(Q47411655)

15 January 2018

http://europepmc.org/abstract/MED/29129716

title

The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study (English)

1 reference

15 January 2018

http://europepmc.org/abstract/MED/29129716

author

George M. Burslem

1

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:29129716%20AND%20SRC:MED&resulttype=core&format=json

8 June 2020

Blake E Smith

2

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:29129716%20AND%20SRC:MED&resulttype=core&format=json

8 June 2020

Daniel McQuaid

5

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:29129716%20AND%20SRC:MED&resulttype=core&format=json

8 June 2020

author name string

Ashton C Lai

3

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:29129716%20AND%20SRC:MED&resulttype=core&format=json

8 June 2020

Saul Jaime-Figueroa

4

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:29129716%20AND%20SRC:MED&resulttype=core&format=json

8 June 2020

Daniel P Bondeson

6

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:29129716%20AND%20SRC:MED&resulttype=core&format=json

8 June 2020

Momar Toure

7

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:29129716%20AND%20SRC:MED&resulttype=core&format=json

8 June 2020

Hanqing Dong

8

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:29129716%20AND%20SRC:MED&resulttype=core&format=json

8 June 2020

Yimin Qian

9

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:29129716%20AND%20SRC:MED&resulttype=core&format=json

8 June 2020

Jing Wang

10

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:29129716%20AND%20SRC:MED&resulttype=core&format=json

8 June 2020

Andrew P Crew

11

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:29129716%20AND%20SRC:MED&resulttype=core&format=json

8 June 2020

John Hines

12

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:29129716%20AND%20SRC:MED&resulttype=core&format=json

8 June 2020

Craig M Crews

13

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:29129716%20AND%20SRC:MED&resulttype=core&format=json

8 June 2020

publication date

25 October 2017

1 reference

15 January 2018

http://europepmc.org/abstract/MED/29129716

published in

Cell chemical biology

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:29129716%20AND%20SRC:MED&resulttype=core&format=json

8 June 2020

volume

25

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:29129716%20AND%20SRC:MED&resulttype=core&format=json

8 June 2020

issue

1

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:29129716%20AND%20SRC:MED&resulttype=core&format=json

8 June 2020

page(s)

67-77.e3

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:29129716%20AND%20SRC:MED&resulttype=core&format=json

Chemically Induced Degradation of Sirtuin 2 (Sirt2) by a Proteolysis Targeting Chimera (PROTAC) Based on Sirtuin Rearranging Ligands (SirReals).

8 June 2020

cites work

1 reference

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Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression.

26 August 2018

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Selective Downregulation of JAK2 and JAK3 by an ATP-Competitive pan-JAK Inhibitor

26 August 2018

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Structural basis of PROTAC cooperative recognition for selective protein degradation

26 August 2018

1 reference

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Protein Degradation by In-Cell Self-Assembly of Proteolysis Targeting Chimeras.

26 August 2018

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Resistance to BET Bromodomain Inhibitors Is Mediated by Kinome Reprogramming in Ovarian Cancer

26 August 2018

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PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer

26 August 2018

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Mutations at the splice sites of exon 14 of MET gene: a new target for sarcomatoid carcinomas?

26 August 2018

1 reference

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MET Exon 14 Alterations in Lung Cancer: Exon Skipping Extends Half-Life

26 August 2018

1 reference

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Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL.

26 August 2018

1 reference

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Phase III Multinational, Randomized, Double-Blind, Placebo-Controlled Study of Tivantinib (ARQ 197) Plus Erlotinib Versus Erlotinib Alone in Previously Treated Patients With Locally Advanced or Metastatic Nonsquamous Non-Small-Cell Lung Cancer.

26 August 2018

1 reference

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Catalytic in vivo protein knockdown by small-molecule PROTACs.

26 August 2018

1 reference

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HaloPROTACS: Use of Small Molecule PROTACs to Induce Degradation of HaloTag Fusion Proteins

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4.

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4.

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

Inhibition of Lapatinib-Induced Kinome Reprogramming in ERBB2-Positive Breast Cancer by Targeting BET Family Bromodomains

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

Pharmacological targeting of the pseudokinase Her3

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

Human Epidermal Growth Factor Receptor 2 (HER2) in Cancers: Overexpression and Therapeutic Implications

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

Structural, Biochemical, and Clinical Characterization of Epidermal Growth Factor Receptor (EGFR) Exon 20 Insertion Mutations in Lung Cancer

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

The HSP90 inhibitor ganetespib synergizes with the MET kinase inhibitor crizotinib in both crizotinib-sensitive and -resistant MET-driven tumor models

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

Epidermal growth factor receptor targeting in cancer: a review of trends and strategies.

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

Posttranslational protein knockdown coupled to receptor tyrosine kinase activation with phosphoPROTACs

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

A comprehensive mathematical model for three-body binding equilibria

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

The dynamic nature of the kinome

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

Small-Molecule Inhibitors of the Interaction between the E3 Ligase VHL and HIF1α

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

Target binding properties and cellular activity of afatinib (BIBW 2992), an irreversible ErbB family blocker

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

Targeting the von Hippel–Lindau E3 Ubiquitin Ligase Using Small Molecules To Disrupt the VHL/HIF-1α Interaction

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

Targeting MET in cancer: rationale and progress

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

Receptor tyrosine kinases and targeted cancer therapeutics

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

An overview of the c-MET signaling pathway

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

Randomized phase II study of erlotinib plus tivantinib versus erlotinib plus placebo in previously treated non-small-cell lung cancer.

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

Small-molecule hydrophobic tagging-induced degradation of HaloTag fusion proteins.

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

A direct role for Met endocytosis in tumorigenesis.

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

Foretinib (GSK1363089), an orally available multikinase inhibitor of c-Met and VEGFR-2, blocks proliferation, induces anoikis, and impairs ovarian cancer metastasis.

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

Cell signaling by receptor tyrosine kinases

26 August 2018

1 reference

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Receptor tyrosine kinase coactivation networks in cancer

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

Gastric cancer cell line Hs746T harbors a splice site mutation of c-Met causing juxtamembrane domain deletion

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

Efficient protection and isolation of ubiquitylated proteins using tandem ubiquitin-binding entities

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

Cancer cells harboring MET gene amplification activate alternative signaling pathways to escape MET inhibition but remain sensitive to Hsp90 inhibitors

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

The plasticity of oncogene addiction: implications for targeted therapies directed to receptor tyrosine kinases

26 August 2018

1 reference

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Targeting HSP90 for cancer therapy

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

An inhibitor of NEDD8-activating enzyme as a new approach to treat cancer

26 August 2018

1 reference

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A pharmacodynamic study of the FLT3 inhibitor KW-2449 yields insight into the basis for clinical response

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

Targeted intracellular protein degradation induced by a small molecule: En route to chemical proteomics

26 August 2018

1 reference

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Low dose geldanamycin inhibits hepatocyte growth factor and hypoxia-stimulated invasion of cancer cells

26 August 2018

1 reference

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

26 August 2018

1 reference

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EGFR targeting therapies: monoclonal antibodies versus tyrosine kinase inhibitors. Similarities and differences.

26 August 2018

1 reference

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Epidermal growth factor receptor (EGFR) antibody down-regulates mutant receptors and inhibits tumors expressing EGFR mutations

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

Small GTPase Rab21 regulates cell adhesion and controls endosomal traffic of beta1-integrins

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

Activity of the dual kinase inhibitor lapatinib (GW572016) against HER-2-overexpressing and trastuzumab-treated breast cancer cells

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

Somatic mutations lead to an oncogenic deletion of met in lung cancer

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

Development and characterization of proteasome inhibitors

26 August 2018

1 reference

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Met/Hepatocyte growth factor receptor ubiquitination suppresses transformation and is required for Hrs phosphorylation

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

Phosphotyrosine signaling networks in epidermal growth factor receptor overexpressing squamous carcinoma cells

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

The discovery of receptor tyrosine kinases: targets for cancer therapy

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

Met, metastasis, motility and more

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

Protein kinase C controls microtubule-based traffic but not proteasomal degradation of c-Met.

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

ZD1839, a specific epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, induces the formation of inactive EGFR/HER2 and EGFR/HER3 heterodimers and prevents heregulin signaling in HER2-overexpressing breast cancer cells

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

Mutation of the c-Cbl TKB domain binding site on the Met receptor tyrosine kinase converts it into a transforming protein

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

Protacs: chimeric molecules that target proteins to the Skp1-Cullin-F box complex for ubiquitination and degradation

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

Cross-talk between epidermal growth factor receptor and c-Met signal pathways in transformed cells

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

Hepatocyte growth factor is predominantly expressed by the carcinoma cells in non–small-cell lung cancer

26 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5831399

Greasy tags for protein removal

1 December 2018

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/29129716

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Identifiers

DOI

10.1016/J.CHEMBIOL.2017.09.009

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:29129716%20AND%20SRC:MED&resulttype=core&format=json

8 June 2020

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:29129716%20AND%20SRC:MED&resulttype=core&format=json

8 June 2020

1 reference