Results 131 to 140 of about 823,777 (226)

Design and Synthesis of Novel Candidate CK1δ Proteolysis Targeting Chimeras (PROTACs)

Molecules
Dysregulation of CK1 isoforms is linked to various types of diseases, including neuro-degeneration and different types of neoplasia such as colon-, pancreatic-, breast-, and ovarian cancer. For CK1 isoforms, a plethora of effective small molecule inhibitors are available.
Malte Arnold, Temi Thompson, Lorraine Glennie, Mattes Hollnagel, Gopal Sapkota, Christian Peifer   +5 more
openaire   +2 more sources

TRIM59 Drives Bladder Cancer Progression Through E3 Ligase‐Dependent K48‐Linked Degradation of PTRF

Cancer Science, EarlyView.
Schematic model of TRIM59‐driven BLCA progression through K48‐linked ubiquitination and proteasomal degradation of PTRF, leading to AKT activation and c‐Myc upregulation. ABSTRACT Tripartite motif‐containing 59 (TRIM59) is an E3 ubiquitin ligase implicated in multiple malignancies, but its role in bladder cancer (BLCA) remains incompletely understood ...
Junlin Gan, Xuesong Bai, Aijie Zhang, Fei Lin, Hang Tong, Tinghao Li, Ning Xu, Xinyuan Li, Zhou Yu, Hubin Yin   +9 more
wiley   +1 more source

Progress of proteolysis-targeting chimeras (PROTACs) delivery system in tumor treatment

International Journal of Biological Macromolecules
Proteolysis targeting chimeras (PROTACs) can use the intrinsic protein degradation system in cells to degrade pathogenic target proteins, and are currently a revolutionary frontier of development strategy for tumor treatment with small molecules. However, the poor water solubility, low cellular permeability, and off-target side effects of most PROTACs ...
Lianlian, Fan, Weifang, Tong, Anhui, Wei, Xupeng, Mu   +3 more
openaire   +2 more sources

Chromatin Remodeller BRD9 Orchestrates Odontoblastic Differentiation via Coordinating RUNX2‐KLF4

Cell Proliferation, EarlyView.
During odontoblast lineage commitment, the chromatin remodeller BRD9 acts as a critical epigenetic coordinator, orchestrating the chromatin landscape to facilitate synergistic binding of key transcription factors RUNX2 and KLF4 to target loci for odontogenesis.
Wenrui Zeng, Yuxiu Lin, Yongyan Gao, Delan Huang, Yuanyuan Li, Honglei Ruan, Guohua Yuan, Huan Liu, Zhi Chen   +8 more
wiley   +1 more source

A guide to transcriptional cyclin‐dependent kinases in cancer

The FEBS Journal, EarlyView.
Transcriptional cyclin‐dependent‐kinases (tCDKs) facilitate gene expression by promoting RNA polymerase II (RNAPII) progression through discrete phases of the transcription cycle. Aberrant tCDK activity is detectable in different human cancers, thereby contributing to de‐regulated gene expression programs that drive oncogenic phenotypes.
Jennifer R. Devlin, Salla Kyheröinen, Ricky W. Johnstone   +2 more
wiley   +1 more source

Histone deacetylase inhibitors as venetoclax‐sensitising partners in acute myeloid leukaemia: Mechanisms, pharmacology and translational perspectives

British Journal of Pharmacology, Volume 183, Issue 21, Page 6261-6290, November 2026.
Abstract Venetoclax combined with hypomethylating agents has improved treatment for older or unfit patients with acute myeloid leukaemia (AML), but resistance and relapse remain common. This review analyses the rationale for combining venetoclax with inhibitors of histone deacetylase (HDAC).
Jaebok Lee, Marc Diederich
wiley   +1 more source

Limiting Trial‐and‐Error: Linker‐Based 2D Descriptor Analysis to Support Very Early Proteolysis‐Targeting Chimeras Design

ChemMedChem, Volume 21, Issue 19, 14 October 2026.
Can simple linker descriptors guide PROTAC design? Analysis of matched CRBN‐ and VHL‐recruiting degraders shows that basic 2D linker properties may capture trends linked to degradation efficiency, in vitro ADME and physicochemical properties. A practical approach to reduce trial‐and‐error in early targeted protein degradation programs. Targeted protein
Giulia Apprato, Serena Traversa, Giulia Caron, Giuseppe Ermondi   +3 more
wiley   +1 more source

Targeted Degradation of eEF2K by a Structure‐Guided PROTAC Strategy for the Treatment of Triple‐Negative Breast Cancer

Advanced Science
Proteolysis‐targeting chimera (PROTAC) have emerged as a promising class of anticancer agents. Eukaryotic elongation factor 2 kinase (eEF2K), a stress‐responsive regulator of translational elongation, has emerged as a pivotal therapeutic target in triple‐
Shijun Cao, Changxin Zhong, Shilong Jiang, Yungui Li, Yang Xi, Mingxuan Xiao, Ting Jiang, Xiaoya Wan, Zonglin Chen, Xiaohui Yu, Yan Cheng   +10 more
doaj   +1 more source

Synthesis and Activity‐Based Protein Profiling Identifies Aldo‐Keto Reductase 1C3 as Target Protein of Myxoglucamides

Angewandte Chemie International Edition, Volume 65, Issue 41, 5 October 2026.
Myxoglucamide A—a novel glycolipopeptide isolated from myxobacteria—was synthesized, and activity‐based protein profiling identified aldo‐keto reductase 1C3 (AKR1C3) as its main target in human cells. Structure‐activity relationship studies, together with biophysical characterization and X‐ray crystallography, elucidated the structural basis of AKR1C3 ...
Thomas Siemon, Vivek K. Mishra, Mingming Zhao, Konrad Büssow, Alexander Popoff, Chengzhang Fu, Rolf Müller, Lothar Jänsch, Wulf Blankenfeldt, Mark Brönstrup   +9 more
wiley   +1 more source

Arginine methylation as a regulatory ratchet in cancer: From substrate selection to malignant‐state stabilization

Molecular Oncology, Volume 20, Issue 10, Page 2466-2489, October 2026.
Arginine methylation can be viewed as a persistence‐prone post‐translational modification regulated by a network of PRMTs. Competitive and compensatory interactions among PRMTs can redistribute methylation across substrate pools shaped by sequence, structural, spatial, and environmental layers, reinforcing RNA‐processing, chromatin, and signaling ...
So Hyun Kwon, Ji Min Lee
wiley   +1 more source