Evidence map›Paper›PMID 20028316›Full record

ReviewCurrent pharmaceutical design2009

Rhodopsin and the others: a historical perspective on structural studies of G protein-coupled receptors.

Stefano Costanzi, Jeffrey Siegel, Irina G Tikhonova, Kenneth A Jacobson

Abstract readHistorical ArticleReview
In one paragraph

Review in Current pharmaceutical design, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.

0numbers the graph read from it
0cells of the map it votes in
25citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

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.

2 · The registry

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.

3 · Its place in the literature

Who cites it

25 citing papers in PubMed.

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  18. Homology modeling of class a G protein-coupled receptors.Methods in molecular biology (Clifton, N.J.) · 2012
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  19. Article
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4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

4 authors.

Stefano CostanziLaboratory of Biological Modeling, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, DHHS, Bethesda, MD 20892, USA. stefanoc@mail.nih.gov
Jeffrey Siegel
Irina G Tikhonova
Kenneth A Jacobson

Funding

Computer Modeling of G Protein-Coupled ReceptorsZIADK031126 · NIDDK · NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES · PI JACOBSON, KENNETH ALAN · 2009 to 2025
$6.6M
Molecular modeling of G protein-coupled receptorsZIADK013025 · NIDDK · NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES · PI SHERMAN, ARTHUR · 2009 to 2012
$1.2M
Molecular modeling of G protein-coupled receptorsZ01DK013025 · NIDDK · NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES · PI SHERMAN, ARTHUR · 2007 to 2008
$742k
Intramural NIH HHS Z01 DK013025
6 · The paper itself

Abstract

The role of rhodopsin as a structural prototype for the study of the whole superfamily of G protein-coupled receptors (GPCRs) is reviewed in an historical perspective. Discovered at the end of the nineteenth century, fully sequenced since the early 1980s, and with direct three-dimensional information available since the 1990s, rhodopsin has served as a platform to gather indirect information on the structure of the other superfamily members. Recent breakthroughs have elicited the solution of the structures of additional receptors, namely the beta(1)- and beta(2)-adrenergic receptors and the A(2A) adenosine receptor, now providing an opportunity to gauge the accuracy of homology modeling and molecular docking techniques and to perfect the computational protocol. Notably, in coordination with the solution of the structure of the A(2A) adenosine receptor, the first "critical assessment of GPCR structural modeling and docking" has been organized, the results of which highlighted that the construction of accurate models, although challenging, is certainly achievable. The docking of the ligands and the scoring of the poses clearly emerged as the most difficult components. A further goal in the field is certainly to derive the structure of receptors in their signaling state, possibly in complex with agonists. These advances, coupled with the introduction of more sophisticated modeling algorithms and the increase in computer power, raise the expectation for a substantial boost of the robustness and accuracy of computer-aided drug discovery techniques in the coming years.

Indexed as

Drug DesignModels, MolecularAnimalsCattleComputer-Aided DesignHistory, 20th CenturyHumansLigandsReceptor, Adenosine A2AReceptors, Adrenergic, beta-1Receptors, Adrenergic, beta-2RhodopsinLigandsReceptor, Adenosine A2AReceptors, Adrenergic, beta-1Receptors, Adrenergic, beta-2Rhodopsin

Identifiers

PMID20028316
PMCPMC2801150

What OpenQuestion holds

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Registered trials

None linked

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.