A type-II kinase inhibitor capable of inhibiting the T315I "gatekeeper" mutant of Bcr-Abl (Q34052015)

30 July 2017

title

A type-II kinase inhibitor capable of inhibiting the T315I "gatekeeper" mutant of Bcr-Abl (English)

1 reference

30 July 2017

16

Nathanael S Gray

1 reference

30 July 2017

Hwan Geun Choi

1

1 reference

30 July 2017

Pingda Ren

2

1 reference

30 July 2017

Francisco Adrian

3

1 reference

30 July 2017

Fangxian Sun

4

1 reference

30 July 2017

Hyun Soo Lee

5

1 reference

30 July 2017

Xia Wang

6

1 reference

30 July 2017

Qiang Ding

7

1 reference

30 July 2017

Guobao Zhang

8

1 reference

30 July 2017

Yongping Xie

9

1 reference

30 July 2017

Jianming Zhang

10

1 reference

30 July 2017

Yi Liu

11

1 reference

30 July 2017

Tove Tuntland

12

1 reference

30 July 2017

Markus Warmuth

13

1 reference

30 July 2017

Paul W Manley

14

1 reference

30 July 2017

Jürgen Mestan

15

1 reference

30 July 2017

Taebo Sim

17

1 reference

30 July 2017

language of work or name

English

0 references

publication date

1 August 2010

1 reference

Journal of Medicinal Chemistry

30 July 2017

published in

1 reference

30 July 2017

volume

53

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30 July 2017

issue

15

1 reference

30 July 2017

page(s)

5439-5448

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9-(Arenethenyl)purines as dual Src/Abl kinase inhibitors targeting the inactive conformation: design, synthesis, and biological evaluation

30 July 2017

cites work

1 reference

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Equally Potent Inhibition of c-Src and Abl by Compounds that Recognize Inactive Kinase Conformations

5 July 2018

1 reference

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Small Molecule Recognition of c-Src via the Imatinib-Binding Conformation

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4134510

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

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4134510

Flying under the radar: the new wave of BCR-ABL 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=4134510

Crystal structure of the T315I Abl mutant in complex with the aurora kinases inhibitor PHA-739358

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4134510

Ba/F3 cells and their use in kinase drug discovery

5 July 2018

1 reference

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In vitro and in vivo activity of SKI-606, a novel Src-Abl inhibitor, against imatinib-resistant Bcr-Abl+ neoplastic cells

5 July 2018

1 reference

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N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor

5 July 2018

1 reference

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Janus kinase 2: a critical target in chronic myelogenous leukemia

5 July 2018

1 reference

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Rational design of inhibitors that bind to inactive kinase conformations

5 July 2018

1 reference

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The structure of Dasatinib (BMS-354825) bound to activated ABL kinase domain elucidates its inhibitory activity against imatinib-resistant ABL mutants

5 July 2018

1 reference

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An efficient rapid system for profiling the cellular activities of molecular libraries.

5 July 2018

1 reference

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Allosteric inhibitors of Bcr-abl-dependent cell proliferation

5 July 2018

1 reference

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

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4134510

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

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4134510

Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl.

5 July 2018

1 reference

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AMN107: tightening the grip of imatinib

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4134510

A non-ATP-competitive inhibitor of BCR-ABL overrides imatinib resistance

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4134510

Overriding imatinib resistance with a novel ABL kinase inhibitor

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4134510

Imatinib (STI571) resistance in chronic myelogenous leukemia: molecular basis of the underlying mechanisms and potential strategies for treatment

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4134510

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

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4134510

Crystal structures of the kinase domain of c-Abl in complex with the small molecule inhibitors PD173955 and imatinib (STI-571)

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4134510

2-Substituted aminopyrido[2,3-d]pyrimidin-7(8H)-ones. structure-activity relationships against selected tyrosine kinases and in vitro and in vivo anticancer activity

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4134510

In vitro pharmacological characterization of PD 166285, a new nanomolar potent and broadly active protein tyrosine kinase inhibitor.

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4134510

A general strategy for creating "inactive-conformation" abl 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=4134510

Prediction of resistance to small molecule FLT3 inhibitors: implications for molecularly targeted therapy of acute leukemia

28 October 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4134510

Characterization of a conserved structural determinant controlling protein kinase sensitivity to selective inhibitors.

28 October 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4134510

Discovery and initial SAR of 2-amino-5-carboxamidothiazoles as inhibitors of the Src-family kinase p56Lck

28 October 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4134510

Characterization of potent inhibitors of the Bcr-Abl and the c-kit receptor tyrosine kinases.

28 October 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4134510

The pyrido[2,3-d]pyrimidine derivative PD180970 inhibits p210Bcr-Abl tyrosine kinase and induces apoptosis of K562 leukemic cells

28 October 2018

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/20604564

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Biochemical and cellular effects of c-Src kinase-selective pyrido[2, 3-d]pyrimidine tyrosine kinase inhibitors

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/20604564

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Identifiers

DOI

10.1021/JM901808W

1 reference

30 July 2017

1 reference

30 July 2017

1 reference