Designing selective inhibitors for calcium-dependent protein kinases in apicomplexans. (July 2015)

• Record Type: Journal Article
• Authors: Hui, Raymond; El Bakkouri, Majida; Sibley, L. David
• Is Part Of: Trends in pharmacological sciences. Volume 36:Number 7(2015)
• Page Start: 452
• Page End: 460
• Publication Date: 2015-07
• Subjects: Pharmacology -- Periodicals; Pharmacology -- trends -- Periodicals; Pharmacologie -- Périodiques; Pharmacology; Electronic journals; Periodicals; 615.1
• DOI: 10.1016/j.tips.2015.04.011
• Languages: English
• ISSNs: 0165-6147

Abstract

<abstract abstract-type="author-highlights" id="abs0005"> <title id="sect0005">Highlights</title> <sec> <p id="spar0005"> <list id="lis0005"> <list-item id="lsti0005"> <label></label> <p id="par0005">Apicomplexan parasites contain a family of plant-like calcium-dependent serine-threonine protein kinases (CDPKs) that control a variety of essential functions.</p> </list-item> <list-item id="lsti0010"> <label></label> <p id="par0010">CDPKs contain an unusual domain architecture and use a unique activation mechanism that is based on an autoinhibitory calmodulin-like domain fused to the C terminus of the kinase domain.</p> </list-item> <list-item id="lsti0015"> <label></label> <p id="par0015">Several CDPKs have been validated as potential drug targets based on genetic experiments demonstrating that they are essential for parasite growth or survival.</p> </list-item> <list-item id="lsti0020"> <label></label> <p id="par0020">Unique chemical scaffolds have been exploited to develop selective inhibitors of essential CDPKs in parasites, offering promise as new therapeutic leads.</p> </list-item> </list> </p> </sec> </abstract>