Results 151 to 160 of about 11,341 (256)

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

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

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

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

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

Contemporary Applications of Chemical Libraries for Drug Discovery and Methods for Their Synthesis

ChemistryEurope, Volume 4, Issue 5, May 2026.
Screening of chemical libraries has over the past decades become a cornerstone of drug discovery. Today, a broad range of chemical libraries exist but they are often not well described in terms of diversity. This review describes current efforts which aim to visualize chemical diversity in compound collections and discuss current trends in synthetic ...
Tobias N. Hansen, Nils J. V. Hansen
wiley   +1 more source

TMEM92 shields DDX3X from TTC3‐mediated degradation to confer chemoresistance in triple‐negative breast cancer

Clinical and Translational Medicine, Volume 16, Issue 5, May 2026.
TMEM92 protects DDX3X from degradation by the E3 ligase TTC3, promoting TNBC cell proliferation and tumour growth. Depleting TMEM92 not only suppresses tumour growth but also sensitises cells to cisplatin, suggesting that targeting this axis is a potential therapeutic strategy.
Hao Shen, Xiaochao Jia, Xu Li, Zhi Li, Zhihua Zhang, Yang Zhao, Lei Shen, Xiaoqiu Bu, Qiang Ma, Chunli Liang, Xiaoti Lin, Lin‐Xiaoxi Ma, Chuan Qin   +12 more
wiley   +1 more source

CDK6 inactivation counteracts CALR‐mutant‐induced MPN evolution and sensitizes MPN stem cells to interferon‐α treatment

HemaSphere, Volume 10, Issue 5, May 2026.
Abstract Interferon‐α (IFNα) remains a potent therapeutic option for myeloproliferative neoplasms (MPNs) with an activated JAK/STAT signaling axis. However, variable patient responses highlight the need for optimized combination strategies. Recent studies suggest a link between cyclin‐dependent kinase 6 (CDK6) and IFN signaling.
Brian Ringhofer, Wolfram Polzer, Michaela Prchal‐Murphy, Eszter Doma, Sebastian Kollmann, Elisabeth Gamper, Jonatan Kendler, Belinda S. Maw, Eva Zebedin‐Brandl, Juan Li, Anthony R. Green, Maria‐Theresa Krauth, Emir Hadzijusufovic, Daniel Ivanov, Peter Valent, Gregor Hoermann, Thorsten Klampfl, Veronika Sexl, Karoline Kollmann   +18 more
wiley   +1 more source

From Platelet Toxicity to Precision Targeting: Evolving Strategies to Overcome Thrombocytopenia in BCL‐2/BCL‐XL Inhibition

Health Science Reports, Volume 9, Issue 5, May 2026.
ABSTRACT Background Simultaneous blockade of the anti‐apoptotic proteins BCL‐2 and BCL‐XL has been shown to be efficacious in preclinical and clinical trials for tumors that are co‐dependent on their survival pathways, although clinical development has been limited owing to dose‐limiting thrombocytopenia associated with BCL‐XL inhibition.
Md Mohiuddin
wiley   +1 more source