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Characterization of TAE684 as a potent LRRK2 kinase inhibitor

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Characterization of TAE684 as a potent LRRK2 kinase inhibitor. / Zhang, Jinwei; Deng, Xianming; Choi, Hwan Geun; Alessi, Dario R.; Gray, Nathanael S.

In: Bioorganic & Medicinal Chemistry Letters, Vol. 22, No. 5, 01.03.2012, p. 1864-1869.

Research output: Contribution to journalArticle

Harvard

Zhang, J, Deng, X, Choi, HG, Alessi, DR & Gray, NS 2012, 'Characterization of TAE684 as a potent LRRK2 kinase inhibitor' Bioorganic & Medicinal Chemistry Letters, vol 22, no. 5, pp. 1864-1869.

APA

Zhang, J., Deng, X., Choi, H. G., Alessi, D. R., & Gray, N. S. (2012). Characterization of TAE684 as a potent LRRK2 kinase inhibitor. Bioorganic & Medicinal Chemistry Letters, 22(5), 1864-1869doi: 10.1016/j.bmcl.2012.01.084

Vancouver

Zhang J, Deng X, Choi HG, Alessi DR, Gray NS. Characterization of TAE684 as a potent LRRK2 kinase inhibitor. Bioorganic & Medicinal Chemistry Letters. 2012 Mar 1;22(5):1864-1869.

Author

Zhang, Jinwei; Deng, Xianming; Choi, Hwan Geun; Alessi, Dario R.; Gray, Nathanael S. / Characterization of TAE684 as a potent LRRK2 kinase inhibitor.

In: Bioorganic & Medicinal Chemistry Letters, Vol. 22, No. 5, 01.03.2012, p. 1864-1869.

Research output: Contribution to journalArticle

Bibtex - Download

@article{7a78c78fae594108b3409e4848f249e6,
title = "Characterization of TAE684 as a potent LRRK2 kinase inhibitor",
author = "Jinwei Zhang and Xianming Deng and Choi, {Hwan Geun} and Alessi, {Dario R.} and Gray, {Nathanael S.}",
year = "2012",
volume = "22",
number = "5",
pages = "1864--1869",
journal = "Bioorganic & Medicinal Chemistry Letters",
issn = "0960-894X",

}

RIS (suitable for import to EndNote) - Download

TY - JOUR

T1 - Characterization of TAE684 as a potent LRRK2 kinase inhibitor

A1 - Zhang,Jinwei

A1 - Deng,Xianming

A1 - Choi,Hwan Geun

A1 - Alessi,Dario R.

A1 - Gray,Nathanael S.

AU - Zhang,Jinwei

AU - Deng,Xianming

AU - Choi,Hwan Geun

AU - Alessi,Dario R.

AU - Gray,Nathanael S.

PY - 2012/3/1

Y1 - 2012/3/1

N2 - <p>Leucine-rich repeat kinase 2 (LRRK2) is linked to Parkinson's disease and may represent an attractive therapeutic target. Here we report a 2,4-dianilino-5-chloro-pyrimidine, TAE684, a previously reported inhibitor of anaplastic lymphoma kinase (ALK), is also a potent inhibitor of LRRK2 kinase activity (IC50 of 7.8 nM against wild-type LRRK2, 6.1 nM against the G2019S mutant). TAE684 substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant at a concentration of 0.1-0.3 mu M in cells and in mouse spleen and kidney, but not in brain, following oral doses of 10 mg/kg. (c) 2012 Elsevier Ltd. All rights reserved.</p>

AB - <p>Leucine-rich repeat kinase 2 (LRRK2) is linked to Parkinson's disease and may represent an attractive therapeutic target. Here we report a 2,4-dianilino-5-chloro-pyrimidine, TAE684, a previously reported inhibitor of anaplastic lymphoma kinase (ALK), is also a potent inhibitor of LRRK2 kinase activity (IC50 of 7.8 nM against wild-type LRRK2, 6.1 nM against the G2019S mutant). TAE684 substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant at a concentration of 0.1-0.3 mu M in cells and in mouse spleen and kidney, but not in brain, following oral doses of 10 mg/kg. (c) 2012 Elsevier Ltd. All rights reserved.</p>

KW - Parkinson's disease

KW - LRRK2

KW - TAE684

U2 - 10.1016/j.bmcl.2012.01.084

DO - 10.1016/j.bmcl.2012.01.084

M1 - Article

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

SN - 0960-894X

IS - 5

VL - 22

SP - 1864

EP - 1869

ER -

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