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Brain penetrant LRRK2 inhibitor

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Brain penetrant LRRK2 inhibitor. / Choi, Hwan Geun; Zhang, Jinwei; Deng, Xianming; Hatcher, John M.; Patricelli, Matthew P.; Zhao, Zheng; Alessi, Dario R.; Gray, Nathanael S.

In: ACS Medicinal Chemistry Letters, Vol. 3, No. 8, 08.2012, p. 658-662.

Research output: Contribution to journalArticle

Harvard

Choi, HG, Zhang, J, Deng, X, Hatcher, JM, Patricelli, MP, Zhao, Z, Alessi, DR & Gray, NS 2012, 'Brain penetrant LRRK2 inhibitor' ACS Medicinal Chemistry Letters, vol 3, no. 8, pp. 658-662., 10.1021/ml300123a

APA

Choi, H. G., Zhang, J., Deng, X., Hatcher, J. M., Patricelli, M. P., Zhao, Z., ... Gray, N. S. (2012). Brain penetrant LRRK2 inhibitor. ACS Medicinal Chemistry Letters, 3(8), 658-662. 10.1021/ml300123a

Vancouver

Choi HG, Zhang J, Deng X, Hatcher JM, Patricelli MP, Zhao Z et al. Brain penetrant LRRK2 inhibitor. ACS Medicinal Chemistry Letters. 2012 Aug;3(8):658-662. Available from: 10.1021/ml300123a

Author

Choi, Hwan Geun; Zhang, Jinwei; Deng, Xianming; Hatcher, John M.; Patricelli, Matthew P.; Zhao, Zheng; Alessi, Dario R.; Gray, Nathanael S. / Brain penetrant LRRK2 inhibitor.

In: ACS Medicinal Chemistry Letters, Vol. 3, No. 8, 08.2012, p. 658-662.

Research output: Contribution to journalArticle

Bibtex - Download

@article{18f20864d3164839a8489e937322e5c0,
title = "Brain penetrant LRRK2 inhibitor",
author = "Choi, {Hwan Geun} and Jinwei Zhang and Xianming Deng and Hatcher, {John M.} and Patricelli, {Matthew P.} and Zheng Zhao and Alessi, {Dario R.} and Gray, {Nathanael S.}",
year = "2012",
doi = "10.1021/ml300123a",
volume = "3",
number = "8",
pages = "658--662",
journal = "ACS Medicinal Chemistry Letters",
issn = "1948-5875",

}

RIS (suitable for import to EndNote) - Download

TY - JOUR

T1 - Brain penetrant LRRK2 inhibitor

A1 - Choi,Hwan Geun

A1 - Zhang,Jinwei

A1 - Deng,Xianming

A1 - Hatcher,John M.

A1 - Patricelli,Matthew P.

A1 - Zhao,Zheng

A1 - Alessi,Dario R.

A1 - Gray,Nathanael S.

AU - Choi,Hwan Geun

AU - Zhang,Jinwei

AU - Deng,Xianming

AU - Hatcher,John M.

AU - Patricelli,Matthew P.

AU - Zhao,Zheng

AU - Alessi,Dario R.

AU - Gray,Nathanael S.

PY - 2012/8

Y1 - 2012/8

N2 - <p>Activating mutations in leucine-rich repeat kinase 2 (LARK2) are present in a subset of Parkinson's disease (PD) patients and may represent an attractive therapeutic target. Here, we report that a 2-anilino-4-methylamino-5-chloropyrimidine, HG-10-102-01 (4), is a potent and selective inhibitor of wild-type LRRK2 and the G2019S mutant. Compound 4 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 is the first compound reported to be capable of inhibiting Ser910 and Ser935 phosphorylation in mouse brain following intraperitoneal delivery of doses as low as 50 mg/kg.</p>

AB - <p>Activating mutations in leucine-rich repeat kinase 2 (LARK2) are present in a subset of Parkinson's disease (PD) patients and may represent an attractive therapeutic target. Here, we report that a 2-anilino-4-methylamino-5-chloropyrimidine, HG-10-102-01 (4), is a potent and selective inhibitor of wild-type LRRK2 and the G2019S mutant. Compound 4 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 is the first compound reported to be capable of inhibiting Ser910 and Ser935 phosphorylation in mouse brain following intraperitoneal delivery of doses as low as 50 mg/kg.</p>

U2 - 10.1021/ml300123a

DO - 10.1021/ml300123a

M1 - Article

JO - ACS Medicinal Chemistry Letters

JF - ACS Medicinal Chemistry Letters

SN - 1948-5875

IS - 8

VL - 3

SP - 658

EP - 662

ER -

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