Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
5
pubmed:dateCreated
1990-5-31
pubmed:abstractText
The molecular basis of ligand binding selectivity to beta-adrenergic receptor subtypes was investigated by designing chimeric beta 1/beta 2-adrenergic receptors. These molecules consisted of a set of reciprocal constructions, obtained by the exchange between the wild-type receptor genes of one to three unmodified transmembrane regions, together with their extracellular flanking regions. Eight different chimeras were expressed in Escherichia coli and studied with selective beta-adrenergic ligands. The evaluation of the relative effect of each chimeric exchange on ligand binding affinity was based on the analysis of delta G values, calculated from the equilibrium binding constants, as a function of the number of substituted beta 2-adrenergic receptor transmembrane domains. The data showed that the contribution of each exchanged region to subtype selectivity varies with each ligand; moreover, while several regions are critical for the pharmacological selectivity of all ligands, others are involved in the selectivity of only some compounds. The selectivity displayed by beta-adrenergic compounds towards beta 1 or beta 2 receptor subtypes thus results from a particular combination of interactions between each ligand and each of the subsites, variably distributed over the seven transmembrane regions of the receptor; these subsites are presumably defined by the individual structural properties of the ligands.
pubmed:commentsCorrections
http://linkedlifedata.com/resource/pubmed/commentcorrection/1970295-1161000, http://linkedlifedata.com/resource/pubmed/commentcorrection/1970295-2431904, http://linkedlifedata.com/resource/pubmed/commentcorrection/1970295-2474546, http://linkedlifedata.com/resource/pubmed/commentcorrection/1970295-2536189, http://linkedlifedata.com/resource/pubmed/commentcorrection/1970295-2542304, http://linkedlifedata.com/resource/pubmed/commentcorrection/1970295-2580220, http://linkedlifedata.com/resource/pubmed/commentcorrection/1970295-2821000, http://linkedlifedata.com/resource/pubmed/commentcorrection/1970295-2823249, http://linkedlifedata.com/resource/pubmed/commentcorrection/1970295-2825170, http://linkedlifedata.com/resource/pubmed/commentcorrection/1970295-2828022, http://linkedlifedata.com/resource/pubmed/commentcorrection/1970295-2831218, http://linkedlifedata.com/resource/pubmed/commentcorrection/1970295-2836401, http://linkedlifedata.com/resource/pubmed/commentcorrection/1970295-2837273, http://linkedlifedata.com/resource/pubmed/commentcorrection/1970295-2840663, http://linkedlifedata.com/resource/pubmed/commentcorrection/1970295-2841758, http://linkedlifedata.com/resource/pubmed/commentcorrection/1970295-2845411, http://linkedlifedata.com/resource/pubmed/commentcorrection/1970295-2846532, http://linkedlifedata.com/resource/pubmed/commentcorrection/1970295-2849109, http://linkedlifedata.com/resource/pubmed/commentcorrection/1970295-2881211, http://linkedlifedata.com/resource/pubmed/commentcorrection/1970295-2885836, http://linkedlifedata.com/resource/pubmed/commentcorrection/1970295-2890637, http://linkedlifedata.com/resource/pubmed/commentcorrection/1970295-2899076, http://linkedlifedata.com/resource/pubmed/commentcorrection/1970295-2948499, http://linkedlifedata.com/resource/pubmed/commentcorrection/1970295-2985470, http://linkedlifedata.com/resource/pubmed/commentcorrection/1970295-3010132, http://linkedlifedata.com/resource/pubmed/commentcorrection/1970295-3025863, http://linkedlifedata.com/resource/pubmed/commentcorrection/1970295-3027509, http://linkedlifedata.com/resource/pubmed/commentcorrection/1970295-3128532, http://linkedlifedata.com/resource/pubmed/commentcorrection/1970295-39246, http://linkedlifedata.com/resource/pubmed/commentcorrection/1970295-4202581
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
May
pubmed:issn
0261-4189
pubmed:author
pubmed:issnType
Print
pubmed:volume
9
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
1471-6
pubmed:dateRevised
2009-11-18
pubmed:meshHeading
pubmed:year
1990
pubmed:articleTitle
Selective binding of ligands to beta 1, beta 2 or chimeric beta 1/beta 2-adrenergic receptors involves multiple subsites.
pubmed:affiliation
Laboratoire de Biologie Moléculaire des Récepteurs, CNRS, Université Paris VII, Institut Pasteur, France.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't