ReviewCurrent opinion in drug discovery & development2010
Orthosteric- and allosteric-induced ligand-directed trafficking at GPCRs.
Review in Current opinion in drug discovery & development, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 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
22 citing papers in PubMed, 32 citations in OpenAlex.
- Review
- Allosteric modulation of Plasmodium falciparum Isoleucyl tRNA synthetase by South African natural compounds.PloS one · 2025Article
- Proteomic Profiling of Serum Extracellular Vesicles Identifies Diagnostic Signatures and Therapeutic Targets in Breast Cancer.Cancer research · 2024Article
- Allosteric activation of the metabolic enzyme GPD1 inhibits bladder cancer growth via the lysoPC-PAFR-TRPV2 axis.Journal of hematology & oncology · 2022Article
- QR code model: a new possibility for GPCR phosphorylation recognition.Cell communication and signaling : CCS · 2022Review
- Covalent allosteric modulation: An emerging strategy for GPCRs drug discovery.European journal of medicinal chemistry · 2020Review
- Identification of Selective Novel Hits againstInternational journal of molecular sciences · 2020Article
- Studying biomolecular folding and binding using temperature-jump mass spectrometry.Nature communications · 2020Article
- Integrated In Silico Fragment-Based Drug Design: Case Study with Allosteric Modulators on Metabotropic Glutamate Receptor 5.The AAPS journal · 2017Article
- Review
- Opportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disorders.Nature reviews. Drug discovery · 2014Review
- Drugs for allosteric sites on receptors.Annual review of pharmacology and toxicology · 2014Review
- Approaches for probing allosteric interactions at 7 transmembrane spanning receptors.Progress in molecular biology and translational science · 2013Review
- Biasing the prostaglandin F2α receptor responses toward EGFR-dependent transactivation of MAPK.Molecular endocrinology (Baltimore, Md.) · 2012Article
- Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery.Journal of medicinal chemistry · 2012Article
- The different ways through which specificity works in orthosteric and allosteric drugs.Current pharmaceutical design · 2012Article
- Muscarinic and nicotinic acetylcholine receptor agonists and allosteric modulators for the treatment of schizophrenia.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2012Review
- Allo-network drugs: harnessing allostery in cellular networks.Trends in pharmacological sciences · 2011Article
- Recent progress on the identification of metabotropic glutamate 4 receptor ligands and their potential utility as CNS therapeutics.ACS chemical neuroscience · 2011Review
- Discovery and optimization of a novel, selective and brain penetrant M1 positive allosteric modulator (PAM): the development of ML169, an MLPCN probe.Bioorganic & medicinal chemistry letters · 2011Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
Many orthosteric agonists differentially activate downstream effectors of GPCRs. Such defined induction of signaling has strongly supported the hypothesis termed 'ligand-directed trafficking of receptor signaling' (LDTRS). More recently, subtype-selective GPCR activators, such as allosteric agonists and positive allosteric modulators, have also exhibited the capacity to activate specific signaling pathways. Based on this finding, it may be possible to achieve ligand-specific receptor active states that optimize the biological responses specific to GPCRs. This review discusses recent studies in which both orthosteric and allosteric compounds have been demonstrated to induce LDTRS.
Indexed as
Identifiers
20812150PMC3821179W2414895801What 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.