Linked Life Data

15992776

Source:http://linkedlifedata.com/resource/pubmed/id/15992776

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
1
pubmed:dateCreated
2005-7-15
pubmed:abstractText
We have developed an inducible HEK293/Tet-On cell line that transiently expresses both FLAG-tagged human angiotensin II type-I receptors (FLAG-hAT(1)R) and G(q)alpha G protein subunits in response to doxycycline. High and tightly regulated levels of FLAG-hAT(1)R (740+/-57 fmol/mg protein) and G(q)alpha (36-fold increase compared with non-induced cells) overexpression were consistently achieved. We investigated the possibility of using an inducible system to increase the proportion of constitutively active wild-type FLAG-hAT(1)Rs by overexpressing G(q)alpha. Following doxycycline treatment, we observed no significant change in the apparent binding affinity or potency (coupling efficiency) of angiotensin II, though significant increases in the intrinsic activity of several partial agonists were observed, indicative of constitutive activity. DUP753 (10 microM), a suggested inverse agonist, did not inhibit the enhanced level of basal (agonist-independent) activity. The data suggest that the resting equilibrium of hAT(1) receptors between the inactive (R) and active (R*) forms is predominantly weighted towards the inactive conformation.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Aug
pubmed:issn
0006-291X
pubmed:author
pubmed:issnType
Print
pubmed:day
19
pubmed:volume
334
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
134-9
pubmed:dateRevised
2009-11-19
pubmed:meshHeading
pubmed:year
2005
pubmed:articleTitle
Constitutive activity of human angiotensin II type-1 receptors by Gq overexpression.
pubmed:affiliation
CRISTAL (Cardiovascular Research Institute at Leeds), School of Medicine, University of Leeds, Leeds LS2 9JT, UK. J.Scragg@leeds.ac.uk
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't