Targeting the cancer kinome through polypharmacology (Q33893019)

29 July 2017

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title

Targeting the cancer kinome through polypharmacology (English)

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29 July 2017

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1

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29 July 2017

Henry Lin

2

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29 July 2017

Kevan M Shokat

series ordinal

3

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29 July 2017

language of work or name

English

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publication date

1 February 2010

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29 July 2017

published in

Nature Reviews Cancer

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29 July 2017

volume

10

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29 July 2017

issue

2

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29 July 2017

page(s)

130-137

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AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance

29 July 2017

cites work

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5 July 2018

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Requirement for NF-kappaB signalling in a mouse model of lung adenocarcinoma

5 July 2018

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A genome-wide RNAi screen identifies multiple synthetic lethal interactions with the Ras oncogene

5 July 2018

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Synthetic lethal interaction between oncogenic KRAS dependency and STK33 suppression in human cancer cells

5 July 2018

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Ligand-independent HER2/HER3/PI3K complex is disrupted by trastuzumab and is effectively inhibited by the PI3K inhibitor GDC-0941

5 July 2018

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PI3K pathway activation mediates resistance to MEK inhibitors in KRAS mutant cancers

5 July 2018

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Results of a phase III, randomized, placebo-controlled study of sorafenib in combination with carboplatin and paclitaxel as second-line treatment in patients with unresectable stage III or stage IV melanoma

5 July 2018

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Challenges and opportunities in defining the essential cancer kinome

5 July 2018

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Chemotherapy, bevacizumab, and cetuximab in metastatic colorectal cancer

5 July 2018

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Kinase-targeted libraries: the design and synthesis of novel, potent, and selective kinase inhibitors

5 July 2018

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Transient potent BCR-ABL inhibition is sufficient to commit chronic myeloid leukemia cells irreversibly to apoptosis

5 July 2018

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

5 July 2018

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Phosphatidylinositol 3-kinase hyperactivation results in lapatinib resistance that is reversed by the mTOR/phosphatidylinositol 3-kinase inhibitor NVP-BEZ235.

5 July 2018

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Kinase requirements in human cells: II. Genetic interaction screens identify kinase requirements following HPV16 E7 expression in cancer cells

5 July 2018

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Kinase requirements in human cells: I. Comparing kinase requirements across various cell types

5 July 2018

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K-ras mutations and benefit from cetuximab in advanced colorectal cancer.

5 July 2018

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Network pharmacology: the next paradigm in drug discovery

5 July 2018

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Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases

5 July 2018

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A phase I-II study of combined blockade of the ErbB receptor network with trastuzumab and gefitinib in patients with HER2 (ErbB2)-overexpressing metastatic breast cancer

5 July 2018

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Efficacy of everolimus in advanced renal cell carcinoma: a double-blind, randomised, placebo-controlled phase III trial

5 July 2018

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Differential effects of oncogenic K-Ras and N-Ras on proliferation, differentiation and tumor progression in the colon

5 July 2018

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SGX393 inhibits the CML mutant Bcr-AblT315I and preempts in vitro resistance when combined with nilotinib or dasatinib.

5 July 2018

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EGFR antagonists in cancer treatment

5 July 2018

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Simultaneous targeting of Aurora kinases and Bcr-Abl kinase by the small molecule inhibitor PHA-739358 is effective against imatinib-resistant BCR-ABL mutations including T315I.

5 July 2018

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A quantitative analysis of kinase inhibitor selectivity

5 July 2018

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Paclitaxel plus bevacizumab versus paclitaxel alone for metastatic breast cancer

5 July 2018

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Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling

5 July 2018

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A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases

5 July 2018

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Cetuximab for the treatment of colorectal cancer.

5 July 2018

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The genomic landscapes of human breast and colorectal cancers

5 July 2018

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Coactivation of receptor tyrosine kinases affects the response of tumor cells to targeted therapies

5 July 2018

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The selectivity of protein kinase inhibitors: a further update

5 July 2018

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A dual phosphoinositide-3-kinase alpha/mTOR inhibitor cooperates with blockade of epidermal growth factor receptor in PTEN-mutant glioma

5 July 2018

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Sequential ABL kinase inhibitor therapy selects for compound drug-resistant BCR-ABL mutations with altered oncogenic potency

5 July 2018

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Trastuzumab--mechanism of action and use in clinical practice

5 July 2018

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Binding of ras to phosphoinositide 3-kinase p110alpha is required for ras-driven tumorigenesis in mice

5 July 2018

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MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling

5 July 2018

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Erlotinib plus gemcitabine compared with gemcitabine alone in patients with advanced pancreatic cancer: a phase III trial of the National Cancer Institute of Canada Clinical Trials Group

5 July 2018

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Sorafenib in advanced clear-cell renal-cell carcinoma

5 July 2018

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Sunitinib versus interferon alfa in metastatic renal-cell carcinoma

5 July 2018

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Escape from HER-family tyrosine kinase inhibitor therapy by the kinase-inactive HER3

5 July 2018

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Lapatinib plus capecitabine for HER2-positive advanced breast cancer

5 July 2018

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Paclitaxel-carboplatin alone or with bevacizumab for non-small-cell lung cancer

5 July 2018

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Five-year follow-up of patients receiving imatinib for chronic myeloid leukemia

5 July 2018

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The consensus coding sequences of human breast and colorectal cancers

5 July 2018

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Nilotinib in imatinib-resistant CML and Philadelphia chromosome-positive ALL

5 July 2018

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Dasatinib in imatinib-resistant Philadelphia chromosome-positive leukemias

5 July 2018

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A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma

5 July 2018

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Synergistic antitumor effects of combined epidermal growth factor receptor and vascular endothelial growth factor receptor-2 targeted therapy

5 July 2018

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Can we rationally design promiscuous drugs?

5 July 2018

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Molecular determinants of the response of glioblastomas to EGFR kinase inhibitors.

5 July 2018

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BRAF mutation predicts sensitivity to MEK inhibition

5 July 2018

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RNAi-based screening of the human kinome identifies Akt-cooperating kinases: a new approach to designing efficacious multitargeted kinase inhibitors.

5 July 2018

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Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases

5 July 2018

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Erlotinib in previously treated non-small-cell lung cancer

5 July 2018

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Features of selective kinase inhibitors

5 July 2018

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Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo

5 July 2018

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Mutant PIK3CA promotes cell growth and invasion of human cancer cells

5 July 2018

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Acquired resistance of lung adenocarcinomas to gefitinib or erlotinib is associated with a second mutation in the EGFR kinase domain

5 July 2018

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A small molecule-kinase interaction map for clinical kinase inhibitors

5 July 2018

1 reference

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KRAS mutations and primary resistance of lung adenocarcinomas to gefitinib or erlotinib

5 July 2018

1 reference

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Renewing the conspiracy theory debate: does Raf function alone to mediate Ras oncogenesis?

5 July 2018

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https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2880454

A missense mutation in KIT kinase domain 1 correlates with imatinib resistance in gastrointestinal stromal tumors

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2880454

A new mutation in the KIT ATP pocket causes acquired resistance to imatinib in a gastrointestinal stromal tumor patient

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2880454

Target identification in chemical genetics: the (often) missing link

5 July 2018

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https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2880454

Treatment of HER-2/neu overexpressing breast cancer xenograft models with trastuzumab (Herceptin) and gefitinib (ZD1839): drug combination effects on tumor growth, HER-2/neu and epidermal growth factor receptor expression, and viable hypoxic cell fr

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2880454

Kinase mutations and imatinib response in patients with metastatic gastrointestinal stromal tumor

5 July 2018

1 reference

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A randomized trial of bevacizumab, an anti-vascular endothelial growth factor antibody, for metastatic renal cancer

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2880454

Benefits of targeting both pericytes and endothelial cells in the tumor vasculature with kinase inhibitors

5 July 2018

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A tyrosine kinase created by fusion of the PDGFRA and FIP1L1 genes as a therapeutic target of imatinib in idiopathic hypereosinophilic syndrome

5 July 2018

1 reference

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The protein kinase complement of the human genome

5 July 2018

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Mutations of the BRAF gene in human cancer

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2880454

Use of isogenic human cancer cells for high-throughput screening and drug discovery

5 July 2018

1 reference

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Discovery of a novel Raf kinase inhibitor

5 July 2018

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Clinical resistance to STI-571 cancer therapy caused by BCR-ABL gene mutation or amplification

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2880454

Efficacy and safety of a specific inhibitor of the BCR-ABL tyrosine kinase in chronic myeloid leukemia

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2880454

Specificity and mechanism of action of some commonly used protein kinase inhibitors

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2880454

Disorders in cell circuitry associated with multistage carcinogenesis: exploitable targets for cancer prevention and therapy.

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2880454

Phosphatidylinositol-3-OH kinase as a direct target of Ras

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2880454

Assessment of chemical coverage of kinome space and its implications for kinase drug discovery.

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2880454

Cancer: mixing cocktails.

29 October 2018

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Chemical genetics: where genetics and pharmacology meet

29 October 2018

1 reference

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Is the gefitinib plus trastuzumab combination feasible in breast cancer patients?

29 October 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2880454

Colorectal cancer: mutations in a signalling pathway

29 October 2018

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A phase I clinical trial of the sequential combination of irinotecan followed by flavopiridol

29 October 2018

1 reference

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For investigational targeted drugs, combination trials pose challenges

29 October 2018

1 reference

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Results of phase I pharmacokinetic and pharmacodynamic studies of the Raf kinase inhibitor BAY 43-9006 in patients with solid tumors.

29 October 2018

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Treatment of hypereosinophilic syndrome with imatinib mesilate

29 October 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2880454

Cooperative inhibitory effect of ZD1839 (Iressa) in combination with trastuzumab (Herceptin) on human breast cancer cell growth.

29 October 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2880454

Augmentation of apoptosis and tumor regression by flavopiridol in the presence of CPT-11 in Hct116 colon cancer monolayers and xenografts.

29 October 2018

1 reference

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Epidermal growth factor receptor (HER1) tyrosine kinase inhibitor ZD1839 (Iressa) inhibits HER2/neu (erbB2)-overexpressing breast cancer cells in vitro and in vivo

29 October 2018

1 reference

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MK-0457, a novel kinase inhibitor, is active in patients with chronic myeloid leukemia or acute lymphocytic leukemia with the T315I BCR-ABL mutation

29 October 2018

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Randomized phase II study of erlotinib combined with bevacizumab compared with bevacizumab alone in metastatic renal cell cancer

31 March 2020

1 reference

Crossref

https://api.crossref.org/works/10.1038/NRC2787

31 March 2020

Identifiers

DOI

10.1038/NRC2787

1 reference

Dimensions Publication ID

29 July 2017

0 references

1 reference

29 July 2017

1 reference