[HTML][HTML] Resistance to BRAF-targeted therapy in melanoma

RJ Sullivan, KT Flaherty - European journal of cancer, 2013 - Elsevier
BRAF mutations are identified in 40–50% of patients with melanoma. Treatment of these
patients with either of two BRAF inhibitors (vemurafenib, dabrafenib) or the MEK inhibitor …

[HTML][HTML] Overcoming resistance to BRAF inhibitors

I Arozarena, C Wellbrock - Annals of translational medicine, 2017 - ncbi.nlm.nih.gov
The discovery of activating mutations in the serine/threonine (S/T) kinase BRAF followed by
a wave of follow-up research manifested that the MAPK-pathway plays a critical role in …

Treatment of BRAF‐mutant melanoma: the role of vemurafenib and other therapies

S Jang, MB Atkins - Clinical Pharmacology & Therapeutics, 2014 - Wiley Online Library
The discovery of activating BRAF mutations in melanomas has led to the investigation of
small molecular inhibitors targeting BRAF mutation and MEK, a downstream protein within …

BRAF inhibitor resistance in melanoma: mechanisms and alternative therapeutic strategies

J Zhong, W Yan, C Wang, W Liu, X Lin, Z Zou… - … Treatment Options in …, 2022 - Springer
Opinion statement Melanoma is caused by a variety of somatic mutations, and among these
mutations, BRAF mutation occurs most frequently and has routinely been evaluated as a …

Combined BRAF and MEK inhibition in melanoma with BRAF V600 mutations

KT Flaherty, JR Infante, A Daud… - … England Journal of …, 2012 - Mass Medical Soc
Background Resistance to therapy with BRAF kinase inhibitors is associated with
reactivation of the mitogen-activated protein kinase (MAPK) pathway. To address this …

Targeting mutant BRAF in melanoma: current status and future development of combination therapy strategies

R Kudchadkar, KHT Paraiso, KSM Smalley - The Cancer Journal, 2012 - journals.lww.com
The discovery of activating BRAF mutations in∼ 50% of all melanomas has proved to be a
turning point in the therapeutic management of the disseminated disease. In this …

BRAF inhibitors for the treatment of metastatic melanoma: clinical trials and mechanisms of resistance

AM Alcalá, KT Flaherty - Clinical cancer research, 2012 - AACR
The efficacy of selective BRAF inhibitors has now been established in the 50% of patients
with metastatic melanoma whose tumors harbor activating mutations. However, for the vast …

[HTML][HTML] The mitogen-activated protein kinase pathway in melanoma part I–activation and primary resistance mechanisms to BRAF inhibition

T Amaral, T Sinnberg, F Meier, C Krepler… - European journal of …, 2017 - Elsevier
Mitogen-activated protein kinase (MAPK) pathway has an important role in normal cells and
can be activated under physiological conditions. MAPK pathway activation is a fundamental …

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 …

Integrating BRAF/MEK inhibitors into combination therapy for melanoma

KSM Smalley, KT Flaherty - British journal of cancer, 2009 - nature.com
The discovery of BRAF mutations in melanoma has not yet translated into clinical success,
suggesting that BRAF/MEK inhibitors will need to be combined with other agents. In the …