ReviewCurrent pharmaceutical design2010
Ligand-based peptide design and combinatorial peptide libraries to target G protein-coupled receptors.
Review in Current pharmaceutical design, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 58 papers.
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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.
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Who cites it
58 citing papers in PubMed, 105 citations in OpenAlex.
- Venom-Derived Enzyme Inhibitors as Anticancer Agents: Structure-Activity Relationships, Molecular Targets and Mechanistic Insights.Molecules (Basel, Switzerland) · 2026Review
- Do GPCRs constitute the target of 30% of newly approved drugs in Germany?Naunyn-Schmiedeberg's archives of pharmacology · 2026Article
- G-Protein-Coupled Receptor Kinase 2 Limits CCL21-Induced T Cell Migration via Phospholipase Cγ1.Receptors (Basel, Switzerland) · 2025Article
- Prediction of SafD adhesin strong binding peptides for pilus proteins assembly suppression in the prevention ofIn silico pharmacology · 2025Article
- Peptide Inhibitor Assay for Allocating Functionally Important Accessible Sites Throughout a Protein Chain: Restriction Endonuclease EcoRI as a Model Protein System.Biotech (Basel (Switzerland)) · 2024Article
- Machine learning designs new GCGR/GLP-1R dual agonists with enhanced biological potency.Nature chemistry · 2024Article
- Targeting the Oxytocin Receptor for Breast Cancer Management: A Niche for Peptide Tracers.Journal of medicinal chemistry · 2024Review
- Photoswitchable Probes of Oxytocin and Vasopressin.Journal of medicinal chemistry · 2023Article
- Peptidomics.Nature reviews. Methods primers · 2023Article
- Cyclic peptide drugs approved in the last two decades (2001-2021).RSC chemical biology · 2022Review
- Antimicrobial Peptide Mimics for Clinical Use: Does Size Matter?Frontiers in immunology · 2022Review
- Complementary Role of Oxytocin and Vasopressin in Cardiovascular Regulation.International journal of molecular sciences · 2021Review
- Trends in peptide drug discovery.Nature reviews. Drug discovery · 2021Article
- Nature-inspired dimerization as a strategy to modulate neuropeptide pharmacology exemplified with vasopressin and oxytocin.Chemical science · 2021Article
- Allosteric Modulator Leads Hiding in Plain Site: Developing Peptide and Peptidomimetics as GPCR Allosteric Modulators.Frontiers in chemistry · 2021Review
- Neuropeptide signalling systems - An underexplored target for venom drug discovery.Biochemical pharmacology · 2020Review
- Supramolecular Peptide Assemblies as Antimicrobial Scaffolds.Molecules (Basel, Switzerland) · 2020Review
- Oxytocin/vasopressin-like neuropeptide signaling in insects.Vitamins and hormones · 2020Review
- Peptide-based protease inhibitors from plants.Drug discovery today · 2019Review
- Predicting protein-ligand interactions based on bow-pharmacological space and Bayesian additive regression trees.Scientific reports · 2019Article
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
G protein-coupled receptors (GPCRs) are considered to represent the most promising drug targets; it has been repeatedly said that a large fraction of the currently marketed drugs elicit their actions by binding to GPCRs (with cited numbers varying from 30-50%). Closer scrutiny, however, shows that only a modest fraction of (≈60) GPCRs are, in fact, exploited as drug targets, only ≈20 of which are peptide-binding receptors. The vast majority of receptors in the humane genome have not yet been explored as sites of action for drugs. Given the drugability of this receptor class, it appears that opportunities for drug discovery abound. In addition, GPCRs provide for binding sites other than the ligand binding sites (referred to as the "orthosteric site"). These additional sites include (i) binding sites for ligands (referred to as "allosteric ligands") that modulate the affinity and efficacy of orthosteric ligands, (ii) the interaction surface that recruits G proteins and arrestins, (iii) the interaction sites of additional proteins (GIPs, GPCR interacting proteins that regulate G protein signaling or give rise to G protein-independent signals). These sites can also be targeted by peptides. Combinatorial and natural peptide libraries are therefore likely to play a major role in identifying new GPCR ligands at each of these sites. In particular the diverse natural peptide libraries such as the venom peptides from marine cone-snails and plant cyclotides have been established as a rich source of drug leads. High-throughput screening and combinatorial chemistry approaches allow for progressing from these starting points to potential drug candidates. This will be illustrated by focusing on the ligand-based drug design of oxytocin (OT) and vasopressin (AVP) receptor ligands using natural peptide leads as starting points.
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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.