ArticleDrug development research1996
Molecular Architecture of G Protein-Coupled Receptors.
Article in Drug development research, 1996. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 50 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
50 citing papers in PubMed, 178 citations in OpenAlex.
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- Purinergic GPCR transmembrane residues involved in ligand recognition and dimerization.Methods in cell biology · 2021Review
- Crystal structure of dopamine receptor D4 bound to the subtype selective ligand, L745870.eLife · 2019Article
- Dopamine DJournal of medicinal chemistry · 2019Article
- Detecting Cell Surface Expression of the G Protein-Coupled Receptor CXCR4.Methods in molecular biology (Clifton, N.J.) · 2018Article
- Chemokines and their receptors: insights from molecular modeling and crystallography.Current opinion in pharmacology · 2016Review
- Integrating structural and mutagenesis data to elucidate GPCR ligand binding.Current opinion in pharmacology · 2016Review
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- DIRECT-ID: An automated method to identify and quantify conformational variations--application to β2 -adrenergic GPCR.Journal of computational chemistry · 2016Article
- Examining the critical roles of human CB2 receptor residues Valine 3.32 (113) and Leucine 5.41 (192) in ligand recognition and downstream signaling activities.Biochemical and biophysical research communications · 2014Article
- Molecular pharmacology and ligand docking studies reveal a single amino acid difference between mouse and human serotonin 5-HT2A receptors that impacts behavioral translation of novel 4-phenyl-2-dimethylaminotetralin ligands.The Journal of pharmacology and experimental therapeutics · 2013Article
- Quantitative Analysis of Guanine Nucleotide Exchange Factors (GEFs) as Enzymes.Cellular logistics · 2013Article
- Nucleotide exchange factors: Kinetic analyses and the rationale for studying kinetics of GEFs.Cellular logistics · 2012Article
- In silico screening for agonists and blockers of the β(2) adrenergic receptor: implications of inactive and activated state structures.Journal of computational chemistry · 2012Article
- Homology modeling of class a G protein-coupled receptors.Methods in molecular biology (Clifton, N.J.) · 2012Article
- Pyrimidine nucleotides with 4-alkyloxyimino and terminal tetraphosphate δ-ester modifications as selective agonists of the P2Y(4) receptor.Journal of medicinal chemistry · 2011Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
2 authors at 1 institution in 1 country.
Funding
Abstract
This review of the current literature on mutations in G protein-coupled receptors (GPCRs) of the rhodopsin-related family intends to draw inferences from amino acid sequences for single receptors and multiple sequence alignments with regard to the molecular architecture of this class of receptors. For this purpose a comprehensive list of mutations within the transmembrane helical regions (TMs; over 390 mutations from 38 different receptor subtypes) and their effects on function was compiled, and an alignment of known GPCR sequences (over 150 separate sequences) was made. Regions most prominently involved in ligand binding are located in TMs 3, 5, 6, and 7. Position 3.32 in TM3 is occupied by a D in all biogenic amine receptors (sequence conservation) but may be occupied by uncharged residues in other receptors while its role in ligand binding is analogous (function conservation). TMs 5, 6, and 7 display considerable sequence conservation throughout the majority of GPCRs investigated, but not necessarily at those positions involved in ligand binding. However, considerable function conservation is observed for positions 5.42 (frequently hydrophilic), 5.46 (small amino acids required for agonist binding to "small ligand" receptors), 6.52 and 7.39 (high variability), and 7.43 (frequently aromatic). A general conclusion of this review is that there is overwhelming conservation of structure-function correlates among GPCRs. Thus, it is now possible to cross-correlate the results of mutagenesis studies between GPCRs of different subfamilies, and to use those results to predict the function of specific residues in new GPCR sequences.
Identifiers
21921973PMC3171971W2114935719What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.