ArticleMedChemComm2012
Optimizing PK properties of cyclic peptides: the effect of side chain substitutions on permeability and clearance().
Article in MedChemComm, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 36 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
36 citing papers in PubMed, 131 citations in OpenAlex.
- Fine-Tuning Side Chain Substitutions: Impacts on the Lipophilicity-Solubility-Permeability Interplay in Macrocyclic Peptides.Marine drugs · 2025Article
- Discovery of Cell-Permeable Macrocyclic Cyclin A/B RxL Inhibitors that Demonstrate Antitumor Activity.Journal of medicinal chemistry · 2025Article
- Predicting Distribution Coefficients (LogD) of Cyclic Peptides Using Molecular Dynamics Simulations.Pharmaceutical research · 2025Article
- Cyclic Peptide C5aR1 Antagonist Design Using Solution Conformational Analysis Derived from Residual Dipolar Couplings.ACS medicinal chemistry letters · 2024Article
- Cell penetration of oxadiazole-containing macrocycles.RSC chemical biology · 2024Article
- An amide to thioamide substitution improves the permeability and bioavailability of macrocyclic peptides.Nature communications · 2023Article
- Advancement from Small Peptide Pharmaceuticals to Orally Active Piperazine-2,5-dion-Based Cyclopeptides.International journal of molecular sciences · 2023Review
- Mixture-Based Screening of Focused Combinatorial Libraries by NMR: Application to the Antiapoptotic Protein hMcl-1.Journal of medicinal chemistry · 2023Article
- In Vivo Pharmacokinetic and Pharmacodynamic Properties of the Antiarrhythmic MoleculeThe Journal of pharmacology and experimental therapeutics · 2023Article
- Amide-to-ester substitution as a stable alternative to N-methylation for increasing membrane permeability in cyclic peptides.Nature communications · 2023Article
- Lessons for Oral Bioavailability: How Conformationally Flexible Cyclic Peptides Enter and Cross Lipid Membranes.Journal of medicinal chemistry · 2023Article
- Article
- Development of Peptide Biopharmaceuticals in Russia.Pharmaceutics · 2022Review
- Cyclic peptide drugs approved in the last two decades (2001-2021).RSC chemical biology · 2022Review
- Geometrically Diverse Lariat Peptide Scaffolds Reveal an Untapped Chemical Space of High Membrane Permeability.Journal of the American Chemical Society · 2021Article
- Macrocycle Cell Permeability Measured by Solvation Free Energies in Polar and Apolar Environments.Journal of chemical information and modeling · 2020Article
- Substrate Plasticity of a Fungal Peptide α-ACS chemical biology · 2020Article
- Current status and future directions of high-throughput ADME screening in drug discovery.Journal of pharmaceutical analysis · 2020Review
- Article
- Permeability of Cyclic Peptide Macrocycles and Cyclotides and Their Potential as Therapeutics.ACS medicinal chemistry letters · 2019Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
16 authors at 4 institutions in 2 countries.
Funding
Abstract
A series of cyclic peptides were designed and prepared to investigate the physicochemical properties that affect oral bioavailabilty of this chemotype in rats. In particular, the ionization state of the peptide was examined by the incorporation of naturally occurring amino acid residues that are charged in differing regions of the gut. In addition, data was generated in a variety of in vitro assays and the usefulness of this data in predicting the subsequent oral bioavailability observed in the rat is discussed.
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.