Evidence map›Paper›PMID 41982730›Full record

ArticleACS medicinal chemistry letters2026

Repurposing Ilaprazole as a PP5 TPR Domain Binder with Modulatory Effects on MAPK Signaling.

Yanyi He, Jinying Gu, Liwen Hua, Daichao Zhai, Qifei Huang, Jiayue Pei, Qidong You, Qiuyue Zhang, Lei Wang

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

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

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0citing papers in PubMed
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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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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

9 authors.

Yanyi HeState Key Laboratory of Natural Medicines and Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009, China.
Jinying GuState Key Laboratory of Natural Medicines and Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009, China.
Liwen HuaDepartment of Pharmacy, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
Daichao ZhaiState Key Laboratory of Natural Medicines and Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009, China.
Qifei HuangState Key Laboratory of Natural Medicines and Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009, China.
Jiayue PeiState Key Laboratory of Natural Medicines and Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009, China.
Qidong YouState Key Laboratory of Natural Medicines and Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009, China.ORCID https://orcid.org/0000-0002-8587-0122
Qiuyue ZhangState Key Laboratory of Natural Medicines and Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009, China.
Lei WangState Key Laboratory of Natural Medicines and Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009, China.ORCID https://orcid.org/0000-0002-8181-5644

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Small-molecule modulators targeting the N-terminal tetratricopeptide repeat (TPR) domain of protein phosphatase 5 (PP5) remain largely unexplored. Here, we report the repurposing of ilaprazole as a PP5 TPR domain binder identified via a fluorescence polarization-based competitive screen. Biophysical assays and molecular docking supported the interaction within the PP5 TPR binding pocket, revealing key structural features distinguishing ilaprazole from related proton pump inhibitors. In KRAS mutant colorectal cancer cells, ilaprazole engaged cellular PP5, leading to reduced RAF stability and suppressed mitogen-activated protein kinase (MAPK) signaling. While exhibiting minimal single-agent effects, ilaprazole sensitized cells to the MEK inhibitor binimetinib. These results validate the PP5 TPR domain as a druggable site and establish ilaprazole as a lead scaffold for pharmacological modulation of PP5-associated MAPK signaling.

Indexed as

combination therapyfluorescence polarization screeningilaprazoleKRAS mutant colorectal cancerMAPK signalingprotein phosphatase 5tetratricopeptide repeat domain

Identifiers

PMID41982730
PMCPMC13071606

What OpenQuestion holds

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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.