
The mitogen-activated protein kinase (MAPK) pathway has emerged as a central target for
melanoma therapy due to its persistent activation in the majority of tumors. Several BRAF …
melanoma therapy due to its persistent activation in the majority of tumors. Several BRAF …
Acquired and intrinsic BRAF inhibitor resistance in BRAF V600E mutant melanoma
IV Fedorenko, KHT Paraiso, KSM Smalley - Biochemical pharmacology, 2011 - Elsevier
The discovery of activating BRAF V600E mutations in 50% of all cutaneous melanomas has
revolutionized the understanding of melanoma biology and provided new strategies for the …
revolutionized the understanding of melanoma biology and provided new strategies for the …