Protein kinase Calpha: disease regulator and therapeutic target

Protein kinase Calpha (PKCalpha) is a member of the AGC (which includes PKD, PKG and PKC) family of serine/threonine protein kinases that is widely expressed in mammalian tissues. It is closely related in structure, function and regulation to other members of the protein kinase C family, but has spe...

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Bibliographic Details
Published in:Trends in pharmacological sciences (Regular ed.) 2010-01, Vol.31 (1), p.8-14
Main Authors: Konopatskaya, Olga, Poole, Alastair W
Format: Article
Language:English
Subjects:
Animals
Cardiovascular Diseases - drug therapy
Cardiovascular Diseases - physiopathology
Disease Models, Animal
Drug Delivery Systems
Humans
Mice
Mice, Knockout
Neoplasms - drug therapy
Neoplasms - physiopathology
Protein Kinase C-alpha - drug effects
Protein Kinase C-alpha - metabolism
Thrombosis - drug therapy
Thrombosis - physiopathology
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Summary:Protein kinase Calpha (PKCalpha) is a member of the AGC (which includes PKD, PKG and PKC) family of serine/threonine protein kinases that is widely expressed in mammalian tissues. It is closely related in structure, function and regulation to other members of the protein kinase C family, but has specific functions within the tissues in which it is expressed. There is substantial recent evidence, from gene knockout studies in particular, that PKCalpha activity regulates cardiac contractility, atherogenesis, cancer and arterial thrombosis. Selective targeting of PKCalpha therefore has potential therapeutic value in a wide variety of disease states, although will be technically complicated by the ubiquitous expression and multiple functions of the molecule.
ISSN:1873-3735
DOI:10.1016/j.tips.2009.10.006