Evidence map›Paper›PMID 34223156›Full record

ReviewRSC medicinal chemistry2021

Comprehensive overview of biased pharmacology at the opioid receptors: biased ligands and bias factors.

Jolien De Neve, Thomas M A Barlow, Dirk Tourwé, Frédéric Bihel, Frédéric Simonin, Steven Ballet

Abstract readReview
In one paragraph

Review in RSC medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.

0numbers the graph read from it
0cells of the map it votes in
19citing 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

19 citing papers in PubMed.

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  9. Design, Synthesis, andACS pharmacology & translational science · 2024
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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

6 authors.

Jolien De NeveResearch Group of Organic Chemistry, Departments of Chemistry and Bioengineering Sciences, Vrije Universiteit Brussel Brussels Belgium steven.ballet@vub.be.ORCID https://orcid.org/0000-0002-8059-646X
Thomas M A BarlowResearch Group of Organic Chemistry, Departments of Chemistry and Bioengineering Sciences, Vrije Universiteit Brussel Brussels Belgium steven.ballet@vub.be.ORCID https://orcid.org/0000-0003-0763-7277
Dirk TourwéResearch Group of Organic Chemistry, Departments of Chemistry and Bioengineering Sciences, Vrije Universiteit Brussel Brussels Belgium steven.ballet@vub.be.ORCID https://orcid.org/0000-0002-2329-0798
Frédéric BihelLaboratoire d'Innovation Thérapeutique, Faculté de Pharmacie, UMR 7200, CNRS Université de Strasbourg Illkirch France.ORCID https://orcid.org/0000-0002-4122-0929
Frédéric SimoninBiotechnologie et Signalisation Cellulaire, UMR 7242, CNRS, Université de Strasbourg Illkirch France.ORCID https://orcid.org/0000-0003-2852-0860
Steven BalletResearch Group of Organic Chemistry, Departments of Chemistry and Bioengineering Sciences, Vrije Universiteit Brussel Brussels Belgium steven.ballet@vub.be.ORCID https://orcid.org/0000-0003-4123-1641

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

One of the main challenges in contemporary medicinal chemistry is the development of safer analgesics, used in the treatment of pain. Currently, moderate to severe pain is still treated with the "gold standard" opioids whose long-term often leads to severe side effects. With the discovery of biased agonism, the importance of this area of pharmacology has grown exponentially over the past decade. Of these side effects, tolerance, opioid misuse, physical dependence and substance use disorder (SUD) stand out, since these have led to many deaths over the past decades in both USA and Europe. New therapeutic molecules that induce a biased response at the opioid receptors (MOR, DOR, KOR and NOP receptor) are able to circumvent these side effects and, consequently, serve as more advantageous therapies with great promise. The concept of biased signaling extends far beyond the already sizeable field of GPCR pharmacology and covering everything would be vastly outside the scope of this review which consequently covers the biased ligands acting at the opioid family of receptors. The limitation of quantifying bias, however, makes this a controversial subject, where it is dependent on the reference ligand, the equation or the assay used for the quantification. Hence, the major issue in the field of biased ligands remains the translation of the

Identifiers

PMID34223156
PMCPMC8221262

What OpenQuestion holds

Textmetadata
Read underepoch 390

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.