Evidence map›Paper›PMID 27059784›Full record

ArticleAngewandte Chemie (International ed. in English)2016

Allosteric Optical Control of a Class B G-Protein-Coupled Receptor.

Johannes Broichhagen, Natalie R Johnston, Yorrick von Ohlen, Helena Meyer-Berg, Ben J Jones, Stephen R Bloom, Guy A Rutter, Dirk Trauner, David J Hodson

Abstract read
In one paragraph

Article in Angewandte Chemie (International ed. in English), 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.

0numbers the graph read from it
0cells of the map it votes in
18citing 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

18 citing papers in PubMed.

  1. Review
  2. Fine-tuned photochromic sulfonylureas for optical control of beta cell CaDiabetic medicine : a journal of the British Diabetic Association · 2023
    Article
  3. Review
  4. Photoswitchable Serotonins for Optical Control of the 5-HTAngewandte Chemie (International ed. in English) · 2022
    Article
  5. Review
  6. Article
  7. Review
  8. Article
  9. Article
  10. Article
  11. Review
  12. Review
  13. Article
  14. Article
  15. Article
  16. Article
  17. Review
  18. Allosteric Optical Control of a Class B G-Protein-Coupled Receptor.Angewandte Chemie (International ed. in English) · 2016
    Article
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

9 authors.

Johannes BroichhagenLMU Munich, Department of Chemistry and Center for Integrated Protein Science (CIPSM), Butenandtstrasse 5-13, 81377, Munich, Germany.ORCID 0000-0003-3084-6595
Natalie R JohnstonImperial College London, Section of Cell Biology and Functional Genomics, Division of Diabetes, Endocrinology and Metabolism, Department of Medicine, Hammersmith Hospital, Du Cane Road, London, W12 0NN, UK.
Yorrick von OhlenImperial College London, Section of Cell Biology and Functional Genomics, Division of Diabetes, Endocrinology and Metabolism, Department of Medicine, Hammersmith Hospital, Du Cane Road, London, W12 0NN, UK.
Helena Meyer-BergLMU Munich, Department of Chemistry and Center for Integrated Protein Science (CIPSM), Butenandtstrasse 5-13, 81377, Munich, Germany.ORCID 0000-0001-6435-7584
Ben J JonesImperial College London, Section of Investigative Medicine, Division of Diabetes, Endocrinology and Metabolism, UK.
Stephen R BloomImperial College London, Section of Investigative Medicine, Division of Diabetes, Endocrinology and Metabolism, UK.
Guy A RutterImperial College London, Section of Cell Biology and Functional Genomics, Division of Diabetes, Endocrinology and Metabolism, Department of Medicine, Hammersmith Hospital, Du Cane Road, London, W12 0NN, UK.
Dirk TraunerLMU Munich, Department of Chemistry and Center for Integrated Protein Science (CIPSM), Butenandtstrasse 5-13, 81377, Munich, Germany. dirk.trauner@lmu.de.
David J HodsonImperial College London, Section of Cell Biology and Functional Genomics, Division of Diabetes, Endocrinology and Metabolism, Department of Medicine, Hammersmith Hospital, Du Cane Road, London, W12 0NN, UK. d.hodson@imperial.ac.uk, d.hodson@bham.ac.uk.ORCID 0000-0002-8641-8568

Funding

Biotechnology and Biological Sciences Research CouncilEuropean Research Council 268795Medical Research Council MC_PC_14100Medical Research Council MR/J0003042/1Medical Research Council MR/K023667/1Medical Research Council MR/N00275X/1Wellcome TrustWellcome Trust WT098424AIA
6 · The paper itself

Abstract

Allosteric regulation promises to open up new therapeutic avenues by increasing drug specificity at G-protein-coupled receptors (GPCRs). However, drug discovery efforts are at present hampered by an inability to precisely control the allosteric site. Herein, we describe the design, synthesis, and testing of PhotoETP, a light-activated positive allosteric modulator of the glucagon-like peptide-1 receptor (GLP-1R), a class B GPCR involved in the maintenance of glucose homeostasis in humans. PhotoETP potentiates Ca(2+) , cAMP, and insulin responses to glucagon-like peptide-1 and its metabolites following illumination of cells with blue light. PhotoETP thus provides a blueprint for the production of small-molecule class B GPCR allosteric photoswitches, and may represent a useful tool for understanding positive cooperativity at the GLP-1R.

Indexed as

Allosteric RegulationAniline CompoundsAnimalsAzo CompoundsCalciumCell SurvivalCHO CellsCricetinaeCricetulusCyclic AMPGlucagon-Like Peptide-1 ReceptorHumansInsulinIsomerismLightPyrimidines4-(3-(benzyloxy)phenyl)-2-(ethylsulfinyl)-6-(trifluoromethyl)pyrimidineAniline CompoundsazobenzeneAzo CompoundsCalciumCyclic AMPGlucagon-Like Peptide-1 ReceptorInsulinPhotoETPPyrimidinesallosteric regulationbeta cellsGLP-1 receptorphotopharmacologytype 2 diabetes

Identifiers

PMID27059784
PMCPMC5031193

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.