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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.

APA

Choi, H. G., Zhang, J., Deng, X., Hatcher, J. M., Patricelli, M. P., Zhao, Z., Alessi, D. R., & Gray, N. S. (2012). Brain penetrant LRRK2 inhibitor. ACS Medicinal Chemistry Letters, 3(8), 658-662doi: 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.

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",
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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