Results 91 to 100 of about 14,786 (290)

Selectivity on-target of bromodomain chemical probes by structure-guided medicinal chemistry and chemical biology [PDF]

, 2016
Targeting epigenetic proteins is a rapidly growing area for medicinal chemistry and drug discovery. Recent years have seen an explosion of interest in developing small molecules binding to bromodomains, the readers of acetyl-lysine modifications.
Alessio Ciulli, Carles Galdeano, Chiang C-M, Lejeune P   +3 more
core   +2 more sources

Understanding and Overcoming Antibody‐Drug Conjugate Resistance: Biological Mechanisms and Emerging Analytical Frameworks in Breast Cancer

Advanced Science, EarlyView.
Antibody–drug conjugates (ADCs) transform breast cancer therapy, yet resistance limits their durability. Emerging evidence reveals that ADC failure is not solely tumor‐intrinsic but shaped by dynamic tumor–microenvironment interactions that alter drug delivery, processing, and response.
Minji Seo, Jangsoon Lee, Naoto T. Ueno
wiley   +1 more source

Halofuginone is a Molecular Glue Degrader of Integrin β4

Advanced Science, EarlyView.
Integrin β4 overexpression is linked to aggressive tumors and poor prognosis, but targeted therapies are lacking. We identified halofuginone (HF) as a molecular glue degrader that promotes integrin β4 degradation via the CRL4BWDR18 E3 ligase. HF suppresses tumor progression in vitro and in vivo, offering a new strategy for targeting oncogenic ...
Wei Gong, Di Yang, Junrui Tian, Yufei Chai, Tiantian Yu, Qingnan Wu, Yan Wang, Weimin Zhang, Qimin Zhan   +8 more
wiley   +1 more source

Development of a novel PROTAC using the nucleic acid aptamer as a targeting ligand for tumor selective degradation of nucleolin

Molecular Therapy: Nucleic Acids, 2022
PROteolysis TArgeting Chimeras (PROTACs) induce targeted protein degradation by hijacking the intracellular ubiquitin proteasome system, thus emerging as a new strategy for drug development.
Lin Zhang, Ling Li, Xia Wang, Huimin Liu, Yibin Zhang, Tiantian Xie, Hui Zhang, Xiaodong Li, Tianhuan Peng, Xing Sun, Jing Dai, Jing Liu, Wencan Wu, Mao Ye, Weihong Tan   +14 more
doaj   +1 more source

Design and applications of bifunctional small molecules: Why two heads are better than one [PDF]

, 2008
Induction of protein−protein interactions is a daunting challenge, but recent studies show promise for small molecules that specifically bring two or more protein molecules together for enhanced or novel biological effect.
Aberle, Nicholas, Corson, Timothy W., Crews, Craig M   +2 more
core   +1 more source

Potent and Selective IGF‐IIR‐Recruiting Bifunctional Molecules for Targeted Lysosomal Degradation of Extracellular and Membrane Proteins

Advanced Science, EarlyView.
Lysosome‐targeting chimeras (LYTACs) enable degradation of extracellular and membrane proteins via lysosomal trafficking. We report a novel IGF‐II mutant (Del1–7, Y27L) that selectively engages IGF‐IIR while avoiding IGF‐IR and IR‐A. mutIGF‐II–based LYTACs enhance target internalization and degradation and support a genetically encodable, all‐protein ...
Yuan Zhao, Yaxian Liao, Pengyun Li, Regina Stasser de Gonzalez, Xuankun Chen, Nicholas S. Nieto, Florence M. Brunel, Nick Cox, Joseph Stock, Matthew McHenry, Guangsen Fu, Penghsuan Huang, Wenxin Wu, Deqin Cai, Lingjun Li, Alexander N. Zaykov, Weiping Tang   +16 more
wiley   +1 more source

Development and Evaluation of Liposomal Celastrol-PROTACs for Treating Triple-Negative Breast Cancer

Pharmaceuticals
Background: Based on our previous study, Celastrol-based proteolysis-targeting chimeras (Celastrol-PROTACs) were shown to induce apoptosis in 4T1 cells by selectively degrading GRP94 and CDK1/4 through the endogenous ubiquitin–proteasome system. However,
Xuebin Li, Chaoqun Yu, Gongyi Zheng, Yanghong Li, Weiguo Cao, Fan Wang   +5 more
doaj   +1 more source

Characteristic roadmap of linker governs the rational design of PROTACs

Acta Pharmaceutica Sinica B
Proteolysis targeting chimera (PROTAC) technology represents a groundbreaking development in drug discovery, leveraging the ubiquitin‒proteasome system to specifically degrade proteins responsible for the disease.
Yawen Dong, Tingting Ma, Ting Xu, Zhangyan Feng, Yonggui Li, Lingling Song, Xiaojun Yao, Charles R Ashby, Ge-fei Hao   +8 more
semanticscholar   +1 more source

Androgen Receptor‐Induced Lactoferrin Accelerates Prostate Tumorigenesis Through Modulating Ferroptosis

Advanced Science, EarlyView.
This study demonstrates that transcription factor androgen receptor (AR) directly binds the LF promoter, driving lactoferrin overexpression to promote ferritin (FTH1/FTL) upregulation and inhibit p53‐ALOX12‐mediated ferroptosis in prostate cancer. Lactoferrin could be a new potential therapeutic target in prostate cancer.
Can Liu, Qiu Peng, Xiaoyue Zhang, Zhengshuo Li, Yangge Wu, Yuqing Wen, Run Zheng, Shuanglong Wu, Chenfei Zhou, Zhengyu Hu, Lanjun Shu, Xinyi Ma, Qiuyang Li, Ya Ma, Chunlin Ou, Ming Zhao, Songqing Fan, Lingyu Wei, Jian Ma   +18 more
wiley   +1 more source

Sequential responsive nano-PROTACs for precise intracellular delivery and enhanced degradation efficacy in colorectal cancer therapy

Signal Transduction and Targeted Therapy
PROteolysis TArgeting Chimeras (PROTACs) have been considered the next blockbuster therapies. However, due to their inherent limitations, the efficacy of PROTACs is frequently impaired by limited tissue penetration and particularly insufficient cellular ...
Liuqing Yang, Ye Yang, Jing Zhang, Minghui Li, Long Yang, Xinglin Wang, Meifang Chen, Hua Zhang, Bing He, Xueqing Wang, Wenbing Dai, Yiguang Wang, Qiang Zhang   +12 more
semanticscholar   +1 more source