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dc.contributor.authorDeng, Xianmingzh_CN
dc.contributor.authorChoi, Hwan Geunzh_CN
dc.contributor.authorBuhrlage, Sara J.zh_CN
dc.contributor.authorGray, Nathanael S.zh_CN
dc.contributor.author邓贤明zh_CN
dc.date.accessioned2015-07-22T07:13:36Z
dc.date.available2015-07-22T07:13:36Z
dc.date.issued2012-12zh_CN
dc.identifier.citationEXPERT OPINION ON THERAPEUTIC PATENTS, 2012,22(12):1415-1426zh_CN
dc.identifier.otherWOS:000311420400003zh_CN
dc.identifier.urihttps://dspace.xmu.edu.cn/handle/2288/90459
dc.descriptionNIH [P41 GM079575-03]; Michael J Fox foundation for Parkinson's disease research; Fundamental Research Funds for the Central Universities of China [2011121030]; 111 Project of Education of China [B06016]zh_CN
dc.description.abstractIntroduction: Leucine-rich repeat kinase 2 (LRRK2) has received considerable attention since the discovery of LRRK2 mutations in families with dominantly inherited Parkinson's disease (PD) in 2004. The missense mutation G2019S is the most common LRRK2 mutation and has been identified in both familial and sporadic PD cases. The G2019S mutation enhances kinase activity suggesting that LRRK2 could be an attractive therapeutic target for PD and small-molecule ATP-competitive LRRK2 kinase inhibitors are one way to investigate this possibility. Areas covered: Currently, LRRK2 kinase inhibitors are being actively pursued by industry and academia. Herein, patents detailing the discovery of LRRK2 kinase inhibitors from 2006 through 2011 and the corresponding publications from 2006 through July of 2012 are summarized. Expert opinion: Wild-type and mutant forms of LRRK2 are currently being actively pursued as therapeutic targets for the potential treatment of PD. The increasing number of patent applications being filed for inhibitors of LRRK2 is a testament to this activity. Numerous distinct chemo-types have been reported as LRRK2 inhibitors with some demonstrating exceptional potency and selectivity for LRRK2 relative to other kinases. These compounds are being used as pharmacological 'tools' to elucidate the physiological and pathophysiological function of LRRK2 and it appears likely that some will be investigated for their potential therapeutic effects for the treatment of PD.zh_CN
dc.language.isoen_USzh_CN
dc.publisherEXPERT OPIN THER PATzh_CN
dc.source.urihttp://dx.doi.org/10.1517/13543776.2012.729041zh_CN
dc.subjectDISEASE-ASSOCIATED MUTATIONSzh_CN
dc.subjectPARKINSONS-DISEASEzh_CN
dc.subjectCYTOPLASMIC LOCALIZATIONzh_CN
dc.subjectANGIOGENESIS INHIBITORzh_CN
dc.subject14-3-3 BINDINGzh_CN
dc.subjectPHASE-Izh_CN
dc.subjectLRRK2zh_CN
dc.subjectPOTENTzh_CN
dc.subjectSELECTIVITYzh_CN
dc.subjectDISCOVERYzh_CN
dc.titleLeucine-rich repeat kinase 2 inhibitors: a patent review (2006-2011)zh_CN
dc.typeArticlezh_CN


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