ReviewMethods in molecular biology (Clifton, N.J.)2011
Pharmacology, biodistribution, and efficacy of GPCR-based pepducins in disease models.
Review in Methods in molecular biology (Clifton, N.J.), 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 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
24 citing papers in PubMed, 82 citations in OpenAlex.
- Cancer-Targeting Applications of Cell-Penetrating Peptides.International journal of molecular sciences · 2024Review
- Pepducin ICL1-9-Mediated β2-Adrenergic Receptor-Dependent Cardiomyocyte Contractility Occurs in a GCardiovascular drugs and therapy · 2023Article
- Intrinsically disordered proteins and proteins with intrinsically disordered regions in neurodegenerative diseases.Biophysical reviews · 2022Review
- GPCRs: The most promiscuous druggable receptor of the mankind.Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society · 2021Review
- CB1 cannabinoid receptor-phosphorylated fourth intracellular loop structure-function relationships.Peptide science (Hoboken, N.J.) · 2019Article
- Magi-1 scaffolds NaFASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2019Article
- Internalized GPCRs as Potential Therapeutic Targets for the Management of Pain.Frontiers in molecular neuroscience · 2019Article
- Emerging Paradigm of Intracellular Targeting of G Protein-Coupled Receptors.Trends in biochemical sciences · 2018Review
- Cell-Penetrating Pepducin Therapy Targeting PAR1 in Subjects With Coronary Artery Disease.Arteriosclerosis, thrombosis, and vascular biology · 2016Article
- Down-regulation of PAR1 activity with a pHLIP-based allosteric antagonist induces cancer cell death.The Biochemical journal · 2015Article
- Allosteric Activation of a G Protein-coupled Receptor with Cell-penetrating Receptor Mimetics.The Journal of biological chemistry · 2015Article
- Inhibition of lethal inflammatory responses through the targeting of membrane-associated Toll-like receptor 4 signaling complexes with a Smad6-derived peptide.EMBO molecular medicine · 2015Article
- Pepducins and Other Lipidated Peptides as Mechanistic Probes and Therapeutics.Methods in molecular biology (Clifton, N.J.) · 2015Article
- Strategic approaches to optimizing peptide ADME properties.The AAPS journal · 2015Review
- Article
- Biological activity of lipophilic derivatives of peptide 562-572 of rat luteinizing hormone receptor.Doklady. Biochemistry and biophysics · 2013Article
- Emerging paradigms in GPCR allostery: implications for drug discovery.Nature reviews. Drug discovery · 2013Review
- Review
- Turning receptors on and off with intracellular pepducins: new insights into G-protein-coupled receptor drug development.The Journal of biological chemistry · 2012Review
- Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
6 authors at 2 institutions in 1 country.
Funding
Abstract
G protein-coupled receptors (GPCR) are a superfamily of receptors that are vital in a wide array of physiological processes. Modulation of GPCR signaling has been an intensive area of therapeutic study, mainly due to the diverse pathophysiological significance of GPCRs. Pepducins are cell-penetrating lipidated peptides designed to target the intracellular loops of the GPCR of interest. Pepducins can function as agonists or antagonists of their cognate receptor, making them highly useful compounds for the study of GPCR signaling. Pepducins have been used to control platelet-dependent hemostasis and thrombosis, tumor growth, invasion, and angiogenesis, as well as to improve sepsis outcomes in mice. Pepducins have been successfully designed against a wide variety of GPCRs including the protease-activated receptors (PAR1, 2, 4), the chemokine receptors (CXCR1, 2, 4), the sphingosine-1-phosphate receptor (S1P3), the adrenergic receptor (ADRA1B), and have the potential to help reveal the functions of intractable GPCRs. Pharmacokinetic, pharmacodynamic, and biodistribution studies have showed that pepducins are widely distributed throughout the body except the brain and possess appropriate drug-like properties for use in vivo. Here, we discuss the delivery, pharmacology, and biodistribution of pepducins, as well as the effects of pepducins in models of inflammation, cardiovascular disease, cancer, and angiogenesis.
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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.