Results 101 to 110 of about 11,335 (243)

Fenofibrate potentiates the therapeutic efficacy of EZH2 inhibitors on melanoma via TRIM21‐ and OTUD4‐mediated EZH2 ubiquitination

British Journal of Pharmacology, EarlyView.
Background and Purpose EZH2 (enhancer of zeste homologue 2) inhibitors are an emerging class of drugs that target epigenetic regulation. However, their efficacy in solid tumours has been limited, partly due to drug‐induced upregulation of fatty acid synthesis.
Rui Cheng, Yuanjun Tang, Xuedi Cao, Xiaotong Yu, Zhanya Huang, Yunyun Guo, Renjing Jin, Yan Wang, Yang Liu, Lixiang Xue, Yuqing Wang   +10 more
wiley   +1 more source

Targeting protein–protein interactions with reversible covalent modalities: Non‐cysteine chemistries

British Journal of Pharmacology, EarlyView.
Abstract Protein–protein interactions (PPIs) are central to diverse cellular functions, and represent a rapidly expanding class of therapeutic targets. Advancements in covalent drug design have enabled small‐molecule drugs to overcome challenges associated with engaging these targets, such as limited durations of action and difficult‐to‐drug (expansive,
Ruchira Basu, Steven Fletcher
wiley   +1 more source

Clinical Applications of Phosphoproteomics: Illuminating Cancer Signaling and Enabling Rational Therapeutic Strategies

Cancer Science, EarlyView.
Mass spectrometry‐based phosphoproteomics for mechanistic dissection of cancer signaling pathways and uncovering therapeutic vulnerabilities. ABSTRACT Protein phosphorylation is a central post‐translational modification regulating cellular signaling, frequently dysregulated in cancer.
Hirokazu Shoji, Narikazu Boku, Jun Adachi   +2 more
wiley   +1 more source

Lock, relax, load, and shoot: a molecular perspective on Nedd4 regulation

The FEBS Journal, EarlyView.
Structural basis of inactive and active states of the Nedd4 HECT E3 ligase subfamily, following a ‘lock, relax, load, and shoot’ mechanism. In the locked, autoinhibited state, intramolecular domain interactions restrain the HECT domain. Relaxation releases these restraints, allowing loading of ubiquitin onto the catalytic cysteine, followed by the ...
Masa Janosev, Tomas Obsil, Veronika Obsilova   +2 more
wiley   +1 more source

Dual targeting and bioresponsive nano-PROTAC induced precise and effective lung cancer therapy

Journal of Nanobiotechnology
Epigenetic regulation has emerged as a promising therapeutic strategy for lung cancer treatment, which can facilitate the antitumor responses by modulating epigenetic dysregulation of target proteins in lung cancer.
Xiaoling Guan, Xiaowei Xu, Yiwen Tao, Xiaohua Deng, Linlong He, Zhongxiao Lin, Jishuo Chang, Jionghua Huang, Dazhi Zhou, Xiyong Yu, Minyan Wei, Lingmin Zhang   +11 more
semanticscholar   +1 more source

Extracellular and Membrane Protein: Structure, Biological Functions, Diseases, and an Emerging Modality for Drug Discovery

MedComm, Volume 7, Issue 4, April 2026.
Targeted protein degradation represents a paradigm shift from traditional protein inhibition to complete protein elimination. This is achieved through three main strategies for degrading extracellular and membrane proteins: recruitment of cell‐surface LTRs, engagement of intracellular proteins, and receptor‐independent mechanisms.
Mengqing Zhao, Wenhao Yin, Jianjian Han, Huimin Wang, Zheng Liu, Lilong Liu, Wuxiang Mao   +6 more
wiley   +1 more source

An engineered DNA aptamer-based PROTAC for precise therapy of p53-R175H hotspot mutant-driven cancer.

Science Bulletin
Targeting oncogenic mutant p53 represents an attractive strategy for cancer treatment due to the high frequency of gain-of-function mutations and ectopic expression in various cancer types.
Lingping Kong, F. Meng, Ping Zhou, Ruixin Ge, Xiaoshan Geng, Zhihao Yang, Guo Li, Linlin Zhang, Jing Wang, Jinfeng Ma, Cheng Dong, Jun Zhou, Sijin Wu, Diansheng Zhong, Songbo Xie   +14 more
semanticscholar   +1 more source

Enhancing Oncolytic Adenovirus Replication by Early Region 1A Protein‐Mediated Degradation of E1A Binding Protein p300

MedComm, Volume 7, Issue 4, April 2026.
E1A is an important protein for adenovirus to initiate viral replication. Previous reports have shown that E1A binds to p300 as a regulatory factor. However, our study provides a new perspective that E1A promotes oncolytic adenovirus replication by degrading p300.
Boduan Xiao, Qingzhe Yang, Shichuan Hu, Jianchuan Hu, Zhongbing Qi, Yao Zhang, Yu Qin, Ping Cheng   +7 more
wiley   +1 more source

Self‐Immolative Systems in Diagnostic and Therapeutic Applications

ChemMedChem, Volume 21, Issue 5, 13 March 2026.
Self‐Immolative Systems enable the precise, residue‐free release of active molecules, drugs, probes, or sensors, via cyclization or elimination, triggered by specific stimuli. Their versatility drives advances in drug delivery, diagnostics, nanotechnology, materials chemistry, and biosensing, offering chemists control over molecular activation and ...
Windbedema Prisca Ouédraogo, Thomas Cailly, Valérie Collot   +2 more
wiley   +1 more source

Bumped pomalidomide-based PROTACs

Communications Chemistry
Pomalidomide is an E3 ligase recruiter exploited by PROTACs to degrade target proteins, but its application is hampered by the off-target degradation of other vital endogenous zinc finger (ZF) proteins. Now, the off-target ZF binding of pomalidomide-based PROTACs is evaluated by a high-throughput imaging screening platform, and minimization of off ...
openaire   +3 more sources