ArticleACS medicinal chemistry letters2018
Discovery of Spiro Oxazolidinediones as Selective, Orally Bioavailable Inhibitors of p300/CBP Histone Acetyltransferases.
Article in ACS medicinal chemistry letters, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 32 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
32 citing papers in PubMed, 72 citations in OpenAlex.
- Dysregulated AKT signaling reprograms osteosarcoma to drive selective reliance on EP300.The Journal of experimental medicine · 2026Article
- Inhibition of p300/CREBBP catalytic activity drives context-dependent transcriptional activation in AML.Blood · 2026Article
- Lactylation enzymes in cancer: Mechanisms and novel therapeutic approaches (Review).Oncology letters · 2026Review
- Sex- and skeletal muscle-specific gene expression response of histone 3 lysine 27-modifying enzymes by voluntary running in mice.Physiological reports · 2026Article
- Chromatin Regulatory Targets for Anticancer Therapeutics.Chemical reviews · 2025Review
- Spiro Hydantoins Can Reverse the Action of Positive Allosteric Modulators on GABAACS medicinal chemistry letters · 2025Article
- Targeting lysine acetylation readers and writers.Nature reviews. Drug discovery · 2025Review
- Targeting the epigenome and tumor heterogeneity: advances in immunotherapy for chemoresistant metastatic colorectal cancer.Frontiers in immunology · 2025Review
- Recent Development in Hydantoins, Thiohydantoins, and Selenohydantoins as Anticancer Agents: Structure-activity Relationship and Design Strategies.Mini reviews in medicinal chemistry · 2025Review
- Maintenance of thermogenic adipose tissues despite loss of the H3K27 acetyltransferases p300 or CBP.American journal of physiology. Endocrinology and metabolism · 2024Article
- Group 3 medulloblastoma transcriptional networks collapse under domain specific EP300/CBP inhibition.Nature communications · 2024Article
- Characterization of molecular mechanisms driving Merkel cell polyomavirus oncogene transcription and tumorigenic potential.PLoS pathogens · 2023Article
- Chemically induced degradation of epigenetic targets.Chemical Society reviews · 2023Review
- Reference compounds for characterizing cellular injury in high-content cellular morphology assays.Nature communications · 2023Article
- Pharmacological targeting of CBP/p300 drives a redox/autophagy axis leading to senescence-induced growth arrest in non-small cell lung cancer cells.Cancer gene therapy · 2023Article
- Identification of ligand linkage vectors for the development of p300/CBP degraders.RSC medicinal chemistry · 2022Article
- EP300 Selectively Controls the Enhancer Landscape of MYCN-Amplified Neuroblastoma.Cancer discovery · 2022Article
- Inactivation of the CIC-DUX4 oncogene through P300/CBP inhibition, a therapeutic approach for CIC-DUX4 sarcoma.Oncogenesis · 2021Article
- Article
- Discovery of a Potent and Selective Covalent p300/CBP Inhibitor.ACS medicinal chemistry letters · 2021Article
Corrections and comments
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Authors and funding
21 authors at 1 institution in 1 country.
Funding
Abstract
p300 and its paralog CBP can acetylate histones and other proteins and have been implicated in a number of diseases characterized by aberrant gene activation, such as cancer. A novel, highly selective, orally bioavailable histone acetyltransferase (HAT) domain inhibitor has been identified through virtual ligand screening and subsequent optimization of a unique hydantoin screening hit. Conformational restraint in the form of a spirocyclization followed by substitution with a urea led to a significant improvement in potency. Replacement of the hydantoin moiety with an oxazolidinedione followed by fluoro substitution led to
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.