(Q34104338)

31 July 2017

title

UNC2025, a potent and orally bioavailable MER/FLT3 dual inhibitor (English)

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31 July 2017

Weihe Zhang

1

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31 July 2017

Deborah DeRyckere

2

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31 July 2017

Debra Hunter

3

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31 July 2017

Jing Liu

4

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31 July 2017

Michael A Stashko

5

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31 July 2017

Katherine A Minson

6

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31 July 2017

Christopher T Cummings

7

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31 July 2017

Minjung Lee

8

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31 July 2017

Trevor G Glaros

9

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31 July 2017

Dianne L Newton

10

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31 July 2017

Susan Sather

11

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31 July 2017

Dehui Zhang

12

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31 July 2017

Dmitri Kireev

13

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31 July 2017

William P Janzen

14

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31 July 2017

H Shelton Earp

15

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31 July 2017

Douglas K Graham

16

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31 July 2017

Stephen V Frye

17

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31 July 2017

Xiaodong Wang

18

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31 July 2017

language of work or name

English

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publication date

6 August 2014

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Journal of Medicinal Chemistry

31 July 2017

published in

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31 July 2017

volume

57

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31 July 2017

issue

16

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31 July 2017

page(s)

7031-7041

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describes a project that uses

31 July 2017

ImageJ

1 reference

11 June 2022

https://www.ebi.ac.uk/europepmc/webservices/rest/PMC4148167/fullTextXML

inferred from PubMed Central ID database lookup

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5 July 2018

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Mer or Axl receptor tyrosine kinase inhibition promotes apoptosis, blocks growth and enhances chemosensitivity of human non-small cell lung cancer

5 July 2018

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Discovery of Small Molecule Mer Kinase Inhibitors for the Treatment of Pediatric Acute Lymphoblastic Leukemia

5 July 2018

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5 July 2018

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5 July 2018

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5 July 2018

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5 July 2018

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In situ kinase profiling reveals functionally relevant properties of native kinases

5 July 2018

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Structure-Guided Lead Optimization of Triazolopyrimidine-Ring Substituents Identifies Potent Plasmodium falciparum Dihydroorotate Dehydrogenase Inhibitors with Clinical Candidate Potential

5 July 2018

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Foretinib (GSK1363089), a multi-kinase inhibitor of MET and VEGFRs, inhibits growth of gastric cancer cell lines by blocking inter-receptor tyrosine kinase networks

5 July 2018

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Discovery of a 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer

5 July 2018

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5 July 2018

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5 July 2018

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Inhibition of Mer and Axl receptor tyrosine kinases in astrocytoma cells leads to increased apoptosis and improved chemosensitivity

5 July 2018

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Molecular target class is predictive of in vitro response profile

5 July 2018

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5 July 2018

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5 July 2018

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5 July 2018

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Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase 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=4148167

Structural insights into the inhibited states of the Mer receptor tyrosine kinase

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4148167

TAM receptor tyrosine kinases: biologic functions, signaling, and potential therapeutic targeting in human cancer

5 July 2018

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Phase 1 clinical results with tandutinib (MLN518), a novel FLT3 antagonist, in patients with acute myelogenous leukemia or high-risk myelodysplastic syndrome: safety, pharmacokinetics, and pharmacodynamics

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4148167

A phase 2 trial of the FLT3 inhibitor lestaurtinib (CEP701) as first-line treatment for older patients with acute myeloid leukemia not considered fit for intensive chemotherapy

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4148167

Ectopic expression of the proto-oncogene Mer in pediatric T-cell acute lymphoblastic 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=4148167

RNAi-induced down-regulation of FLT3 expression in AML cell lines increases sensitivity to MLN518.

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4148167

Can the pharmaceutical industry reduce attrition rates?

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4148167

The presence of a FLT3 internal tandem duplication in patients with acute myeloid leukemia (AML) adds important prognostic information to cytogenetic risk group and response to the first cycle of chemotherapy: analysis of 854 patients from the Unite

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4148167

Kinetics of the reversible inhibition of enzyme-catalysed reactions by tight-binding 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=4148167

Pyrazolopyridine inhibitors of B-Raf(V600E). Part 3: an increase in aqueous solubility via the disruption of crystal packing.

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4148167

Lymphoblastic leukemia/lymphoma in mice overexpressing the Mer (MerTK) receptor tyrosine kinase

28 October 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4148167

Patients with acute myeloid leukemia and an activating mutation in FLT3 respond to a small-molecule FLT3 tyrosine kinase inhibitor, PKC412.

28 October 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4148167

Strain energy of small ring hydrocarbons. Influence of C-h bond dissociation energies

28 October 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4148167

Identification of Gas6 as a ligand for Mer, a neural cell adhesion molecule related receptor tyrosine kinase implicated in cellular transformation.

28 October 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4148167

FLT3 internal tandem duplication mutations in adult acute myeloid leukaemia define a high-risk group

28 October 2018

1 reference

12 December 2020

New horizons in drug metabolism, pharmacokinetics and drug discovery

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12 December 2020

Evaluation of enzyme inhibitors in drug discovery. A guide for medicinal chemists and pharmacologists

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12 December 2020

Picornavirus inhibitors: trifluoromethyl substitution provides a global protective effect against hepatic metabolism

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12 December 2020

Identifiers

DOI

10.1021/JM500749D

1 reference

31 July 2017

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31 July 2017

1 reference