Evidence map›Paper›PMID 40672683›Full record

ArticleACS pharmacology & translational science2025

Targeting of a Bile Acid Receptor, Takeda G Protein Receptor 5 [TGR5], by a Novel First-in-Class Competitive Antagonist, SBI-364, Diminishes Hepatic and Renal Cystogenesis in Polycystic Liver and Kidney Disease.

Tetyana Masyuk, Anatoliy Masyuk, Christy Trussoni, Maria Lorenzo-Pisarello, Robert Ardecky, Anthony Pinkerton, Edward Sergienko, Steven Olson, Jiwen Zou, Santhi Reddy Ganji and 13 more

Abstract read
In one paragraph

Article in ACS pharmacology & translational science, 2025. 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

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

1 citing paper in PubMed.

  1. Review
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

23 authors.

Tetyana MasyukMayo Clinic College of Medicine and Science, Rochester, Minnesota 55905, United States.
Anatoliy MasyukMayo Clinic College of Medicine and Science, Rochester, Minnesota 55905, United States.
Christy TrussoniMayo Clinic College of Medicine and Science, Rochester, Minnesota 55905, United States.
Maria Lorenzo-PisarelloMayo Clinic College of Medicine and Science, Rochester, Minnesota 55905, United States.
Robert ArdeckyConrad Prebys Center for Chemical Genomics at Sanford-Burnham Prebys Medical, Discovery Institute, La Jolla, California 92307, United States.
Anthony PinkertonConrad Prebys Center for Chemical Genomics at Sanford-Burnham Prebys Medical, Discovery Institute, La Jolla, California 92307, United States.
Edward SergienkoConrad Prebys Center for Chemical Genomics at Sanford-Burnham Prebys Medical, Discovery Institute, La Jolla, California 92307, United States.
Steven OlsonConrad Prebys Center for Chemical Genomics at Sanford-Burnham Prebys Medical, Discovery Institute, La Jolla, California 92307, United States.
Jiwen ZouConrad Prebys Center for Chemical Genomics at Sanford-Burnham Prebys Medical, Discovery Institute, La Jolla, California 92307, United States.
Santhi Reddy GanjiConrad Prebys Center for Chemical Genomics at Sanford-Burnham Prebys Medical, Discovery Institute, La Jolla, California 92307, United States.
Bryan KramerConrad Prebys Center for Chemical Genomics at Sanford-Burnham Prebys Medical, Discovery Institute, La Jolla, California 92307, United States.
Krystine VuongConrad Prebys Center for Chemical Genomics at Sanford-Burnham Prebys Medical, Discovery Institute, La Jolla, California 92307, United States.
She-Chia JankowskiConrad Prebys Center for Chemical Genomics at Sanford-Burnham Prebys Medical, Discovery Institute, La Jolla, California 92307, United States.
Chen-Ting MaConrad Prebys Center for Chemical Genomics at Sanford-Burnham Prebys Medical, Discovery Institute, La Jolla, California 92307, United States.
John HolleranConrad Prebys Center for Chemical Genomics at Sanford-Burnham Prebys Medical, Discovery Institute, La Jolla, California 92307, United States.
Sirkku PollariConrad Prebys Center for Chemical Genomics at Sanford-Burnham Prebys Medical, Discovery Institute, La Jolla, California 92307, United States.
Brock BrownConrad Prebys Center for Chemical Genomics at Sanford-Burnham Prebys Medical, Discovery Institute, La Jolla, California 92307, United States.
Raghuveer RamachandraConrad Prebys Center for Chemical Genomics at Sanford-Burnham Prebys Medical, Discovery Institute, La Jolla, California 92307, United States.
Thomas ChungConrad Prebys Center for Chemical Genomics at Sanford-Burnham Prebys Medical, Discovery Institute, La Jolla, California 92307, United States.
Carys TurnerMayo Clinic College of Medicine and Science, Rochester, Minnesota 55905, United States.
Olivia MorgenthalerMayo Clinic College of Medicine and Science, Rochester, Minnesota 55905, United States.
Hanako KawashimaMayo Clinic College of Medicine and Science, Rochester, Minnesota 55905, United States.
Nicholas LaRussoMayo Clinic College of Medicine and Science, Rochester, Minnesota 55905, United States.ORCID https://orcid.org/0000-0003-3266-0831

Funding

The Development of TGR5 Antagonists for the Treatment of CholangiopathiesR01DK117133 · NIDDK · SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTE · PI LARUSSO, NICHOLAS F., OLSON, STEVEN H · 2019 to 2022
$2.0M
NIDDK NIH HHS R01 DK117133
6 · The paper itself

Abstract

Polycystic kidney disease (PKD) and associated polycystic liver disease (PLD) are genetic disorders with limited therapeutic options. In this work, we report SBI-364, a novel first in-class competitive antagonist of a G protein-coupled bile acid receptor, Takeda G protein receptor 5 (TGR5), as a potent small-molecule compound for concurrent treatment of both PLD and PKD. We found that elevated expression of TGR5 in hepatic epithelial cells (cholangiocytes) and renal epithelial cells (REC) from which cysts originate contributes to disease progression. To pharmacologically reduce TGR5-mediated cystogenesis, we developed a competitive TGR5 antagonist, SBI-364, and demonstrated in

Indexed as

cholangiocytescystogenesispolycystic kidney diseasepolycystic liver diseaseTakeda G protein receptor Five (TGR5)TGR5-competitive antagonist SBI-364

Identifiers

PMID40672683
PMCPMC12261218

What OpenQuestion holds

Textmetadata
LicenceCC BY-NC-ND
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.