Evidence map›Paper›PMID 35192363›Full record

ArticleJournal of medicinal chemistry2022

Design, Synthesis, and Biological Evaluation of the First Inhibitors of Oncogenic CHD1L.

Brett J Prigaro, Hector Esquer, Qiong Zhou, Laura A Pike, Paul Awolade, Xin-He Lai, Adedoyin D Abraham, Joshua M Abbott, Brock Matter, Uday B Kompella and 3 more

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2022. 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
2.1field-weighted citation impact, top 13% 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, 21 citations in OpenAlex.

  1. Article
  2. CHD1L in cancer and beyond: structure, oncogenic functions, and therapeutic potential.Journal of experimental & clinical cancer research : CR · 2025
    Review
  3. Article
  4. Article
  5. Article
  6. Chromatin remodellers as therapeutic targets.Nature reviews. Drug discovery · 2024
    Review
  7. Article
  8. Review
  9. The validation of new CHD1L inhibitors as a therapeutic strategy for cancer.Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie · 2024
    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

13 authors at 1 institution in 1 country.

Brett J PrigaroThe Skaggs School of Pharmacy and Pharmaceutical Sciences, Department of Pharmaceutical Sciences, The CU Cancer Center, Aurora, Colorado 80045, United States.
Hector EsquerThe Skaggs School of Pharmacy and Pharmaceutical Sciences, Department of Pharmaceutical Sciences, The CU Cancer Center, Aurora, Colorado 80045, United States.
Qiong ZhouThe Skaggs School of Pharmacy and Pharmaceutical Sciences, Department of Pharmaceutical Sciences, The CU Cancer Center, Aurora, Colorado 80045, United States.
Laura A PikeThe Skaggs School of Pharmacy and Pharmaceutical Sciences, Department of Pharmaceutical Sciences, The CU Cancer Center, Aurora, Colorado 80045, United States.
Paul AwoladeThe Skaggs School of Pharmacy and Pharmaceutical Sciences, Department of Pharmaceutical Sciences, The CU Cancer Center, Aurora, Colorado 80045, United States.ORCID 0000-0003-3995-121X
Xin-He LaiThe Skaggs School of Pharmacy and Pharmaceutical Sciences, Department of Pharmaceutical Sciences, The CU Cancer Center, Aurora, Colorado 80045, United States.
Adedoyin D AbrahamThe Skaggs School of Pharmacy and Pharmaceutical Sciences, Department of Pharmaceutical Sciences, The CU Cancer Center, Aurora, Colorado 80045, United States.
Joshua M AbbottThe Skaggs School of Pharmacy and Pharmaceutical Sciences, Department of Pharmaceutical Sciences, The CU Cancer Center, Aurora, Colorado 80045, United States.
Brock MatterThe Skaggs School of Pharmacy and Pharmaceutical Sciences, Department of Pharmaceutical Sciences, The CU Cancer Center, Aurora, Colorado 80045, United States.
Uday B KompellaThe Skaggs School of Pharmacy and Pharmaceutical Sciences, Department of Pharmaceutical Sciences, The CU Cancer Center, Aurora, Colorado 80045, United States.
Wells A MessersmithThe School of Medicine, Division of Medical Oncology, The CU Cancer Center, Aurora, Colorado 80045, United States.
Daniel L GustafsonFlint Animal Cancer Center and Department of Clinical Sciences, School of Biomedical Engineering, Colorado State University, Fort Collins, Colorado 80523, United States.
Daniel V LaBarberaThe Skaggs School of Pharmacy and Pharmaceutical Sciences, Department of Pharmaceutical Sciences, The CU Cancer Center, Aurora, Colorado 80045, United States.ORCID 0000-0001-9460-3862
University of Colorado Cancer Center · US

Funding

X-RAY CRYSTALLOGRAPHYP30CA008748 · NCI · SLOAN-KETTERING INSTITUTE FOR CANCER RES · PI Hongbiao Carl Lekaye · 1985 to 2026
$347.4M
University of Colorado Cancer Center Support Grant - Lung Cancer Patient-Derived Xenografts with Autologous Human Immune SystemsP30CA046934 · NCI · UNIVERSITY OF COLORADO DENVER · PI James V Degregori · 1988 to 2026
$117.0M
The Development of First-in-Class Inhibitors of Oncogenic CHD1L for the Treatment of Colorectal Cancer.R01CA251361 · NCI · UNIVERSITY OF COLORADO DENVER · PI LABARBERA, DANIEL V. · 2020 to 2024
$1.9M
NCI NIH HHS P30 CA008748NCI NIH HHS P30 CA046934NCI NIH HHS R01 CA251361
6 · The paper itself

Abstract

Chromodomain helicase DNA-binding protein 1 like (CHD1L) is an oncogene implicated in tumor progression, multidrug resistance, and metastasis in many types of cancer. In this article, we described the optimization of the first lead CHD1L inhibitors (CHD1Li) through drug design and medicinal chemistry. More than 30 CHD1Li were synthesized and evaluated using a variety of colorectal cancer (CRC) tumor organoid models and functional assays. The results led to the prioritization of six lead CHD1Li analogues with improved potency, antitumor activity, and drug-like properties including metabolic stability and in vivo pharmacokinetics. Furthermore, lead CHD1Li

Indexed as

Antineoplastic AgentsDNA-Binding ProteinsDNA HelicasesCarcinogenesisCell Line, TumorDrug DesignHumansOncogenesAntineoplastic AgentsCHD1L protein, humanDNA-Binding ProteinsDNA Helicases

Identifiers

PMID35192363
PMCPMC8981980
OpenAlexW4213445414

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.