ArticleJournal of medicinal chemistry2008
Modulating G-protein coupled receptor/G-protein signal transduction by small molecules suggested by virtual screening.
Article in Journal of medicinal chemistry, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 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
10 citing papers in PubMed, 23 citations in OpenAlex.
- The Retinoid and Non-Retinoid Ligands of the Rod Visual G Protein-Coupled Receptor.International journal of molecular sciences · 2019Review
- Intracellular Receptor Modulation: Novel Approach to Target GPCRs.Trends in pharmacological sciences · 2018Review
- Tauroursodeoxycholic acid binds to the G-protein site on light activated rhodopsin.Experimental eye research · 2018Article
- PubChem structure-activity relationship (SAR) clusters.Journal of cheminformatics · 2015Article
- The receptor concept in 3D: from hypothesis and metaphor to GPCR-ligand structures.Neurochemical research · 2014Review
- Inhibition of bacterial virulence: drug-like molecules targeting the Salmonella enterica PhoP response regulator.Chemical biology & drug design · 2012Article
- The cytoplasmic rhodopsin-protein interface: potential for drug discovery.Current drug targets · 2012Review
- Allosteric Modulation of G Protein Coupled Receptors by Cytoplasmic, Transmembrane and Extracellular Ligands.Pharmaceuticals (Basel, Switzerland) · 2010Article
- Using ligand-based virtual screening to allosterically stabilize the activated state of a GPCR.Chemical biology & drug design · 2010Article
- Recent advances in structure-based virtual screening of G-protein coupled receptors.The AAPS journal · 2009Review
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 at 2 institutions in 1 country.
Funding
Abstract
Modulation of interactions between activated GPCRs (G-protein coupled receptors) and the intracellular (IC) signal transducers, heterotrimeric G-proteins, is an attractive, yet essentially unexplored, paradigm for treatment of certain diseases. Regulating downstream signaling for treatment of congenital diseases due to constitutively active GPCRs, as well as tumors where GPCRs are often overexpressed, requires the development of new methodologies. Modeling, experimental data, docking, scoring, and experimental testing (MEDSET) was developed to discover inhibitors that target the IC loops of activated GPCRs. As proof-of-concept, MEDSET developed and utilized a model of the interface between photoactivated rhodopsin (R*) and transducin (Gt), its G-protein. A National Cancer Institute (NCI) compound library was screened to identify compounds that bound at the interface between R* and its G-protein. High-scoring compounds from this virtual screen were obtained and tested experimentally for their ability to stabilize R* and prevent Gt from binding to R*. Several compounds that modulate signal transduction have been identified.
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.