(Q38270129)

1 September 2017

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title

The biology and clinical development of MEK inhibitors for cancer (English)

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1 September 2017

Jason J Luke

1

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1 September 2017

Patrick A Ott

series ordinal

2

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1 September 2017

Geoffrey I Shapiro

series ordinal

3

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1 September 2017

publication date

1 December 2014

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1 September 2017

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1 September 2017

volume

74

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1 September 2017

issue

18

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1 September 2017

page(s)

2111-2128

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https://scigraph.springernature.com/pub.10.1007/s40265-014-0315-4

1 September 2017

exact match

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cites work

Mammalian MAP kinase signalling cascades

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Structural evidence for feedback activation by Ras.GTP of the Ras-specific nucleotide exchange factor SOS

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

A Ras-induced conformational switch in the Ras activator Son of sevenless

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

The RalGEF-Ral Effector Signaling Network: The Road Less Traveled for Anti-Ras Drug Discovery

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Ras oncogenes and their downstream targets

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Oligomerization activates c-Raf-1 through a Ras-dependent mechanism

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Critical tyrosine residues regulate the enzymatic and biological activity of Raf-1 kinase

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Suppression of Raf-1 kinase activity and MAP kinase signalling by RKIP

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

COT drives resistance to RAF inhibition through MAP kinase pathway reactivation

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

MEK1 and MEK2 differentially control the duration and amplitude of the ERK cascade response.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

IQGAPs in cancer: a family of scaffold proteins underlying tumorigenesis

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

BRAFV600E mutation is associated with preferential sensitivity to mitogen-activated protein kinase kinase inhibition in thyroid cancer cell lines

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Sprouty proteins: multifaceted negative-feedback regulators of receptor tyrosine kinase signaling.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

The RAS/RAF/MEK/ERK and the PI3K/AKT signalling pathways: role in cancer pathogenesis and implications for therapeutic approaches.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Relief of profound feedback inhibition of mitogenic signaling by RAF inhibitors attenuates their activity in BRAFV600E melanomas

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

A comprehensive survey of Ras mutations in cancer

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Isoform-specific ras functions in development and cancer

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

TP53 and KRAS mutation load and types in lung cancers in relation to tobacco smoke: distinct patterns in never, former, and current smokers

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Mutations of the BRAF gene in human cancer

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Distinct sets of genetic alterations in melanoma

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Clinical characteristics of patients with lung adenocarcinomas harboring BRAF mutations

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Mutation profiling identifies numerous rare drug targets and distinct mutation patterns in different clinical subtypes of breast cancers.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Diverse tumorigenic pathways in ovarian serous carcinoma

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

In ovarian neoplasms, BRAF, but not KRAS, mutations are restricted to low-grade serous tumours

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Association of BRAF V600E mutation with poor clinicopathological outcomes in 500 consecutive cases of papillary thyroid carcinoma.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Role of BRAF in thyroid oncogenesis.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Value of mismatch repair, KRAS, and BRAF mutations in predicting recurrence and benefits from chemotherapy in colorectal cancer.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Mutation analysis of the BRAF, ARAF and RAF-1 genes in human colorectal adenocarcinomas

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Mechanism of activation of the RAF-ERK signaling pathway by oncogenic mutations of B-RAF

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Novel MEK1 mutation identified by mutational analysis of epidermal growth factor receptor signaling pathway genes in lung adenocarcinoma

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Exome sequencing identifies recurrent somatic MAP2K1 and MAP2K2 mutations in melanoma.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Preexisting MEK1 exon 3 mutations in V600E/KBRAF melanomas do not confer resistance to BRAF inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

MEK1 mutations confer resistance to MEK and B-RAF inhibition

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Dissecting therapeutic resistance to RAF inhibition in melanoma by tumor genomic profiling

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

The genetic landscape of clinical resistance to RAF inhibition in metastatic melanoma

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

MAP kinase pathway alterations in BRAF-mutant melanoma patients with acquired resistance to combined RAF/MEK inhibition

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

BRAF mutation predicts sensitivity to MEK inhibition

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Effective use of PI3K and MEK inhibitors to treat mutant Kras G12D and PIK3CA H1047R murine lung cancers

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

GSK1120212 (JTP-74057) is an inhibitor of MEK activity and activation with favorable pharmacokinetic properties for sustained in vivo pathway inhibition

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

BRAF V600E disrupts AZD6244-induced abrogation of negative feedback pathways between extracellular signal-regulated kinase and Raf proteins

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

(V600E)BRAF is associated with disabled feedback inhibition of RAF-MEK signaling and elevated transcriptional output of the pathway

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Targeting RAS signalling pathways in cancer therapy

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

PD 098059 is a specific inhibitor of the activation of mitogen-activated protein kinase kinase in vitro and in vivo

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Discovery of novel allosteric mitogen-activated protein kinase kinase (MEK) 1,2 inhibitors possessing bidentate Ser212 interactions

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Structures of human MAP kinase kinase 1 (MEK1) and MEK2 describe novel noncompetitive kinase inhibition.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Wild-type and mutant B-RAF activate C-RAF through distinct mechanisms involving heterodimerization

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Distinct requirement for an intact dimer interface in wild-type, V600E and kinase-dead B-Raf signalling

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Disruption of CRAF-mediated MEK activation is required for effective MEK inhibition in KRAS mutant tumors

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Phase I and pharmacodynamic study of the oral MEK inhibitor CI-1040 in patients with advanced malignancies

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Phase I pharmacokinetic and pharmacodynamic study of the oral MAPK/ERK kinase inhibitor PD-0325901 in patients with advanced cancers

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Safety, pharmacokinetic, pharmacodynamic, and efficacy data for the oral MEK inhibitor trametinib: a phase 1 dose-escalation trial

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Activity of the oral MEK inhibitor trametinib in patients with advanced melanoma: a phase 1 dose-escalation trial

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Improved survival with MEK inhibition in BRAF-mutated melanoma

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Combined BRAF and MEK inhibition in melanoma with BRAF V600 mutations

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Biological characterization of ARRY-142886 (AZD6244), a potent, highly selective mitogen-activated protein kinase kinase 1/2 inhibitor

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Targeted inhibition of the extracellular signal-regulated kinase kinase pathway with AZD6244 (ARRY-142886) in the treatment of hepatocellular carcinoma.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Phase I pharmacokinetic and pharmacodynamic study of the oral, small-molecule mitogen-activated protein kinase kinase 1/2 inhibitor AZD6244 (ARRY-142886) in patients with advanced cancers

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

The first-in-human study of the hydrogen sulfate (Hyd-sulfate) capsule of the MEK1/2 inhibitor AZD6244 (ARRY-142886): a phase I open-label multicenter trial in patients with advanced cancer

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

A phase I, open-label, randomized crossover study to assess the effect of dosing of the MEK 1/2 inhibitor Selumetinib (AZD6244; ARRY-142866) in the presence and absence of food in patients with advanced solid tumors

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Phase II, open-label, randomized trial of the MEK1/2 inhibitor selumetinib as monotherapy versus temozolomide in patients with advanced melanoma

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

A phase II open-label randomized study to assess the efficacy and safety of selumetinib (AZD6244 [ARRY-142886]) versus capecitabine in patients with advanced or metastatic pancreatic cancer who have failed first-line gemcitabine therapy.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

A phase II, open-label, randomized study to assess the efficacy and safety of AZD6244 (ARRY-142886) versus pemetrexed in patients with non-small cell lung cancer who have failed one or two prior chemotherapeutic regimens

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Multi-institutional phase II study of selumetinib in patients with metastatic biliary cancers

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Phase II study of the mitogen-activated protein kinase 1/2 inhibitor selumetinib in patients with advanced hepatocellular carcinoma

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Selumetinib in women with recurrent low-grade serous carcinoma of the ovary or peritoneum: an open-label, single-arm, phase 2 study

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Selumetinib plus dacarbazine versus placebo plus dacarbazine as first-line treatment for BRAF-mutant metastatic melanoma: a phase 2 double-blind randomised study

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Phase II trial of MEK inhibitor selumetinib (AZD6244, ARRY-142886) in patients with BRAFV600E/K-mutated melanoma.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

DOC-MEK: a double-blind randomized phase II trial of docetaxel with or without selumetinib in wild-type BRAF advanced melanoma.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Therapeutic implications of the emerging molecular biology of uveal melanoma.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Selumetinib plus docetaxel for KRAS-mutant advanced non-small-cell lung cancer: a randomised, multicentre, placebo-controlled, phase 2 study

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Phase II efficacy and pharmacogenomic study of Selumetinib (AZD6244; ARRY-142886) in iodine-131 refractory papillary thyroid carcinoma with or without follicular elements

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Selumetinib-enhanced radioiodine uptake in advanced thyroid cancer

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

In vivo antitumor activity of MEK and phosphatidylinositol 3-kinase inhibitors in basal-like breast cancer models.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Preclinical disposition of GDC-0973 and prospective and retrospective analysis of human dose and efficacy predictions

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Bridging the gap between preclinical and clinical studies using pharmacokinetic-pharmacodynamic modeling: an analysis of GDC-0973, a MEK inhibitor

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Absolute bioavailability and effect of formulation change, food, or elevated pH with rabeprazole on cobimetinib absorption in healthy subjects

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

RDEA119/BAY 869766: a potent, selective, allosteric inhibitor of MEK1/2 for the treatment of cancer

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Antitumour activity of a potent MEK inhibitor RDEA119/BAY 869766 combined with rapamycin in human orthotopic primary pancreatic cancer xenografts

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Multicenter phase I trial of the mitogen-activated protein kinase 1/2 inhibitor BAY 86-9766 in patients with advanced cancer

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

MEK162 for patients with advanced melanoma harbouring NRAS or Val600 BRAF mutations: a non-randomised, open-label phase 2 study

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Blockade of the MEK/ERK signalling cascade by AS703026, a novel selective MEK1/2 inhibitor, induces pleiotropic anti-myeloma activity in vitro and in vivo

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

MEK1/2 inhibitors AS703026 and AZD6244 may be potential therapies for KRAS mutated colorectal cancer that is resistant to EGFR monoclonal antibody therapy

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Antitumor activity of pimasertib, a selective MEK 1/2 inhibitor, in combination with PI3K/mTOR inhibitors or with multi-targeted kinase inhibitors in pimasertib-resistant human lung and colorectal cancer cells

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

The safety, tolerability, pharmacokinetics, and pharmacodynamics of single oral doses of CH4987655 in healthy volunteers: target suppression using a biomarker.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Phase I expansion and pharmacodynamic study of the oral MEK inhibitor RO4987655 (CH4987655) in selected patients with advanced cancer with RAS-RAF mutations

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

The RAF inhibitor PLX4032 inhibits ERK signaling and tumor cell proliferation in a V600E BRAF-selective manner

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Inhibition of both BRAF and MEK in BRAF(V600E) mutant melanoma restores compromised dendritic cell (DC) function while having differential direct effects on DC properties.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Kinase inhibitors and immune check-point blockade for the treatment of metastatic melanoma and advanced cancer: synergistic or antagonistic?

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS40265-014-0315-4

A Phase II, open-label, randomised study to assess the efficacy and safety of the MEK1/2 inhibitor AZD6244 (ARRY-142886) versus capecitabine monotherapy in patients with colorectal cancer who have failed one or two prior chemotherapeutic regimens

21 January 2018

1 reference

12 December 2020

A first-in-human phase I study to evaluate the MEK1/2 inhibitor, cobimetinib, administered daily in patients with advanced solid tumors.

1 reference

12 December 2020

Antitumor activities of JTP-74057 (GSK1120212), a novel MEK1/2 inhibitor, on colorectal cancer cell lines in vitro and in vivo

1 reference

12 December 2020

ras oncogenes in human cancer: a review

1 reference

12 December 2020

High prevalence of BRAF mutations in thyroid cancer: genetic evidence for constitutive activation of the RET/PTC-RAS-BRAF signaling pathway in papillary thyroid carcinoma

1 reference

12 December 2020

Identification of the sites in MAP kinase kinase-1 phosphorylated by p74raf-1

1 reference

12 December 2020

Ras isoforms vary in their ability to activate Raf-1 and phosphoinositide 3-kinase

1 reference

12 December 2020

Mutations in BRAF and KRAS characterize the development of low-grade ovarian serous carcinoma

1 reference

12 December 2020

Mapping of UV photoproducts within ras proto-oncogenes in UV-irradiated cells: correlation with mutations in human skin cancer.

1 reference

12 December 2020

10.1007/S40265-014-0315-4

Identifiers

DOI

1 reference

Dimensions Publication ID

1 September 2017

1045041575

0 references

1 reference