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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.

APA

Cleghorn, L. A. T., Woodland, A., Collie, I. T., Torrie, L. S., Norcross, N., Luksch, T., Mpamhanga, C., Walker, R. G., Mottram, J. C., Brenk, R., Frearson, J. A., Gilbert, I. H., & Wyatt, P. G. (2011). Identification of Inhibitors of the Leishmania cdc2-Related Protein Kinase CRK3. ChemMedChem, 6(12), 2214-2224doi: 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.

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",
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",
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

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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