Evidence map›Paper›PMID 42068300›Full record

ArticleJournal of medicinal chemistry2026

Intracellular Activation of Dual-Pharmacophore Artezomib Enhances Selective Cytotoxicity in Hematologic Malignancies.

Daqiang Li, Xiangao Huang, Zoe Chow, Jianxiang Ye, Renee Ma, Michael Zhu, David Jayabalan, Hao Zhang, Pengbo Zhou, Selina Chen-Kiang and 2 more

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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

0 citing papers in PubMed.

No citing paper in PubMed yet.

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

12 authors.

Daqiang LiDepartment of Microbiology & Immunology, Weill Cornell Medicine, New York, New York10065, United States.ORCID 0000-0001-8762-3339
Xiangao HuangDepartment of Pathology & Laboratory Medicine, Weill Cornell Medicine, New York, New York10065, United States.
Zoe ChowDepartment of Microbiology & Immunology, Weill Cornell Medicine, New York, New York10065, United States.
Jianxiang YeDepartment of Microbiology & Immunology, Weill Cornell Medicine, New York, New York10065, United States.
Renee MaDepartment of Microbiology & Immunology, Weill Cornell Medicine, New York, New York10065, United States.
Michael ZhuDepartment of Microbiology & Immunology, Weill Cornell Medicine, New York, New York10065, United States.
David JayabalanDepartment of Pathology & Laboratory Medicine, Weill Cornell Medicine, New York, New York10065, United States.
Hao ZhangDepartment of Microbiology & Immunology, Weill Cornell Medicine, New York, New York10065, United States.ORCID 0000-0002-1187-5844
Pengbo ZhouDepartment of Pathology & Laboratory Medicine, Weill Cornell Medicine, New York, New York10065, United States.
Selina Chen-KiangDepartment of Pathology & Laboratory Medicine, Weill Cornell Medicine, New York, New York10065, United States.
Ruben NiesvizkyDepartment of Pathology & Laboratory Medicine, Weill Cornell Medicine, New York, New York10065, United States.
Gang LinDepartment of Microbiology & Immunology, Weill Cornell Medicine, New York, New York10065, United States.ORCID 0000-0003-4797-7073

Funding

Project 3: Targeting PRMT5 in Mantle Cell LymphomaP01CA214274 · NCI · WEILL MEDICAL COLL OF CORNELL UNIV · PI BAIOCCHI, ROBERT ALAN · 2018 to 2022
$8.9M
Hijacking Plasmodium ubiquitin-proteasome system to defeat drug resistanceR01AI177635 · NIAID · WEILL MEDICAL COLL OF CORNELL UNIV · PI Gang Lin · 2023 to 2026
$3.1M
Novel proteasome inhibitors targeting both beta5 and beta2 subunits for treatment of triple negative breast cancerR01CA276053 · NCI · WEILL MEDICAL COLL OF CORNELL UNIV · PI Gang Lin · 2024 to 2026
$1.9M
NCI NIH HHS P01 CA214274NCI NIH HHS R01 CA276053NIAID NIH HHS R01 AI177635
6 · The paper itself

Abstract

We describe DQ-9, a dual-pharmacophore artezomib analogue that combines selective inhibition of immunoproteasome β5i with iron-dependent activation of artemisinin. DQ-9 exploits the elevated labile iron pool characteristic of hematologic malignancies, yielding selective cytotoxicity toward leukemia and multiple myeloma cells. DQ-9 affords sustained proteasome inhibition and induces oxidative stress and apoptosis through its iron-mediated activation and subsequent intracellular conversion to additional inhibitory species. In contrast, the deoxy analogue DQ-10, which lacks this activatable component, displays activity attributable solely to β5i inhibition, with correspondingly reduced cytotoxic potency. These findings establish iron-activable, β5i-targeting hybrids as a promising strategy to achieve enhanced selectivity and therapeutic efficacy against hematological malignancies.

Indexed as

Antineoplastic AgentsArtemisininsHematologic NeoplasmsProteasome InhibitorsPyrrolesApoptosisCell Line, TumorDrug Screening Assays, AntitumorHumansIronOxidative StressProteasome Endopeptidase ComplexStructure-Activity RelationshipAntineoplastic AgentsArtemisininsIronProteasome Endopeptidase ComplexProteasome InhibitorsPyrroles

Identifiers

PMID42068300
PMCPMC13177615

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.