Evidence map›Paper›PMID 35080528›Full record

ArticleChemical communications (Cambridge, England)2022

3-Aminophthalic acid, a new cereblon ligand for targeted protein degradation by O'PROTAC.

Yuqian Yan, Jingwei Shao, Donglin Ding, Yunqian Pan, Phuc Tran, Wei Yan, Zhengyu Wang, Hong-Yu Li, Haojie Huang

Open access · greenAbstract read
In one paragraph

Article in Chemical communications (Cambridge, England), 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing papers in PubMed
1.6field-weighted citation impact, top 18% 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

6 citing papers in PubMed, 18 citations in OpenAlex.

  1. Evolving CRBN ligands enhance the drug-like properties of protein degraders.Journal of enzyme inhibition and medicinal chemistry · 2026
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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 at 2 institutions in 1 country.

Yuqian YanDepartment of Biochemistry and Molecular Biology, Mayo Clinic College of Medicine and Science, Rochester, MN 55905, USA. Huang.Haojie@Mayo.edu.
Jingwei ShaoDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, Little Rock, AR 72205, USA. HLi2@uams.edu.
Donglin DingDepartment of Biochemistry and Molecular Biology, Mayo Clinic College of Medicine and Science, Rochester, MN 55905, USA. Huang.Haojie@Mayo.edu.
Yunqian PanDepartment of Biochemistry and Molecular Biology, Mayo Clinic College of Medicine and Science, Rochester, MN 55905, USA. Huang.Haojie@Mayo.edu.
Phuc TranDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, Little Rock, AR 72205, USA. HLi2@uams.edu.
Wei YanDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, Little Rock, AR 72205, USA. HLi2@uams.edu.
Zhengyu WangDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, Little Rock, AR 72205, USA. HLi2@uams.edu.
Hong-Yu LiDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, Little Rock, AR 72205, USA. HLi2@uams.edu.
Haojie HuangDepartment of Biochemistry and Molecular Biology, Mayo Clinic College of Medicine and Science, Rochester, MN 55905, USA. Huang.Haojie@Mayo.edu.ORCID http://orcid.org/0000-0003-2751-6413
University of Arkansas for Medical Sciences · USMayo Clinic · US

Funding

Role of proinflammatory cytokine-induced AR degradation in castration-resistant prostate cancerR01CA130908 · NCI · STATE UNIVERSITY NEW YORK STONY BROOK · PI HUANG, HAOJIE · 2010 to 2021
$3.5M
Impact of myeloid leukemia associated mutations (ASXL1, DNMT3A, TET2, IDH1 and IDH2) on treatment responses among Chronic Myeloid Leukemia (CML) patients in TanzaniaR01CA249282 · NCI · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI LI, HONG-YU, SHAH, NEIL P · 2021 to 2025
$3.4M
Role of FOXO1 Inactivation in Prostate TumorigenesisR01CA134514 · NCI · UNIVERSITY OF MINNESOTA · PI HUANG, HAOJIE · 2009 to 2019
$3.3M
Cooperativity of TMPRSS2-ERG fusion with p53 inactivation in prostate cancer pathogenesisR01CA271486 · NCI · MAYO CLINIC ROCHESTER · PI Liewei Wang · 2022 to 2026
$1.8M
Selective RET Kinase and Its Mutant Inhibitors for the Treatment of Medullary Thyroid CancerR01CA197178 · NCI · UNIV OF ARKANSAS FOR MED SCIS · PI LI, HONG-YU, MCDONALD, NEIL · 2015 to 2019
$1.5M
NCI NIH HHS R01 CA130908NCI NIH HHS R01 CA134514NCI NIH HHS R01 CA197178NCI NIH HHS R01 CA249282NCI NIH HHS R01 CA271486
6 · The paper itself

Abstract

In this study, we identified 3-aminophthalic acid as a new ligand of cereblon (CRBN) E3 ubiquitin ligase and developed a phthalic acid-based O'PROTAC for degradation of the ERG transcription factor. This phthalic acid-based O'PROTAC presented an efficacy in degrading ERG comparable to those displayed by pomalidomide-based ERG O'PROTACs. Moreover, phthalic acid-being more chemically stable and economical than classical immunomodulatory drugs (IMiDs)-represents, as a ligand, a new alternative for the development of PROTACs, especially O'PROTACs.

Indexed as

Dose-Response Relationship, DrugHumansLigandsMolecular StructurePhthalic AcidsProteolysisStructure-Activity RelationshipTranscription FactorsUbiquitin-Protein Ligases3-aminophthalateLigandsPhthalic AcidsTranscription FactorsUbiquitin-Protein Ligases

Identifiers

PMID35080528
PMCPMC10467047
OpenAlexW4210467038

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.