Document Detail

Protein kinase C, an elusive therapeutic target?
MedLine Citation:
PMID:  23197040     Owner:  NLM     Status:  MEDLINE    
Protein kinase C (PKC) has been a tantalizing target for drug discovery ever since it was first identified as the receptor for the tumour promoter phorbol ester in 1982. Although initial therapeutic efforts focused on cancer, additional indications--including diabetic complications, heart failure, myocardial infarction, pain and bipolar disorder--were targeted as researchers developed a better understanding of the roles of eight conventional and novel PKC isozymes in health and disease. Unfortunately, both academic and pharmaceutical efforts have yet to result in the approval of a single new drug that specifically targets PKC. Why does PKC remain an elusive drug target? This Review provides a short account of some of the efforts, challenges and opportunities in developing PKC modulators to address unmet clinical needs.
Daria Mochly-Rosen; Kanad Das; Kevin V Grimes
Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural; Review    
Journal Detail:
Title:  Nature reviews. Drug discovery     Volume:  11     ISSN:  1474-1784     ISO Abbreviation:  Nat Rev Drug Discov     Publication Date:  2012 Dec 
Date Detail:
Created Date:  2012-11-30     Completed Date:  2013-03-20     Revised Date:  2013-09-08    
Medline Journal Info:
Nlm Unique ID:  101124171     Medline TA:  Nat Rev Drug Discov     Country:  England    
Other Details:
Languages:  eng     Pagination:  937-57     Citation Subset:  IM    
Department of Chemical and Systems Biology, Stanford University School of Medicine, Stanford, California 94305-5174, USA.
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MeSH Terms
Bipolar Disorder / drug therapy,  etiology
Clinical Trials as Topic
Diabetes Complications / drug therapy
Enzyme Activation
Heart Diseases / drug therapy,  etiology
Isoenzymes / physiology
Neoplasms / drug therapy,  etiology
Organ Transplantation
Protein Kinase C / antagonists & inhibitors*,  chemistry,  physiology
Protein Kinase Inhibitors / therapeutic use*
Grant Support
Reg. No./Substance:
0/Isoenzymes; 0/Protein Kinase Inhibitors; EC Kinase C

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

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