(Q36874745)

English

Kinase scaffold repurposing for neglected disease drug discovery: discovery of an efficacious, lapatinib-derived lead compound for trypanosomiasis

scientific article published on 3 May 2013

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scholarly article

1 reference

Europe PubMed Central

PMC publication ID

16 August 2017

Kinase scaffold repurposing for neglected disease drug discovery: discovery of an efficacious, lapatinib-derived lead compound for trypanosomiasis (English)

1 reference

Europe PubMed Central

PMC publication ID

16 August 2017

trypanosomiasis

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1 reference

based on heuristic

inferred from title

object named as

Paul J Guyett

4

0 references

Michael P. Pollastri

object named as

Michael P Pollastri

9

0 references

author name string

Gautam Patel

1

1 reference

Europe PubMed Central

PMC publication ID

16 August 2017

Caitlin E Karver

2

1 reference

Europe PubMed Central

PMC publication ID

16 August 2017

Ranjan Behera

3

1 reference

Europe PubMed Central

PMC publication ID

16 August 2017

Catherine Sullenberger

5

1 reference

Europe PubMed Central

PMC publication ID

16 August 2017

Peter Edwards

6

1 reference

Europe PubMed Central

PMC publication ID

16 August 2017

Norma E Roncal

7

1 reference

Europe PubMed Central

PMC publication ID

16 August 2017

Kojo Mensa-Wilmot

8

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Europe PubMed Central

PMC publication ID

16 August 2017

language of work or name

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publication date

3 May 2013

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Europe PubMed Central

PMC publication ID

16 August 2017

Journal of Medicinal Chemistry

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Europe PubMed Central

PMC publication ID

16 August 2017

56

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Europe PubMed Central

PMC publication ID

16 August 2017

10

1 reference

Europe PubMed Central

PMC publication ID

16 August 2017

3820-3832

1 reference

Europe PubMed Central

PMC publication ID

16 August 2017

Lapatinib-binding protein kinases in the African trypanosome: identification of cellular targets for kinase-directed chemical scaffolds

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

Identification of compounds with anti-proliferative activity against Trypanosoma brucei brucei strain 427 by a whole cell viability based HTS campaign

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

The human Aurora kinase inhibitor danusertib is a lead compound for anti-trypanosomal drug discovery via target repurposing.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

Moving beyond rules: the development of a central nervous system multiparameter optimization (CNS MPO) approach to enable alignment of druglike properties

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

Defining desirable central nervous system drug space through the alignment of molecular properties, in vitro ADME, and safety attributes

1 reference

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29 September 2017

Small molecule kinase inhibitors as anti-cancer therapeutics

1 reference

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29 September 2017

Pharmacological validation of Trypanosoma brucei phosphodiesterases as novel drug targets

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

Pharmacological validation of Trypanosoma brucei phosphodiesterases B1 and B2 as druggable targets for African sleeping sickness

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

The susceptibility of trypanosomatid pathogens to PI3/mTOR kinase inhibitors affords a new opportunity for drug repurposing

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

Target repurposing for neglected diseases

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

SCYX-7158, an orally-active benzoxaborole for the treatment of stage 2 human African trypanosomiasis

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

Trypanosoma brucei glycogen synthase kinase-3, a target for anti-trypanosomal drug development: a public-private partnership to identify novel leads

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

Cyclic-nucleotide signalling in protozoa

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

Cross-resistance to nitro drugs and implications for treatment of human African trypanosomiasis

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

Diacylglycerol-stimulated endocytosis of transferrin in trypanosomatids is dependent on tyrosine kinase activity

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

Targeting protein kinases in central nervous system disorders

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

The phosphoproteome of bloodstream form Trypanosoma brucei, causative agent of African sleeping sickness

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

Tyrosine kinases and inflammatory signalling

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

Tyrosine kinase inhibitors reverse type 1 diabetes in nonobese diabetic mice

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

Analysis of the Trypanosoma brucei cell cycle by quantitative DAPI imaging.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

Cytokinesis in trypanosomatids

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

Cell cycle regulation in Trypanosoma brucei

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

Innovative lead discovery strategies for tropical diseases

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

Therapeutic potential of phosphatidylinositol 3-kinase inhibitors in inflammatory respiratory disease.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

Lessons from the drug discovery of lapatinib, a dual ErbB1/2 tyrosine kinase inhibitor

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

Protein kinases as drug targets in trypanosomes and Leishmania

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

Comparative analysis of the kinomes of three pathogenic trypanosomatids: Leishmania major, Trypanosoma brucei and Trypanosoma cruzi

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

Both of the Rab5 subfamily small GTPases of Trypanosoma brucei are essential and required for endocytosis.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

Axenic culture of African trypanosome bloodstream forms

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

AEE788: a dual family epidermal growth factor receptor/ErbB2 and vascular endothelial growth factor receptor tyrosine kinase inhibitor with antitumor and antiangiogenic activity

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

Ligand efficiency: a useful metric for lead selection

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

Discovery and development of GSK3 inhibitors for the treatment of type 2 diabetes

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

CI-1033, a pan-erbB tyrosine kinase inhibitor

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

The characterization of novel, dual ErbB-2/EGFR, tyrosine kinase inhibitors: potential therapy for cancer

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

The transferrin receptor of Trypanosoma brucei

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

Epidermal growth factor receptor efficiently activates mitogen-activated protein kinase in HeLa cells and Hep2 cells conditionally defective in clathrin-dependent endocytosis

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

29 September 2017

Identification and specific localization of tyrosine-phosphorylated proteins in Trypanosoma brucei.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

27 June 2018

Endocytosis by African trypanosomes. II. Occurrence in different life-cycle stages and intracellular sorting.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

27 June 2018

Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

4 September 2018

Discovery and structure-activity relationships of a novel class of quinazoline glucokinase activators

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

4 September 2018

Glycosylphosphatidylinositol-specific phospholipase C regulates transferrin endocytosis in the African trypanosome

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

4 September 2018

Discovery of trypanocidal compounds by whole cell HTS of Trypanosoma brucei

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

4 September 2018

Anti-tumor activity of GW572016: a dual tyrosine kinase inhibitor blocks EGF activation of EGFR/erbB2 and downstream Erk1/2 and AKT pathways

1 reference

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4 September 2018

MTT colorimetric assay for testing macrophage cytotoxic activity in vitro

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3663906

4 September 2018

Tyrosine Kinase Inhibitors

1 reference

https://pubmed.ncbi.nlm.nih.gov/23597080

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Drug to Genome to Drug: Discovery of New Antiplasmodial Compounds

1 reference

https://pubmed.ncbi.nlm.nih.gov/23597080

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Identifiers

10.1021/JM400349K

1 reference

Europe PubMed Central

PMC publication ID

16 August 2017

PMC publication ID

1 reference

Europe PubMed Central

PMC publication ID

16 August 2017

PubMed publication ID

1 reference

Europe PubMed Central

PMC publication ID

16 August 2017

ResearchGate publication ID

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