Evidence map›Paper›PMID 40145447›Full record

ArticleJournal of medicinal chemistry2025

Potent and Selective Human Constitutive Androstane Receptor Activator DL5055 Facilitates Cyclophosphamide-Based Chemotherapies.

Dongdong Liang, Linhao Li, Yong Ai, Zhihui Li, William D Hedrich, Srilatha Sakamuru, Caitlin Lynch, Wenbo Yu, Ismael Watts-Ouattara, Scott Heyward and 4 more

Abstract read
PubMed Full text at PMC Publisher
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. 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

14 authors.

Dongdong LiangDepartment of Pharmaceutical Sciences, University of Maryland School of Pharmacy, 20 Penn Street, Baltimore, Maryland 21201, United States.
Linhao LiDepartment of Pharmaceutical Sciences, University of Maryland School of Pharmacy, 20 Penn Street, Baltimore, Maryland 21201, United States.
Yong AiDepartment of Pharmaceutical Sciences, University of Maryland School of Pharmacy, 20 Penn Street, Baltimore, Maryland 21201, United States.
Zhihui LiDepartment of Pharmaceutical Sciences, University of Maryland School of Pharmacy, 20 Penn Street, Baltimore, Maryland 21201, United States.
William D HedrichDepartment of Pharmaceutical Sciences, University of Maryland School of Pharmacy, 20 Penn Street, Baltimore, Maryland 21201, United States.
Srilatha Sakamuru9800 Medical Center Drive, National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, Maryland 20892, United States.ORCID 0000-0002-9693-1832
Caitlin Lynch9800 Medical Center Drive, National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, Maryland 20892, United States.
Wenbo YuDepartment of Pharmaceutical Sciences, University of Maryland School of Pharmacy, 20 Penn Street, Baltimore, Maryland 21201, United States.
Ismael Watts-OuattaraDepartment of Pharmaceutical Sciences, University of Maryland School of Pharmacy, 20 Penn Street, Baltimore, Maryland 21201, United States.ORCID 0009-0005-5375-5639
Scott HeywardBioIVT, 1450 S Rolling Rd, Halethorpe, Maryland 21227, United States.
Menghang Xia9800 Medical Center Drive, National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, Maryland 20892, United States.ORCID 0000-0001-7285-8469
Alexander D MacKerellDepartment of Pharmaceutical Sciences, University of Maryland School of Pharmacy, 20 Penn Street, Baltimore, Maryland 21201, United States.ORCID 0000-0001-8287-6804
Hongbing WangDepartment of Pharmaceutical Sciences, University of Maryland School of Pharmacy, 20 Penn Street, Baltimore, Maryland 21201, United States.ORCID 0000-0002-6224-6888
Fengtian XueDepartment of Pharmaceutical Sciences, University of Maryland School of Pharmacy, 20 Penn Street, Baltimore, Maryland 21201, United States.ORCID 0000-0002-4132-9887

Funding

Macromolecular Conformational HeterogeneityR35GM131710 · NIGMS · UNIVERSITY OF MARYLAND BALTIMORE · PI ALEXANDER D MACKERELL · 2019 to 2026
$6.2M
Novel noncanonical actions of CAR in human LiverR01CA262084 · NCI · UNIVERSITY OF MARYLAND BALTIMORE · PI WANG, HONGBING · 2021 to 2025
$2.0M
Function and Regulation of SLC13A5 in the LiverR01GM121550 · NIGMS · UNIVERSITY OF MARYLAND BALTIMORE · PI WANG, HONGBING · 2018 to 2021
$1.3M
Role of constitutive androstane receptor in cyclophosphamide-based chemotherapyR01GM107058 · NIGMS · UNIVERSITY OF MARYLAND BALTIMORE · PI WANG, HONGBING · 2013 to 2016
$1.2M
NCI NIH HHS R01 CA262084NIGMS NIH HHS R01 GM107058NIGMS NIH HHS R01 GM121550NIGMS NIH HHS R35 GM131710
6 · The paper itself

Abstract

Enhancement of the metabolic conversion of cyclophosphamide (CPA) increases its therapeutic effects. Activation of the human constitutive androstane receptor (hCAR) induces CYP2B6, a key enzyme responsible for CPA bioactivation. Based on our previous hCAR activator DL5016, we designed and synthesized a series of new hCAR activators. Compared to DL5016, three new compounds

Indexed as

CyclophosphamideReceptors, Cytoplasmic and NuclearAnimalsConstitutive Androstane ReceptorCytochrome P-450 CYP2B6HepatocytesHumansMiceMice, TransgenicStructure-Activity RelationshipXenograft Model Antitumor AssaysConstitutive Androstane ReceptorCyclophosphamideCYP2B6 protein, humanCytochrome P-450 CYP2B6Receptors, Cytoplasmic and Nuclear

Identifiers

PMID40145447
PMCPMC12239146

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.