Evidence map›Paper›PMID 33999620›Full record

ArticleJournal of medicinal chemistry2021

Discovery of an H3K36me3-Derived Peptidomimetic Ligand with Enhanced Affinity for Plant Homeodomain Finger Protein 1 (PHF1).

Isabelle A Engelberg, Jiuyang Liu, Jacqueline L Norris-Drouin, Stephanie H Cholensky, Samantha A Ottavi, Stephen V Frye, Tatiana G Kutateladze, Lindsey I James

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.

0numbers the graph read from it
0cells of the map it votes in
10citing papers in PubMed
1.3field-weighted citation impact, top 20% of its field
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

10 citing papers in PubMed, 20 citations in OpenAlex.

  1. Article
  2. Review
  3. Development of Dimethylsulfonium Probes for Broad Profiling of Methyllysine Reader Proteins.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026
    Article
  4. Article
  5. Article
  6. Article
  7. Chemical tools targeting readers of lysine methylation.Current opinion in chemical biology · 2023
    Review
  8. Virtual Special Issue: Epigenetics 2022.ACS pharmacology & translational science · 2022
    Article
  9. Virtual Special Issue: Epigenetics 2022.ACS medicinal chemistry letters · 2022
    Article
  10. Article
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

8 authors at 2 institutions in 1 country.

Isabelle A EngelbergCenter for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States.
Jiuyang LiuDepartment of Pharmacology, University of Colorado School of Medicine, Aurora, Colorado 80045, United States.
Jacqueline L Norris-DrouinCenter for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States.
Stephanie H CholenskyCenter for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States.
Samantha A OttaviCenter for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States.
Stephen V FryeCenter for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States.ORCID 0000-0002-2415-2215
Tatiana G KutateladzeDepartment of Pharmacology, University of Colorado School of Medicine, Aurora, Colorado 80045, United States.ORCID 0000-0001-7375-6990
Lindsey I JamesCenter for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States.ORCID 0000-0002-6034-7116
University of North Carolina at Chapel Hill · USUniversity of Colorado Denver · US

Funding

DISCOVERY OF CHEMICAL PROBES FOR METHYL-LYSINE READERSR01GM100919 · NIGMS · UNIV OF NORTH CAROLINA CHAPEL HILL · PI FRYE, STEPHEN VERNON · 2012 to 2019
$2.9M
POLYCOMB REPRESSIVE COMLEXE AS KEY REGULATORS OF HIV LATENCY AND TARGETS FOR LATENCY REVERSALR61DA047023 · NIDA · UNIV OF NORTH CAROLINA CHAPEL HILL · PI JAMES, LINDSEY INGERMAN · 2018 to 2020
$2.7M
Targeting acetylated histone H4 by MLL4R01AG067664 · NIA · UNIVERSITY OF COLORADO DENVER · PI KUTATELADZE, TATIANA G · 2021 to 2025
$2.1M
Molecular analysis of ASH1LR01CA252707 · NCI · UNIVERSITY OF COLORADO DENVER · PI TATIANA G KUTATELADZE · 2020 to 2026
$1.9M
The role of JADE in HBO complexesR01HL151334 · NHLBI · UNIVERSITY OF COLORADO DENVER · PI KUTATELADZE, TATIANA G · 2020 to 2023
$1.8M
NCI NIH HHS R01 CA252707NHLBI NIH HHS R01 HL151334NIA NIH HHS R01 AG067664NIDA NIH HHS R61 DA047023NIGMS NIH HHS R01 GM100919
6 · The paper itself

Abstract

Plant homeodomain finger protein 1 (PHF1) is an accessory component of the gene silencing complex polycomb repressive complex 2 and recognizes the active chromatin mark, trimethylated lysine 36 of histone H3 (H3K36me3). In addition to its role in transcriptional regulation, PHF1 has been implicated as a driver of endometrial stromal sarcoma and fibromyxoid tumors. We report the discovery and characterization of UNC6641, a peptidomimetic antagonist of the PHF1 Tudor domain which was optimized through in silico modeling and incorporation of non-natural amino acids. UNC6641 binds the PHF1 Tudor domain with a

Indexed as

Amino Acid SequenceCrystallography, X-RayDNA-Binding ProteinsHumansLigandsMutagenesis, Site-DirectedNuclear Magnetic Resonance, BiomolecularPeptidomimeticsPolycomb-Group ProteinsProtein BindingTudor DomainDNA-Binding ProteinsLigandsPeptidomimeticsPHF1 protein, humanPolycomb-Group Proteins

Identifiers

PMID33999620
PMCPMC8225578
OpenAlexW3162472821

What OpenQuestion holds

Textmetadata
LicenceTDM
Read underepoch 390

Registered trials

None linked

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.