Novel mutant-selective EGFR kinase inhibitors against EGFR T790M (Q27658766)

ChEBI release 2020-05-28

12

Kwok-Kin Wong

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John R. Engen

John R Engen

11

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Marzia Capelletti

Marzia Capelletti

6

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Pasi A Jänne

15

Pasi A Jänne

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Nathanael Gray

14

Nathanael S Gray

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author name string

Wenjun Zhou

1

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Dalia Ercan

2

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Liang Chen

3

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Cai-Hong Yun

4

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Danan Li

5

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Alexis B Cortot

7

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Lucian Chirieac

8

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Roxana E Iacob

9

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Robert Padera

10

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Michael J Eck

Crystal Structures of the FAK Kinase in Complex with TAE226 and Related Bis-Anilino Pyrimidine Inhibitors Reveal a Helical DFG Conformation

13

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language of work or name

English

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publication date

24 December 2009

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published in

Nature

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volume

462

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page(s)

1070-4

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issue

7276

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cites work

1 reference

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BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models

20 March 2017

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Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity

20 March 2017

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The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP

20 March 2017

1 reference

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Synthesis and SAR of aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors

20 March 2017

1 reference

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Structures of Lung Cancer-Derived EGFR Mutants and Inhibitor Complexes: Mechanism of Activation and Insights into Differential Inhibitor Sensitivity

20 March 2017

1 reference

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

20 March 2017

1 reference

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EGFR mutation and resistance of non-small-cell lung cancer to gefitinib

20 March 2017

1 reference

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

20 March 2017

1 reference

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Allelic dilution obscures detection of a biologically significant resistance mutation in EGFR-amplified lung cancer

20 March 2017

1 reference

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The impact of human EGFR kinase domain mutations on lung tumorigenesis and in vivo sensitivity to EGFR-targeted therapies

20 March 2017

1 reference

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Gefitinib or carboplatin-paclitaxel in pulmonary adenocarcinoma

20 March 2017

1 reference

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Screening for epidermal growth factor receptor mutations in lung cancer

20 March 2017

1 reference

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Autocrine production of amphiregulin predicts sensitivity to both gefitinib and cetuximab in EGFR wild-type cancers

7 April 2017

1 reference

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PHA-680626 exhibits anti-proliferative and pro-apoptotic activity on Imatinib-resistant chronic myeloid leukemia cell lines and primary CD34+ cells by inhibition of both Bcr-Abl tyrosine kinase and Aurora kinases

29 September 2017

1 reference

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

29 September 2017

1 reference

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PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefitinib

29 September 2017

1 reference

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Multicenter, randomized, phase II trial of CI-1033, an irreversible pan-ERBB inhibitor, for previously treated advanced non small-cell lung cancer

29 September 2017

1 reference

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Emergence of epidermal growth factor receptor T790M mutation during chronic exposure to gefitinib in a non small cell lung cancer cell line

29 September 2017

1 reference

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Bronchial and peripheral murine lung carcinomas induced by T790M-L858R mutant EGFR respond to HKI-272 and rapamycin combination therapy

29 September 2017

1 reference

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Kinetic analysis of epidermal growth factor receptor somatic mutant proteins shows increased sensitivity to the epidermal growth factor receptor tyrosine kinase inhibitor, erlotinib

29 September 2017

1 reference

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Comparison of imatinib mesylate, dasatinib (BMS-354825), and nilotinib (AMN107) in an N-ethyl-N-nitrosourea (ENU)-based mutagenesis screen: high efficacy of drug combinations

29 September 2017

1 reference

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Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase

2 June 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2879581

The T790M "gatekeeper" mutation in EGFR mediates resistance to low concentrations of an irreversible EGFR inhibitor

27 November 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2879581

Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 2: identification and optimisation of substituted 2,4-bis anilino pyrimidines

27 November 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2879581

Allele-dependent variation in the relative cellular potency of distinct EGFR inhibitors

27 November 2018

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/20033049

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Micronutrient sprinkles to control childhood anaemia

1 reference

Crossref

https://api.crossref.org/works/10.1038%2FNATURE08622

inferred from DOI database lookup

7 January 2021

based on heuristic

Identifiers

DOI

10.1038/NATURE08622

1 reference

Dimensions Publication ID

8341

1009588480

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8341

1 reference

1 reference

1 reference