ReviewhLife2024
Exploring structure-based drug discovery of GPCRs beyond the orthosteric binding site.
Review in hLife, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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
0 citing papers in PubMed.
No citing paper in PubMed yet.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
4 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
G-protein coupled receptors (GPCRs) are the largest family of druggable targets. In recent years, GPCR structural biology has made great advances, revealing the three-dimensional structures of many GPCRs and their interactions with ligands, proteins, and membrane components, which also have inspired a surge of structure-based drug discovery campaigns. This article provides a comprehensive summary of the currently available structural insights into the allosteric pockets of GPCRs and their regulatory mechanisms governing GPCR conformational changes. Furthermore, this article also presents several structure-inspired studies that utilize both orthosteric and allosteric modulation to discover small molecular modulators targeting GPCRs. The article emphasizes the promising potential of drug discovery targeting GPCR allosteric sites, while acknowledging the challenges arising from the limited structural information regarding the lipids and cholesterols in the membrane. Finally, the article discusses the future prospects of using large-scale or focused compound libraries to discover novel chemotypes, as well as the application of artificial intelligence (AI) in structure-based virtual screening (SBVS) against GPCRs.
Indexed as
Identifiers
What 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.