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Identification of Inhibitors of the Leishmania cdc2-Related Protein Kinase CRK3

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Identification of Inhibitors of the Leishmania cdc2-Related Protein Kinase CRK3. / Cleghorn, Laura A. T.; Woodland, Andrew; Collie, Iain T.; Torrie, Leah S.; Norcross, Neil; Luksch, Torsten; Mpamhanga, Chido; Walker, Roderick G.; Mottram, Jeremy C.; Brenk, Ruth; Frearson, Julie A.; Gilbert, Ian H.; Wyatt, Paul G. (Lead / Corresponding author).

In: ChemMedChem, Vol. 6, No. 12, 09.12.2011, p. 2214-2224.

Research output: Contribution to journalArticle

Harvard

Cleghorn, LAT, Woodland, A, Collie, IT, Torrie, LS, Norcross, N, Luksch, T, Mpamhanga, C, Walker, RG, Mottram, JC, Brenk, R, Frearson, JA, Gilbert, IH & Wyatt, PG 2011, 'Identification of Inhibitors of the Leishmania cdc2-Related Protein Kinase CRK3' ChemMedChem, vol 6, no. 12, pp. 2214-2224., 10.1002/cmdc.201100344

APA

Cleghorn, L. A. T., Woodland, A., Collie, I. T., Torrie, L. S., Norcross, N., Luksch, T., ... Wyatt, P. G. (2011). Identification of Inhibitors of the Leishmania cdc2-Related Protein Kinase CRK3. ChemMedChem, 6(12), 2214-2224. 10.1002/cmdc.201100344

Vancouver

Cleghorn LAT, Woodland A, Collie IT, Torrie LS, Norcross N, Luksch T et al. Identification of Inhibitors of the Leishmania cdc2-Related Protein Kinase CRK3. ChemMedChem. 2011 Dec 9;6(12):2214-2224. Available from: 10.1002/cmdc.201100344

Author

Cleghorn, Laura A. T.; Woodland, Andrew; Collie, Iain T.; Torrie, Leah S.; Norcross, Neil; Luksch, Torsten; Mpamhanga, Chido; Walker, Roderick G.; Mottram, Jeremy C.; Brenk, Ruth; Frearson, Julie A.; Gilbert, Ian H.; Wyatt, Paul G. (Lead / Corresponding author) / Identification of Inhibitors of the Leishmania cdc2-Related Protein Kinase CRK3.

In: ChemMedChem, Vol. 6, No. 12, 09.12.2011, p. 2214-2224.

Research output: Contribution to journalArticle

Bibtex - Download

@article{da4a4674a064480d8ea707c732b55eed,
title = "Identification of Inhibitors of the Leishmania cdc2-Related Protein Kinase CRK3",
keywords = "CRK3, cyclin-dependent cdc2-related kinases, leishmaniasis, triazolopyridines, ureas, CYCLIN-DEPENDENT KINASE, TRYPANOSOMA-BRUCEI, 3-AMINOPYRAZOLE INHIBITORS, ANTITUMOR AGENTS, DISCOVERY, MEXICANA, DISEASES",
author = "Cleghorn, {Laura A. T.} and Andrew Woodland and Collie, {Iain T.} and Torrie, {Leah S.} and Neil Norcross and Torsten Luksch and Chido Mpamhanga and Walker, {Roderick G.} and Mottram, {Jeremy C.} and Ruth Brenk and Frearson, {Julie A.} and Gilbert, {Ian H.} and Wyatt, {Paul G.}",
year = "2011",
doi = "10.1002/cmdc.201100344",
volume = "6",
number = "12",
pages = "2214--2224",
journal = "ChemMedChem",
issn = "1860-7179",

}

RIS (suitable for import to EndNote) - Download

TY - JOUR

T1 - Identification of Inhibitors of the Leishmania cdc2-Related Protein Kinase CRK3

A1 - Cleghorn,Laura A. T.

A1 - Woodland,Andrew

A1 - Collie,Iain T.

A1 - Torrie,Leah S.

A1 - Norcross,Neil

A1 - Luksch,Torsten

A1 - Mpamhanga,Chido

A1 - Walker,Roderick G.

A1 - Mottram,Jeremy C.

A1 - Brenk,Ruth

A1 - Frearson,Julie A.

A1 - Gilbert,Ian H.

A1 - Wyatt,Paul G.

AU - Cleghorn,Laura A. T.

AU - Woodland,Andrew

AU - Collie,Iain T.

AU - Torrie,Leah S.

AU - Norcross,Neil

AU - Luksch,Torsten

AU - Mpamhanga,Chido

AU - Walker,Roderick G.

AU - Mottram,Jeremy C.

AU - Brenk,Ruth

AU - Frearson,Julie A.

AU - Gilbert,Ian H.

AU - Wyatt,Paul G.

PY - 2011/12/9

Y1 - 2011/12/9

N2 - <p>New drugs are urgently needed for the treatment of tropical parasitic diseases such as leishmaniasis and human African trypanosomiasis (HAT). This work involved a high-throughput screen of a focussed kinase set of similar to 3400 compounds to identify potent and parasite-selective inhibitors of an enzymatic Leishmania CRK3-cyclin 6 complex. The aim of this study is to provide chemical validation that Leishmania CRK3-CYC6 is a drug target. Eight hit series were identified, of which four were followed up. The optimisation of these series using classical SAR studies afforded low-nanomolar CRK3 inhibitors with significant selectivity over the closely related human cyclin dependent kinase CDK2.</p>

AB - <p>New drugs are urgently needed for the treatment of tropical parasitic diseases such as leishmaniasis and human African trypanosomiasis (HAT). This work involved a high-throughput screen of a focussed kinase set of similar to 3400 compounds to identify potent and parasite-selective inhibitors of an enzymatic Leishmania CRK3-cyclin 6 complex. The aim of this study is to provide chemical validation that Leishmania CRK3-CYC6 is a drug target. Eight hit series were identified, of which four were followed up. The optimisation of these series using classical SAR studies afforded low-nanomolar CRK3 inhibitors with significant selectivity over the closely related human cyclin dependent kinase CDK2.</p>

KW - CRK3

KW - cyclin-dependent cdc2-related kinases

KW - leishmaniasis

KW - triazolopyridines

KW - ureas

KW - CYCLIN-DEPENDENT KINASE

KW - TRYPANOSOMA-BRUCEI

KW - 3-AMINOPYRAZOLE INHIBITORS

KW - ANTITUMOR AGENTS

KW - DISCOVERY

KW - MEXICANA

KW - DISEASES

UR - http://ukpmc.ac.uk/articles/PMC3272345

UR - http://www.scopus.com/inward/record.url?scp=82955186879&partnerID=8YFLogxK

U2 - 10.1002/cmdc.201100344

DO - 10.1002/cmdc.201100344

M1 - Article

JO - ChemMedChem

JF - ChemMedChem

SN - 1860-7179

IS - 12

VL - 6

SP - 2214

EP - 2224

ER -

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