Matches in SemOpenAlex for { <https://semopenalex.org/work/W66574992> ?p ?o ?g. }
Showing items 1 to 70 of
70
with 100 items per page.
- W66574992 abstract "Allosteric modulators of adenosine A1 receptors are potentially novel therapeutic agents; however, their mode of interaction with the receptor remains largely unknown. Two previously-described A1 modulators, SCH-202676 and LUF-5484, both contain a sulfur atom within their structure, leading to the hypothesis that their mode of binding may involve interaction with one or more cysteine residues within the receptor. In radioligand binding assays, SCH-202676 significantly reduced the dissociation rate of the antagonist, [3H]DPCPX, from CHO-A1 membranes, suggestive of an allosteric change in receptor conformation. A similar effect was noted for LUF-5484 on the dissociation rate of the agonist, [3H] CCPA. In functional assays, SCH-202676 acted as an inhibitor of R-PIA-mediated ERK1/2 phosphorylation, while LUF-5484 enhanced the potency of R-PIA in a manner quantitatively consistent with the predictions of a simple allosteric receptor model. When both binding and functional experiments were repeated in the presence of the disulfide reducing agent, dithiothreitol (10 mM), the effects of SCH-202676 were abolished, but not those of LUF-5484. These results support the hypothesis that SCH-202676 is a non-specific modulator of GPCRs that interacts with receptor sulfhydryl groups. In contrast, LUF-5484 is a specific A1 receptor enhancer that does not necessarily utilize cysteine residues for its interaction with the receptor's allosteric site." @default.
- W66574992 created "2016-06-24" @default.
- W66574992 creator A5016689951 @default.
- W66574992 creator A5036022995 @default.
- W66574992 creator A5075463548 @default.
- W66574992 creator A5077280255 @default.
- W66574992 date "2006-03-01" @default.
- W66574992 modified "2023-09-23" @default.
- W66574992 title "Divergent mechanisms for allosteric modulators of adenosine A1 receptors" @default.
- W66574992 doi "https://doi.org/10.1096/fasebj.20.5.a1119" @default.
- W66574992 hasPublicationYear "2006" @default.
- W66574992 type Work @default.
- W66574992 sameAs 66574992 @default.
- W66574992 citedByCount "1" @default.
- W66574992 crossrefType "journal-article" @default.
- W66574992 hasAuthorship W66574992A5016689951 @default.
- W66574992 hasAuthorship W66574992A5036022995 @default.
- W66574992 hasAuthorship W66574992A5075463548 @default.
- W66574992 hasAuthorship W66574992A5077280255 @default.
- W66574992 hasConcept C109964505 @default.
- W66574992 hasConcept C12554922 @default.
- W66574992 hasConcept C135285700 @default.
- W66574992 hasConcept C166342909 @default.
- W66574992 hasConcept C170493617 @default.
- W66574992 hasConcept C181199279 @default.
- W66574992 hasConcept C182683403 @default.
- W66574992 hasConcept C185592680 @default.
- W66574992 hasConcept C2776038425 @default.
- W66574992 hasConcept C2778938600 @default.
- W66574992 hasConcept C2779201268 @default.
- W66574992 hasConcept C55493867 @default.
- W66574992 hasConcept C67907053 @default.
- W66574992 hasConcept C71240020 @default.
- W66574992 hasConcept C86803240 @default.
- W66574992 hasConcept C98274493 @default.
- W66574992 hasConceptScore W66574992C109964505 @default.
- W66574992 hasConceptScore W66574992C12554922 @default.
- W66574992 hasConceptScore W66574992C135285700 @default.
- W66574992 hasConceptScore W66574992C166342909 @default.
- W66574992 hasConceptScore W66574992C170493617 @default.
- W66574992 hasConceptScore W66574992C181199279 @default.
- W66574992 hasConceptScore W66574992C182683403 @default.
- W66574992 hasConceptScore W66574992C185592680 @default.
- W66574992 hasConceptScore W66574992C2776038425 @default.
- W66574992 hasConceptScore W66574992C2778938600 @default.
- W66574992 hasConceptScore W66574992C2779201268 @default.
- W66574992 hasConceptScore W66574992C55493867 @default.
- W66574992 hasConceptScore W66574992C67907053 @default.
- W66574992 hasConceptScore W66574992C71240020 @default.
- W66574992 hasConceptScore W66574992C86803240 @default.
- W66574992 hasConceptScore W66574992C98274493 @default.
- W66574992 hasIssue "5" @default.
- W66574992 hasLocation W665749921 @default.
- W66574992 hasOpenAccess W66574992 @default.
- W66574992 hasPrimaryLocation W665749921 @default.
- W66574992 hasRelatedWork W2000749144 @default.
- W66574992 hasRelatedWork W2001643841 @default.
- W66574992 hasRelatedWork W2073648757 @default.
- W66574992 hasRelatedWork W2153758876 @default.
- W66574992 hasRelatedWork W2272684044 @default.
- W66574992 hasRelatedWork W2908579861 @default.
- W66574992 hasRelatedWork W3142688211 @default.
- W66574992 hasRelatedWork W4210809282 @default.
- W66574992 hasRelatedWork W4225319437 @default.
- W66574992 hasRelatedWork W66574992 @default.
- W66574992 hasVolume "20" @default.
- W66574992 isParatext "false" @default.
- W66574992 isRetracted "false" @default.
- W66574992 magId "66574992" @default.
- W66574992 workType "article" @default.