Evidence map›Paper›PMID 40784515›Full record

ArticleBioorganic & medicinal chemistry letters2025

Novel small molecule analogs for advancing apelin receptor antagonism with enhanced plasma and microsomal stability.

Ganesh Bist, Ahmed Elsheikh, Sewon Kim, Ruea-Yea Huang, Donna Ruszaj, Sukyung Woo, Youngjae You

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 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

7 authors.

Ganesh BistDepartment of Pharmaceutical Sciences, The State University of New York at Buffalo, Buffalo, NY 14214, USA.
Ahmed ElsheikhDepartment of Pharmaceutical Sciences, The State University of New York at Buffalo, Buffalo, NY 14214, USA.
Sewon KimDepartment of Pharmaceutical Sciences, The State University of New York at Buffalo, Buffalo, NY 14214, USA.
Ruea-Yea HuangDepartment of Pharmaceutical Sciences, The State University of New York at Buffalo, Buffalo, NY 14214, USA.
Donna RuszajDepartment of Pharmaceutical Sciences, The State University of New York at Buffalo, Buffalo, NY 14214, USA.
Sukyung WooDepartment of Pharmaceutical Sciences, The State University of New York at Buffalo, Buffalo, NY 14214, USA. Electronic address: skwoo@buffalo.edu.
Youngjae YouDepartment of Pharmaceutical Sciences, The State University of New York at Buffalo, Buffalo, NY 14214, USA. Electronic address: yjyou@buffalo.edu.

Funding

Site Specific Drug Delivery with Light-responsive Conjugates for Photo-biomodulationR01GM113940 · NIGMS · UNIVERSITY OF OKLAHOMA HLTH SCIENCES CTR · PI Youngjae You · 2015 to 2026
$3.0M
Targeting ovarian cancer spheroid formation and metabolic adaptation by APJ inhibitionR01CA258546 · NCI · STATE UNIVERSITY OF NEW YORK AT BUFFALO · PI Sukyung Woo · 2022 to 2026
$2.0M
NCI NIH HHS R01 CA258546NIGMS NIH HHS R01 GM113940
6 · The paper itself

Abstract

The apelin receptor (APJ), a G protein-coupled receptor, has emerged as a promising therapeutic target in oncology due to its role in tumor growth, angiogenesis, metastasis, and resistance to anti-VEGF therapy. However, ML221, the only reported small-molecule APJ antagonist, exhibits extremely poor plasma (<1 % remaining after 1 h) and liver microsomal (t

Indexed as

Apelin ReceptorsMicrosomes, LiverSmall Molecule LibrariesDose-Response Relationship, DrugHumansMolecular StructureStructure-Activity RelationshipApelin ReceptorsAPLNR protein, humanSmall Molecule LibrariesApelin receptor (APJ)APJ antagonistML221 analogsPlasma and liver microsomal stabilityStructure-activity relationship (SAR)Sulfonate linkageβ-arrestin inhibition

Identifiers

PMID40784515
PMCPMC12569688

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Registered trials

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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.