Discover Community Create You

Loading publication...

Noodle always counts identifier-free feature events for service operation. With your permission, Google Analytics can also estimate audience and engagement. Search text, publication identifiers, cookies, IP addresses and browser fingerprints are never included in Noodle's first-party event counters.

Privacy details

Article

Ligand function at constitutively active receptor mutants is affected by two distinct yet interacting mechanisms.

Molecular pharmacology - 1 Mar 2004

Beinborn Martin, Ren Yong, Bläker Michael, Chen Ci, Kopin Alan S

Abstract excerpt

It has been proposed that mutations that induce constitutive activity in G-protein-coupled receptors (GPCRs) concomitantly enhance the ability of partial agonists to trigger second-messenger signaling. Using the cholecystokinin type 2 receptor (CCK-2R) as a model system, we have explored whether this association applies to a diverse set of activating mutations. Consistent with established principles,...

Read the complete abstract on PubMed

Topics

Share this publication in a Topic to start or enrich a Post.

Share to COS Cells
Share to CCK gene
Share to Ligands

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to Mutation

Share to Receptors, G-Protein-Coupled

Share to Signal Transduction

Source

Identifiers

PMID: 14978254
DOI: 10.1124/mol.65.3.753

Genes

CCK

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 6 Sept 2026. Manifest publication-graph-cohort-2026-09-06.1.

Source receipt: pubmed, retrieved 6 Sept 2026.

Related research

Semantic proximity does not establish scientific evidence.

Research trail→

Click a neighbor to travelStep 1 · 12 closest

Ligand function at constitutively active receptor mutants is affected by two distinct yet interacting mechanisms.PMID 14978254Read ↗

Constitutively active G protein-coupled receptor mutants: implications on receptor function and drug action.Semantic proximity Read ↗

Lessons from constitutively active mutants of G protein-coupled receptors.Semantic proximity Read ↗

Characterization of constitutively active mutants of G protein-coupled receptors.Semantic proximity Read ↗

Ligand rescue of constitutively active mutant receptors.Semantic proximity Read ↗

Constitutive activity of G-protein-coupled receptors: cause of disease and common property of wild-type receptors.Semantic proximity Read ↗

Constitutive activation of G protein-coupled receptors and diseases: insights into mechanisms of activation and therapeutics.Semantic proximity Read ↗

Pharmacogenomic and Structural Analysis of Constitutive G Protein–Coupled Receptor ActivitySemantic proximity Read ↗

Domains for activation and inactivation in G protein-coupled receptors--a mutational analysis of constitutive activity of the adenosine A2B receptor.Semantic proximity Read ↗

Estimation of the receptor-state affinity constants of ligands in functional studies using wild type and constitutively active mutant receptors: Implications for estimation of agonist bias.Semantic proximity Read ↗

Constitutively active mutants of the alpha 2-adrenergic receptor.Semantic proximity Read ↗

The use of constitutively active receptors for drug discovery at the G protein-coupled receptor gene pool.Semantic proximity Read ↗

Computational design of constitutively active mutants of Dopamine D2 receptor inspired by ligand-independent activation mechanisms.Semantic proximity Read ↗

⌁Select a neighboring publication to make it the new centre.