Evidence map›Paper›PMID 39746899›Full record

ArticleJournal of medicinal chemistry2025

Development of PRC1 Inhibitors Employing Fragment-Based Approach and NMR-Guided Optimization.

Yiwu Yao, Miranda L Simes, Weijiang Ying, Qingjie Zhao, Alyssa Winkler, Shirish Shukla, Felicia Gray, Caroline Nikolaidis, Geoff Hewett, Jolanta Grembecka and 1 more

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing 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

3 citing papers in PubMed.

  1. Article
  2. Review
  3. 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

11 authors.

Yiwu YaoDepartment of Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.ORCID 0000-0003-4642-5840
Miranda L SimesDepartment of Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.
Weijiang YingDepartment of Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.
Qingjie ZhaoDepartment of Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.
Alyssa WinklerDepartment of Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.
Shirish ShuklaDepartment of Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.
Felicia GrayDepartment of Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.
Caroline NikolaidisDepartment of Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.
Geoff HewettDepartment of Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.
Jolanta GrembeckaDepartment of Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.ORCID 0000-0002-6180-9095
Tomasz CierpickiDepartment of Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.ORCID 0000-0003-2058-0658

Funding

Michigan Chemistry-Biology Interface Training ProgramT32GM132046 · NIGMS · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI Emily E Scott, Wenjing Wang · 2019 to 2026
$4.1M
Development of ASH1L inhibitors for acute leukemiaR01CA244254 · NCI · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI GREMBECKA, JOLANTA · 2020 to 2024
$2.8M
Targeting Menin in Acute Leukemia with Upregulated HOX GenesR01CA272561 · NCI · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI Jolanta Grembecka · 2023 to 2026
$2.5M
Targeting PRC1 in leukemiaR01CA282082 · NCI · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI Tomasz Cierpicki · 2023 to 2026
$2.5M
Targeting NSD1 in leukemiaR01CA226759 · NCI · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI CIERPICKI, TOMASZ · 2019 to 2023
$2.3M
Screening for inhibitors of NSD3 as a treatment for lung cancerR01CA276074 · NCI · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI Jolanta Grembecka · 2023 to 2026
$2.0M
Development of chemical probe targeting NSD3 SET domain in breast cancerR01CA285304 · NCI · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI Tomasz Cierpicki · 2024 to 2026
$1.7M
NCI NIH HHS R01 CA226759NCI NIH HHS R01 CA244254NCI NIH HHS R01 CA272561NCI NIH HHS R01 CA276074NCI NIH HHS R01 CA282082NCI NIH HHS R01 CA285304NIGMS NIH HHS T32 GM132046
6 · The paper itself

Abstract

Polycomb Repressive Complex 1 (PRC1) is associated with transcriptional silencing, and its dysregulation plays an important role in various cancers. Well-characterized PRC1 inhibitors can facilitate the exploration of PRC1 inhibition as therapeutic agents. By employing an NMR-based fragment screening approach, we have previously identified a very weak millimolar ligand

Indexed as

Polycomb Repressive Complex 1Cell Cycle ProteinsHumansMagnetic Resonance SpectroscopyStructure-Activity RelationshipCell Cycle ProteinsPolycomb Repressive Complex 1PRC1 protein, human

Identifiers

PMID39746899
PMCPMC11969575

What OpenQuestion holds

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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.