Results 51 to 60 of about 8,212 (230)

Dual targeting of EZH2 and PD-L1 in Burkitt’s lymphoma enhances immune activation and induces apoptotic pathway

Frontiers in Immunology
IntroductionEnhancer of zeste homolog 2 (EZH2) catalyzes H3K27me3, an epigenetic modification linked to gene silencing, and its overexpression contributes to the progression of hematological malignancies.
Yurim Jeong, Hyewon Jang, Se Been Kim, Minseo Yu, Ra Eun Kim, Wan-Su Choi, Youngwoo Jeon, Jung-Yeon Lim   +7 more
doaj   +1 more source

Targeted Degradation of Picornaviral 3C Protease via PROTACs Confers High Barrier to Viral Resistance and Broad‐Spectrum Antiviral Activity

Advanced Science, EarlyView.
This study reports D34 as the first PROTAC degrader that targets the 3C protease of picornaviruses. D34 effectively degrades EV71 3C protease via the ubiquitin‐proteasome pathway. More importantly, D34 exhibits a high resistance barrier and shows broad‐spectrum antiviral activity against multiple picornaviruses, highlighting its potential as a novel ...
Weilong Deng, Junyu Chen, Yingyue Pang, Yuanyuan Zhang, Siqian Chen, Guoliang You, Xiaoman Tian, Zhongxin Xu, Jing Wang, Luqing Shang   +9 more
wiley   +1 more source

PROTACs: The Future of Leukemia Therapeutics

Frontiers in Cell and Developmental Biology, 2022
The fight to find effective, long-lasting treatments for cancer has led many researchers to consider protein degrading entities. Recent developments in PROteolysis TArgeting Chimeras (PROTACs) have signified their potential as possible cancer therapies.
Anwar, Zubair, Ali, Muhammad Shahzad, Galvano, Antonio, Perez, Alessandro, La Mantia, Maria, Bukhari, Ihtisham, Swiatczak, Bartlomiej   +6 more
openaire   +5 more sources

Trafficking Deficiency of TMEM175 Variants in Parkinson's Disease Pathogenesis and the Prospects of Precision Medicine

Advanced Science, EarlyView.
This study identifies that the PD‐associated TMEM175‐L156P variant disrupts lysosomal ion channel trafficking by causing aberrant endoplasmic reticulum retention. A “chaperone–agonist” bifunctional small molecule restores TMEM175‐L156P lysosomal localization and channel function, thereby alleviating PD‐relevant cellular phenotypes and highlighting a ...
Ting Luo, Yu He, Shuyao Li, Haoyu Guan, Ruili Cui, Yu Shi, Zhongwen Jiang, Siyu Wang, Xuan Li, Jiyuan Li, Mei Hu, Yupeng Zhou, Beisha Tang, Yanyan Zhang, Zhaobing Gao, Yu Zhou, Zhenhua Liu, Ping Li   +17 more
wiley   +1 more source

Interpretable PROTAC Degradation Prediction With Structure‐Informed Deep Ternary Attention Framework

Advanced Science
Proteolysis Targeting Chimeras (PROTACs) are heterobifunctional ligands bridging Proteins‐Of‐Interest (POIs) and E3 ligases for ubiquitin‐proteasome degradation, promising to target the ‘undruggable’.
Zhenglu Chen, Chunbin Gu, Shuoyan Tan, Xiaorui Wang, Yuquan Li, Mutian He, Ruiqiang Lu, Shijia Sun, Chang‐Yu Hsieh, Xiaojun Yao, Huanxiang Liu, Pheng‐Ann Heng   +11 more
doaj   +1 more source

A Single‐Amino‐Acid Ligand for LAT1: A Minimalist and Modular Platform for Lysosome‐Targeted Degradation of Membrane Proteins

Advanced Science, EarlyView.
LA‐LYTAC repurposes the cancer‐enriched amino acid transporter LAT1 as a lysosomal trafficking receptor for targeted membrane‐protein degradation. A single phenylalanine‐derived ligand, modularly linked to antibodies or small‐molecule binders, recruits PD‐L1, EGFR, or integrins to LAT1, triggering transporter‐mediated internalization, lysosomal ...
Liquan Zhu, Ke Liu, Haotian Liu, Chaoqi He, Xiaozhen Liu, Xin Zeng, Misha Mao, Yuxiao Mu, Ying Li, Qinghui Zheng, Hongchao Tang, Da Qian, Xuli Meng   +12 more
wiley   +1 more source

PROTAC the protein [PDF]

Science-Business eXchange, 2012
GSK and Yale researchers have announced a collaboration to develop a platform that selectively tags disease-associated proteins with an E3 ubiquitin ligase ligand, thus targeting them to a cell's protein degradation machinery. GSK hopes the platform could be a cornerstone for a new Discovery Performance Unit at the pharma and the partners are aiming to
openaire   +1 more source

Targeting Excessively Accumulated Pathological Tau: PROTAC Molecular Design Strategies and Challenges

Shengwu huaxue yu shengwu wuli jinzhan
The abnormal accumulation, structural change, and spread of tau protein in the brain are now considered important factors in the progression of Alzheimer’s disease (AD) and many other tau-related neurodegenerative diseases.
LI Han, LEI Yi-Qiao, FANG Tian, DING Yi, WU Zhong-Hui, XU Jia   +5 more
doaj   +1 more source

Repurposing a Small Molecule Plant Hormone as a Tunable ON‐Switch for CAR‐T Cell Immunotherapy

Advanced Science, EarlyView.
By engineering a receptor system integrating the plant auxin receptor AFB1 with its co‐receptor IAA7, we enable ligand‐dependent interactions triggered by the plant hormone auxins. This design allows rapid, reversible, and dose‐dependent T cell activation, resulting in potent cytotoxicity against B‐cell lymphoma in vitro and in vivo.
Hongxiang Zeng, Lei Zheng, Rongkun Tao, Sirui Zheng, Yanke Zhong, Yongxia Niu, Peng Zhang, Xiang Ma, Chen Yang, Min Zhang, Fuyu Duan, Jing Yang, Xuan Wei, Xiang Zhou, Zhenbiao Yang, Zhaoxi Sun, Qizhou Lian   +16 more
wiley   +1 more source

Design and development of PROTACs: A new paradigm in anticancer drug discovery

Medicine in Drug Discovery
PROTAC (Proteolysis targeting chimera) is a potential revolutionary strategy in cancer drug development focusing on their ability to target specific receptors like androgen and BRD4, which are vital for the progression and development of several cancers.
Vishal Mathur, Mukund Jha, Iqra Zai, Moksh Mahajan, Shagufi Nazar, Shaheen Ali, Anam Ilyas, Sana Tanweer, Javed Ali, Ozair Alam   +9 more
doaj   +1 more source