ArticleAngewandte Chemie (International ed. in English)2016
Unveiling (-)-Englerin A as a Modulator of L-Type Calcium Channels.
Article in Angewandte Chemie (International ed. in English), 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 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
16 citing papers in PubMed, 40 citations in OpenAlex.
- Natural product drug discovery in the artificial intelligence era.Chemical science · 2022Review
- Natural products targeting cancer cell dependency.The Journal of antibiotics · 2021Review
- Allosteric Antagonist Modulation of TRPV2 by Piperlongumine Impairs Glioblastoma Progression.ACS central science · 2021Article
- Cheminformatics in Natural Product-based Drug Discovery.Molecular informatics · 2020Review
- Investigation of the Selectivity of L-Type Voltage-Gated Calcium Channels 1.3 for Pyrimidine-2,4,6-Triones Derivatives Based on Molecular Dynamics Simulation.Molecules (Basel, Switzerland) · 2020Article
- Validation strategies for target prediction methods.Briefings in bioinformatics · 2020Review
- Englerin A-sensing charged residues for transient receptor potential canonical 5 channel activation.The Korean journal of physiology & pharmacology : official journal of the Korean Physiological Society and the Korean Society of Pharmacology · 2019Article
- Computational advances in combating colloidal aggregation in drug discovery.Nature chemistry · 2019Review
- NP-Scout: Machine Learning Approach for the Quantification and Visualization of the Natural Product-Likeness of Small Molecules.Biomolecules · 2019Article
- Machine intelligence decrypts β-lapachone as an allosteric 5-lipoxygenase inhibitor.Chemical science · 2018Article
- TRPC4/TRPC5 channels mediate adverse reaction to the cancer cell cytotoxic agent (-)-Englerin A.Oncotarget · 2018Article
- Review
- NaScientific reports · 2017Article
- Englerins: A Comprehensive Review.Journal of natural products · 2017Review
- Article
- Unveiling (-)-Englerin A as a Modulator of L-Type Calcium Channels.Angewandte Chemie (International ed. in English) · 2016Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
7 authors at 3 institutions in 4 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The voltage-dependent L-type Ca(2+) channel was identified as a macromolecular target for (-)-englerin A. This finding was reached by using an unprecedented ligand-based prediction platform and the natural product piperlongumine as a pharmacophore probe. (-)-Englerin A features high substructure dissimilarity to known ligands for voltage-dependent Ca(2+) channels, selective binding affinity for the dihydropyridine site, and potent modulation of calcium signaling in muscle cells and vascular tissue. The observed activity was rationalized at the atomic level by molecular dynamics simulations. Experimental confirmation of this hitherto unknown macromolecular target expands the bioactivity space for this natural product and corroborates the effectiveness of chemocentric computational methods for prioritizing target-based screens and identifying binding counterparts of complex natural products.
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.