Evidence map›Paper›PMID 38680566›Full record

ArticleACS central science2024

Leveraging a Phage-Encoded Noncanonical Amino Acid: A Novel Pathway to Potent and Selective Epigenetic Reader Protein Inhibitors.

Peng-Hsun Chase Chen, Xuejiao Shirley Guo, Hanyuan Eric Zhang, Gopal K Dubey, Zhi Zachary Geng, Carol A Fierke, Shiqing Xu, J Trae Hampton, Wenshe Ray Liu

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in ACS central science, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.

0numbers the graph read from it
0cells of the map it votes in
17citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

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.

2 · The registry

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.

3 · Its place in the literature

Who cites it

17 citing papers in PubMed.

  1. Article
  2. Incorporation of Butyryl-Lysine into Phage-Displayed Peptide Libraries.Methods in molecular biology (Clifton, N.J.) · 2026
    Article
  3. Review
  4. Article
  5. Review
  6. Review
  7. Review
  8. Review
  9. Review
  10. Review
  11. Review
  12. Review
  13. Article
  14. Epigenetics-targeted drugs: current paradigms and future challenges.Signal transduction and targeted therapy · 2024
    Review
  15. Repurposing Copper(II)/THPTA as A Bioorthogonal Catalyst for Thiazolidine Bond Cleavage.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2024
    Article
  16. Genome Mining and Biological Engineering of Type III Borosins from Bacteria.International journal of molecular sciences · 2024
    Article
  17. Review
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

9 authors.

Peng-Hsun Chase ChenTexas A&M Drug Discovery Center and Department of Chemistry, Texas A&M University, College Station, Texas 77843, United States.ORCID https://orcid.org/0000-0001-9822-6398
Xuejiao Shirley GuoTexas A&M Drug Discovery Center and Department of Chemistry, Texas A&M University, College Station, Texas 77843, United States.
Hanyuan Eric ZhangTexas A&M Drug Discovery Center and Department of Chemistry, Texas A&M University, College Station, Texas 77843, United States.
Gopal K DubeyTexas A&M Drug Discovery Center and Department of Chemistry, Texas A&M University, College Station, Texas 77843, United States.
Zhi Zachary GengTexas A&M Drug Discovery Center and Department of Chemistry, Texas A&M University, College Station, Texas 77843, United States.
Carol A FierkeDepartment of Biochemistry, Brandeis University, Waltham, Massachusetts 02453, United States.ORCID https://orcid.org/0000-0002-1481-0579
Shiqing XuTexas A&M Drug Discovery Center and Department of Chemistry, Texas A&M University, College Station, Texas 77843, United States.ORCID https://orcid.org/0000-0001-6260-9290
J Trae HamptonTexas A&M Drug Discovery Center and Department of Chemistry, Texas A&M University, College Station, Texas 77843, United States.ORCID https://orcid.org/0000-0001-5562-162X
Wenshe Ray LiuTexas A&M Drug Discovery Center and Department of Chemistry, Texas A&M University, College Station, Texas 77843, United States.ORCID https://orcid.org/0000-0002-7078-6534

Funding

Use of the Noncanonical Amino Acid Mutagenesis Technique in Combination with Other Approaches to Study Functions of Posttranslational Lysine Modifications in ProteinsR35GM145351 · NIGMS · TEXAS A&M UNIVERSITY · PI Wenshe Ray Liu · 2022 to 2026
$2.6M
Targeting the ENL YEATS domain for the development of anti-leukemia agentsR21CA267512 · NCI · TEXAS A&M UNIVERSITY · PI LIU, WENSHE RAY · 2022 to 2023
$377k
NCI NIH HHS R21 CA267512NIGMS NIH HHS R35 GM145351
6 · The paper itself

Abstract

Epigenetic reader proteins interpret histone epigenetic marks to regulate gene expression. Given their vital roles and the link between their dysfunction and various diseases, these proteins present compelling targets for therapeutic interventions. Nevertheless, designing selective inhibitors for these proteins poses significant challenges, primarily due to their unique properties such as shallow binding sites and similarities with homologous proteins. To overcome these challenges, we propose an innovative strategy that uses phage display with a genetically encoded noncanonical amino acid (ncAA) containing an epigenetic mark. This ncAA guides binding to the reader protein's active site, allowing the identification of peptide inhibitors with enhanced affinity and selectivity. In this study, we demonstrate this novel approach's effectiveness by identifying potent inhibitors for the ENL YEATS domain that plays a critical role in leukemogenesis. Our strategy involved genetically incorporating

Identifiers

PMID38680566
PMCPMC11046469

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Registered trials

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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.