Evidence map›Paper›PMID 39508435›Full record

ArticleJournal of medicinal chemistry2024

Discovery of CHD1 Antagonists for PTEN-Deficient Prostate Cancer.

Rebecca L Johnson, Amanda L Graboski, Fengling Li, Jacqueline L Norris-Drouin, William G Walton, Cheryl H Arrowsmith, Matthew R Redinbo, Stephen V Frye, Lindsey I James

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.

0numbers the graph read from it
0cells of the map it votes in
8citing 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

8 citing papers in PubMed.

  1. Review
  2. Article
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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.

Rebecca L JohnsonCenter 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.
Amanda L GraboskiDepartment of Pharmacology, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States.
Fengling LiStructural Genomics Consortium, University of Toronto, Toronto, ON M5G 1L7, Canada.
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.
William G WaltonDepartments of Chemistry, Biochemistry & Biophysics, and Microbiology & Immunology, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States.
Cheryl H ArrowsmithStructural Genomics Consortium, University of Toronto, Toronto, ON M5G 1L7, Canada.ORCID 0000-0002-4971-3250
Matthew R RedinboDepartments of Chemistry, Biochemistry & Biophysics, and Microbiology & Immunology, 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
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

Funding

PROBING ALLOSTERY IN METHYL-LYSINE READER DOMAINSR35GM139514 · NIGMS · UNIV OF NORTH CAROLINA CHAPEL HILL · PI FRYE, STEPHEN VERNON · 2021 to 2025
$2.1M
POLYCOMB REPRESSIVE COMLEXE AS KEY REGULATORS OF HIV LATENCY AND TARGETS FOR LATENCY REVERSALR33DA047023 · NIDA · UNIV OF NORTH CAROLINA CHAPEL HILL · PI JAMES, LINDSEY INGERMAN · 2022 to 2023
$1.8M
DISCOVERY OF FIRST-IN-CLASS NSD2 DEGRADERS FOR CANCER THERAPYR01CA242305 · NCI · UNIV OF NORTH CAROLINA CHAPEL HILL · PI JAMES, LINDSEY INGERMAN · 2019 to 2024
$1.7M
Gut Microbial Enzymes and Human DiseaseR35GM152079 · NIGMS · UNIV OF NORTH CAROLINA CHAPEL HILL · PI Matthew R Redinbo · 2024 to 2026
$1.6M
NCI NIH HHS R01 CA242305NIDA NIH HHS R33 DA047023NIGMS NIH HHS R35 GM139514NIGMS NIH HHS R35 GM152079
6 · The paper itself

Abstract

CHD1 is a chromodomain-helicase DNA-binding protein that preferentially recognizes di- and trimethylated lysine 4 on histone H3 (H3K4me2/3). Genetic studies have established CHD1 as a synthetic lethal target in phosphatase and tensin homologue (PTEN)-deficient cancers. Despite this attractive therapeutic link, no inhibitors or antagonists of CHD1 have been reported to date. Herein, we report the discovery of UNC10142, a first-in-class small molecule antagonist of the tandem chromodomains of CHD1 that binds with an IC

Indexed as

DNA-Binding ProteinsProstatic NeoplasmsPTEN PhosphohydrolaseAntineoplastic AgentsCell Line, TumorCrystallography, X-RayDNA HelicasesDrug DiscoveryHumansMaleSmall Molecule LibrariesStructure-Activity RelationshipAntineoplastic AgentsCHD1 protein, humanDNA-Binding ProteinsDNA HelicasesPTEN PhosphohydrolasePTEN protein, humanSmall Molecule Libraries

Identifiers

PMID39508435
PMCPMC11694488

What OpenQuestion holds

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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.