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Nightly index of recent papers from PubMed, bioRxiv, and medRxiv. Filters are designed for both researcher precision and patient-friendly navigation.

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Cholangiocarcinoma

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2 papersSorted by most recent
Discovery and Preclinical Evaluations of Potent, Selective, and Allosteric Covalent WRN Inhibitors with Improved PK Properties.
ACS medicinal chemistry letters • 2026-02-12 • DOI: 10.1021/acsmedchemlett.5c00787
Peer-reviewedImpact 68

Topics

Not listed

Modality

Targeted therapy, Imaging

Study type

Lab / Preclinical

Abstract

Werner syndrome helicase (WRN) has received significant interest due to its implication as a synthetic lethal target in microsatellite instability-high (MSI-H) cancers. Here we report the discovery of a novel allosteric covalent WRN inhibitor, compound 22 , via structure-based medicinal design and pharmacokinetic optimization…

Authors

Zhaobing Xu, Qi Xiao, Yong Liu, Wen Jiang +7

AI-generated summary

Discovery and Preclinical Evaluations of Potent, Selective, and Allosteric Covalent WRN Inhibitors with Improved PK Properties. reports: Werner syndrome helicase (WRN) has received significant interest due to its implication as a synthetic lethal target in microsatellite instability-high (MSI-H) cancers. Here we report the discovery of a novel allosteric covalent WRN inhibitor, compound 22 , via structure-based medicinal design and pharmacokinetic optimization from VVD-214. Compound 22 occupied a new cavity and formed an additional hydrogen bond with K894, thereby improving its activities.

This summary may be inaccurate. Verify with the primary paper.

Primary source: PubMed.

Peer-reviewedImpact 69

Topics

Treatment, Biology / Mechanism, Outcomes / Survival, Prevention / Risk

Modality

Immunotherapy, Cell therapy, Imaging

Study type

Review / Meta-analysis

Abstract

The development of endometrial cancer is a gradual malignant transformation process driven by multiple factors, and the immune microenvironment is closely related to clinical outcomes and immunotherapy responses. Under physiological conditions, the immune microenvironment of the normal endometrium undergoes periodic reshaping under the regulation…

Authors

Yingying Peng, Guanglei Zhong, Minqi Zhou, Yuwei Yao +8

AI-generated summary

The dysregulation of the immune microenvironment during endometrial intraepithelial neoplasia serves as a marker of endometrial carcinogenesis. reports: The development of endometrial cancer is a gradual malignant transformation process driven by multiple factors, and the immune microenvironment is closely related to clinical outcomes and immunotherapy responses. Under physiological conditions, the immune microenvironment of the normal endometrium undergoes periodic reshaping under the regulation of estrogen and progesterone, maintaining the balance between immune defense and reproductive capacity. However, continuous exposure to risk factors, such as non-antagonistic estrogen, may trigger endometrial intraepithelial neoplasia.

This summary may be inaccurate. Verify with the primary paper.

Primary source: PubMed.