Results 161 to 170 of about 14,786 (290)

An Update on Clinically Advanced PROTAC Degraders and Their Synthesis

Molecules
Proteolysis-targeting chimeras (PROTACs) have emerged as a revolutionary therapeutic modality that enables degradation of therapeutically relevant proteins through the protein disposal machinery, the ubiquitin-proteasome system (UPS).
Ranjan Kumar Acharyya, Yugandhar Kothapalli, Suresh Yarlagadda, Chayan K. De, Srinivasa Rao Allu, Joyeeta Roy, Rohan Kalyan Rej   +6 more
doaj   +1 more source

Targeting EZH2 in Cancer: From Molecular Mechanisms to Clinical Translation

MedComm – Oncology, Volume 5, Issue 2, June 2026.
The abnormal overexpression or gain‐of‐function mutations of EZH2 play a significant role in cancer occurrence and progression, highlighting the importance and potential of EZH2 as a cancer biomarker. Therefore, screening for effective and safe small‐molecule inhibitors, degraders, and natural compounds targeting EZH2 through preclinical cancer models ...
Xi Zhong, Jieni Li, Mingxuan Pan, Xiaoxue Ke, Hongjuan Cui   +4 more
wiley   +1 more source

Protocol for constructing tumor-targeting ANM-PROTACs for degradation of transcription factors

STAR Protocols
Summary: AS1411-NCL-MDM2-based proteolysis-targeting chimeras (ANM-PROTACs) are capable of inducing selective degradation of transcription factors (TFs) in tumor cells. Here, we present a protocol for constructing ANM-PROTACs.
Jin Li, Chao Liang
doaj   +1 more source

PTMs of PD-1/PD-L1 and PROTACs application for improving cancer immunotherapy

Frontiers in Immunology
Immunotherapy has been developed, which harnesses and enhances the innate powers of the immune system to fight disease, particularly cancer. PD-1 (programmed death-1) and PD-L1 (programmed death ligand-1) are key components in the regulation of the ...
Xiaohui Ren, Lijuan Wang, Likun Liu, Juan Liu   +3 more
semanticscholar   +1 more source

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

British Journal of Pharmacology, Volume 183, Issue 11, Page 2675-2694, June 2026.
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

Coacervate‐Mediated Lysosome‐Targeting Antibody Delivery for Protein Degradation

Advanced Science, Volume 13, Issue 25, 4 May 2026.
Targeting coacervates to the lysosome in the cytoplasm is a challenge. Here, we convert a tetrapeptide into lysosome‐targeting, membrane‐translocating coacervates. The lysosome‐sorting peptide coacervates facilitate coacervate‐mediated delivery of antibody antigen complexes and a PROTAC compound to the lysosome for the targeted degradation of cancer ...
Dingdong Yuan, Yishu Bao, Zhiyi Xu, Zhong Zheng, Yongxu Han, Kai Cheng, Yuan‐Di Zhao, Jiang Xia   +7 more
wiley   +1 more source

Discovery of an LSD1 PROTAC degrader

Proceedings of the National Academy of Sciences
Aberrant expression of lysine-specific demethylase 1 (LSD1) has been implicated in various cancers, including acute myeloid leukemia (AML). Recent studies have revealed both catalytic and noncatalytic oncogenic functions of LSD1, which cannot be effectively addressed by traditional small-molecule inhibitors.
Amir Hosseini, Xing Qiu, Yan Xiong, Ki Him Nicholas Chiang, Jerrel Catlett, Ines Kaltheuner, Zhijie Deng, Sudipta Ghosh, Yang Shi, Jian Jin   +9 more
openaire   +2 more sources

G4‐Ligand‐Directed PROTACs Unveil DR1 as a Novel Ligand‐Co‐Binding G4‐Protein and Reshape G4‐Dependent Transcription

Advanced Science, Volume 13, Issue 27, 13 May 2026.
G4‐binding proteins (G4BPs) that specifically co‐bind G4s in the presence of small‐molecule ligands represent a critical but unexplored class of proteins. We introduce G4‐Ligand‐Directed PROTACs (G4L‐TACs), a chemical platform that couples G4 ligands (PDS) to E3 recruiters to selectively degrade these ligand‐co‐binding G4BPs.
Mao‐Lin Li, Shu‐Min Xu, Xin‐Chen Jiang, Le‐Tian Dai, Yu‐Tao Hu, Kai‐Bo Wang, Jia‐Heng Tan, Zhi‐Shu Huang, Shuo‐Bin Chen   +8 more
wiley   +1 more source

Deacetylase inhibitors CM‐444 and CM‐1758 enhance chemotherapy response in AML via ALOX5

British Journal of Haematology, EarlyView.
Naroa Gimenez‐Camino, Edurne San José‐Enériz, Leire Garate, Estibaliz Miranda, Elena Sáez, Antonio Pineda‐Lucena, Felipe Prósper, Xabier Agirre   +7 more
wiley   +1 more source

Cucurbit[7]uril‐Based Plug‐and‐Play Platform on Bacterial Surfaces for Constructing Functional Supramolecular Biohybrids

Aggregate, Volume 7, Issue 5, May 2026.
This study establishes a supramolecular “plug‐and‐play” platform on bacterial surfaces via cucurbit[7]uril host–guest chemistry. The platform successfully generates functional biohybrids for fluorescence imaging, drug delivery, and in vivo bioorthogonal catalysis, demonstrating its potential for functional living materials with broad biomedical ...
Fang Huang, Jun Zhu, Bingfa Wu, Xinyuan Sun, Linghong Huang, Yiliu Liu   +5 more
wiley   +1 more source