Evidence map›Paper›PMID 40765086›Full record

ArticleCurrent pharmaceutical design2026

Cholesterol-Lowering Effects of BMS-303141 Analogues via Inhibition of Adenosine Triphosphate-Citrate Lyase.

In-Gyu Je, Joon-Tae Park, Hyeong Jun Lee, A-Rang Im, Jaecheol Lee, Ki-Young Kim

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Article in Current pharmaceutical design, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing 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

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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

1 citing paper in PubMed.

  1. New insights into the ACLY-mediated metabolic and epigenetic interplay in macrophages.Journal of enzyme inhibition and medicinal chemistry · 2026
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4 · The record

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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

6 authors.

In-Gyu JeResearch Laboratories, Ildong Pharmaceutical Co., Ltd, Hwaseong-si, 18449, Republic of Korea.ORCID 0000-0003-3530-340X
Joon-Tae ParkYunovia Co., Ltd, Hwaseong-si, 18449, Republic of Korea.ORCID 0000-0003-1862-8560
Hyeong Jun LeeResearch Laboratories, Ildong Pharmaceutical Co., Ltd, Hwaseong-si, 18449, Republic of Korea.ORCID 0009-0003-6815-1841
A-Rang ImYunovia Co., Ltd, Hwaseong-si, 18449, Republic of Korea.ORCID 0000-0002-2819-1932
Jaecheol LeeSchool of Pharmacy, Sungkyunkwan University, Suwon-si, 16419, Republic of Korea.ORCID 0000-0002-2070-7463
Ki-Young KimGraduate School of Biotechnology, Kyung Hee University, Yongin-si, 17104, Republic of Korea.ORCID 0000-0002-0407-3018

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

backgroundCholesterol is considered a major factor contributing to cardiovascular diseases. Statins, the most commonly prescribed cholesterol-lowering drugs, are known to have various limitations. Inhibition of Adenosine Triphosphate-Citrate Lyase (ACLY) has been proposed as an alternative therapeutic strategy for managing hypercholesterolemia by lowering cholesterol levels. This has led to the discovery of a cell-permeable small molecule ACLY inhibitor.

methodsACLY enzyme activity was assessed using an ACLY Assay Kit with the ADP-Glo Kinase Assay Kit. HepG2 cells were treated with test compounds to demonstrate cholesterol and fatty acid synthesis. Pharmacokinetic studies were performed on CD-1 mice following a single oral dose of the compounds. Hypercholesterolemia was induced in mice through a High-Fat and High Cholesterol Diet (HFHCD), and drugs were administered orally for six weeks. Serum and hepatic lipid profiles were subsequently analyzed.

resultsTo increase the pharmacochemical properties, four analogues of BMS-303141, ID0018, ID0023, ID0085, and ID0106, were designed and synthesized. These compounds showed superior ACLY inhibitory activity and dose-dependent suppression of cholesterol and fatty acid synthesis in HepG2 cells. Among the analogues, ID0085 exhibited the most potent ACLY inhibition (IC DISCUSSION: Among the synthesized analogues, ID0085 exhibited the most potent ACLY inhibition, superior pharmacokinetic properties, and significant improvements in both serum and hepatic cholesterol profiles compared to BMS-303141.

conclusionBased on the results, ID0085 appears to be the most promising therapeutic candidate for the treatment of hypercholesterolemia.

Indexed as

Anticholesteremic AgentsATP Citrate (pro-S)-LyaseCholesterolEnzyme InhibitorsHypercholesterolemiaAnimalsDiet, High-FatDose-Response Relationship, DrugHep G2 CellsHumansMaleMiceStructure-Activity RelationshipAnticholesteremic AgentsATP Citrate (pro-S)-LyaseCholesterolEnzyme Inhibitorsadenosine triphosphate-citrate lyase inhibitorBempedoic acidBMS-303141HepG2 cellhigh-fat and high-cholesterol dietHypercholesterolemia

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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.