Document Detail


Leucine-rich repeat kinase 2 inhibitors: a patent review (2006 - 2011).
MedLine Citation:
PMID:  23126385     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
INTRODUCTION: 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.
Authors:
Xianming Deng; Hwan Geun Choi; Sara J Buhrlage; Nathanael S Gray
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't; Review     Date:  2012-11-06
Journal Detail:
Title:  Expert opinion on therapeutic patents     Volume:  22     ISSN:  1744-7674     ISO Abbreviation:  Expert Opin Ther Pat     Publication Date:  2012 Dec 
Date Detail:
Created Date:  2012-11-20     Completed Date:  2013-05-10     Revised Date:  2013-11-06    
Medline Journal Info:
Nlm Unique ID:  9516419     Medline TA:  Expert Opin Ther Pat     Country:  England    
Other Details:
Languages:  eng     Pagination:  1415-26     Citation Subset:  IM    
Affiliation:
Xiamen University, School of Life Sciences, State Key Laboratory of Cellular Stress Biology, Fujian 361005, China. xmdeng@xmu.edu.cn
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MeSH Terms
Descriptor/Qualifier:
Animals
Antiparkinson Agents / chemistry,  pharmacology*,  therapeutic use
Drug Design*
Genetic Predisposition to Disease
Humans
Molecular Structure
Mutation
Parkinson Disease / drug therapy,  enzymology,  genetics
Patents as Topic*
Protein Conformation
Protein Kinase Inhibitors / chemistry,  pharmacology*,  therapeutic use
Protein-Serine-Threonine Kinases / antagonists & inhibitors*,  genetics,  metabolism
Structure-Activity Relationship
Grant Support
ID/Acronym/Agency:
P41 GM079575-03/GM/NIGMS NIH HHS
Chemical
Reg. No./Substance:
0/Antiparkinson Agents; 0/Protein Kinase Inhibitors; EC 2.7.11.1/LRRK2 protein, human; EC 2.7.11.1/Protein-Serine-Threonine Kinases
Comments/Corrections
Comment In:
Expert Opin Ther Pat. 2013 Feb;23(2):279   [PMID:  23268730 ]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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