ArticleChemical biology & drug design2019
Bisubstrate inhibitors to target histone acetyltransferase 1.
Article in Chemical biology & drug design, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
What it found
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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
12 citing papers in PubMed, 26 citations in OpenAlex.
- Inhibition of Histone Lysine Acetyltransferases by Coenzyme A Analogs.Molecules (Basel, Switzerland) · 2026Article
- An Acetyl-Click Chemistry Assay to Measure Histone Acetyltransferase 1 Acetylation.Journal of visualized experiments : JoVE · 2024Article
- Acetyl-Click Screening Platform Identifies Small-Molecule Inhibitors of Histone Acetyltransferase 1 (HAT1).Journal of medicinal chemistry · 2023Article
- Understanding HAT1: A Comprehensive Review of Noncanonical Roles and Connection with Disease.Genes · 2023Review
- Advances in the Histone Acetylation Modification in the Oral Squamous Cell Carcinoma.Journal of oncology · 2023Review
- Article
- Histone acetylation modifications: A potential targets for the diagnosis and treatment of papillary thyroid cancer.Frontiers in oncology · 2022Review
- Histone modification and histone modification-targeted anti-cancer drugs in breast cancer: Fundamentals and beyond.Frontiers in pharmacology · 2022Review
- Recent insights intoEpigenetics · 2021Review
- Targeting a critical step in fungal hexosamine biosynthesis.The Journal of biological chemistry · 2020Article
- Regulation of epigenetic state by non-histone chromatin proteins and transcription factors: Implications in disease.Journal of biosciences · 2020Review
- Review
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
Developing selective enzyme inhibitors allows for the expansion of molecular toolboxes to investigate functions and activities of target enzymes. The histone acetyltransferase 1 (HAT1) is among the first histone acetyltransferase (HAT) enzymes that were discovered in the mid-1990s; however, it remains one of the poorly studied enzymes in comparison with the other HATs. Although HAT1 has been linked to various disease states, no inhibitors have been reported to target HAT1. Here, we designed a set of peptide-CoA conjugates as bisubstrate inhibitors of HAT1 with submicromolar potency. In particular, the bisubstrate inhibitor H4K12CoA exhibited a low K
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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.