ArticleJournal of medicinal chemistry2015
Proteasome inhibitors with pyrazole scaffolds from structure-based virtual screening.
Article in Journal of medicinal chemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 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
17 citing papers in PubMed, 54 citations in OpenAlex.
- Primed for Interactions: Investigating the Primed Substrate Channel of the Proteasome for Improved Molecular Engagement.Molecules (Basel, Switzerland) · 2024Review
- A Shortcut from Genome to Drug: The Employment of Bioinformatic Tools to Find New Targets for Gastric Cancer Treatment.Pharmaceutics · 2023Article
- Attempting to Increase the Effectiveness of the Antidepressant Trazodone Hydrochloride Drug Using π-Acceptors.International journal of environmental research and public health · 2022Article
- Developing New Treatments for COVID-19 through Dual-Action Antiviral/Anti-Inflammatory Small Molecules and Physiologically Based Pharmacokinetic Modeling.International journal of molecular sciences · 2022Review
- Drug Discovery forInternational journal of molecular sciences · 2021Review
- Bioactive recombinant human oncostatin M for NMR-based screening in drug discovery.Scientific reports · 2021Article
- An Updated Review of Computer-Aided Drug Design and Its Application to COVID-19.BioMed research international · 2021Review
- Ubiquitination Regulators Discovered by Virtual Screening for the Treatment of Cancer.Frontiers in cell and developmental biology · 2021Review
- Novel Compounds Identified by Structure-Based Prion Disease Drug Discovery Using In Silico Screening Delay the Progression of an Illness in Prion-Infected Mice.Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics · 2020Article
- Assessing and improving the performance of consensus docking strategies using the DockBox package.Journal of computer-aided molecular design · 2019Article
- A Structure-Based Drug Discovery Paradigm.International journal of molecular sciences · 2019Review
- Next-generation proteasome inhibitors for cancer therapy.Translational research : the journal of laboratory and clinical medicine · 2018Review
- Fusing Docking Scoring Functions Improves the Virtual Screening Performance for Discovering Parkinson's Disease Dual Target Ligands.Current neuropharmacology · 2017Article
- Blockade of the malignant phenotype by β-subunit selective noncovalent inhibition of immuno- and constitutive proteasomes.Oncotarget · 2017Article
- Computational Approaches for the Discovery of Human Proteasome Inhibitors: An Overview.Molecules (Basel, Switzerland) · 2016Review
- Molecular docking and structure-based drug design strategies.Molecules (Basel, Switzerland) · 2015Review
- Fundamental reaction pathway and free energy profile of proteasome inhibition by syringolin A (SylA).Organic & biomolecular chemistry · 2015Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
18 authors at 5 institutions in 2 countries.
Funding
Abstract
We performed a virtual screen of ∼340 000 small molecules against the active site of proteasomes followed by in vitro assays and subsequent optimization, yielding a proteasome inhibitor with pyrazole scaffold. The pyrazole-scaffold compound displayed excellent metabolic stability and was highly effective in suppressing solid tumor growth in vivo. Furthermore, the effectiveness of this compound was not negatively impacted by resistance to bortezomib or carfilzomib.
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.