Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2
pubmed:dateCreated
2010-3-10
pubmed:abstractText
In addition to the key role of thrombin in blood coagulation, this multifunctional serine protease activates platelets and regulates the behavior of other cells through G-protein coupled protease activated receptors (PARs). PAR-1 is the principal thrombin-activated receptor involved in platelet aggregation and in endothelial and tumor cell proliferation. PAR-1 is overexpressed in invasive and metastatic tumors and the expression levels directly correlate with the degree of invasiveness of the cancer. In an attempt to give some insight into the perspectives of targeting PAR-1 in cancer and angiogenesis, this review provides an overview on the thrombin/PAR-1 interaction, receptor activation, signaling, desensitization and dysregulation mechanisms in relation to these diseases. A central aspect of this review is that directed to summarize the approaches that have been followed to the search of PAR-1 antagonists, illustrating with some significant examples. Attention is called to the scarce data concerning the effects of these antagonists on anticancer assay models.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:issn
1875-533X
pubmed:author
pubmed:issnType
Electronic
pubmed:volume
17
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
109-28
pubmed:dateRevised
2010-9-28
pubmed:meshHeading
pubmed:year
2010
pubmed:articleTitle
Thrombin-activated receptors: promising targets for cancer therapy?
pubmed:affiliation
Instituto de Química Médica, Juan de la Cierva 3, E-28006 Madrid, Spain.
pubmed:publicationType
Journal Article, Review, Research Support, Non-U.S. Gov't