Results 11 to 20 of about 14,786 (290)

New-generation advanced PROTACs as potential therapeutic agents in cancer therapy

Molecular Cancer
Proteolysis-targeting chimeras (PROTACs) technology has garnered significant attention over the last 10 years, representing a burgeoning therapeutic approach with the potential to address pathogenic proteins that have historically posed challenges for ...
Chao Wang, Yujing Zhang, Wujun Chen, Yudong Wu, Dongming Xing   +4 more
doaj   +2 more sources

PROTACs: past, present and future.

Chemical Society Reviews, 2022
This review highlights important milestones in the evolution of PROTACs, briefly discusses recent lessons about targeted protein degradation, and conjectures on the efforts still needed to expand the toolbox for PROTAC discovery.
Ke Li, C. Crews
semanticscholar   +3 more sources

PROTAC-DB 3.0: an updated database of PROTACs with extended pharmacokinetic parameters

Nucleic Acids Research
Proteolysis-targeting chimera (PROTAC) is an emerging therapeutic technology that leverages the ubiquitin-proteasome system to target protein degradation.
Jingxuan Ge, Shimeng Li, Gaoqi Weng, Huating Wang, Meijing Fang, Huiyong Sun, Yafeng Deng, Changyu Hsieh, Dan Li, Tingjun Hou   +9 more
semanticscholar   +3 more sources

Dual-Action-Only PROTACs.

Journal of the American Chemical Society
Proteolysis targeting chimera (PROTAC)-based degraders are highly potent pseudocatalytic drugs, but on-target off-site homing could yield undesirable consequences.
Ranit Dutta, Anirudh Devarajan, A. Talluri, Ritam Das, S. Thayumanavan   +4 more
semanticscholar   +3 more sources

mRNA PROTACs: engineering PROTACs for high‐efficiency targeted protein degradation

MedComm
Proteolysis‐targeting chimeras (PROTACs) are essential bifunctional molecules that target proteins of interest (POIs) for degradation by cellular ubiquitination machinery.
Xiaoqi Xue, Chen Zhang, Xiaolin Li, Junqiao Wang, Haowei Zhang, Ying Feng, Naihan Xu, Hongyan Li, Chunyan Tan, Yuyang Jiang, Ying Tan   +10 more
doaj   +3 more sources

Self-assembled PROTACs enable protein degradation to reprogram the tumor microenvironment for synergistically enhanced colorectal cancer immunotherapy

Bioactive Materials
Both β-catenin and STAT3 drive colorectal cancer (CRC) growth, progression, and immune evasion, and their co-overexpression is strongly associated with a poor prognosis.
Xinchen Lu, Jinmei Jin, Ye Wu, Jiayi Lin, Xiaokun Zhang, Shengxin Lu, Jiyuan Zhang, Chunling Zhang, Maomao Ren, Hongzhuan Chen, Weidong Zhang, Xin Luan   +11 more
doaj   +2 more sources

Synthesis, biological evaluation and clinical trials of Cereblon-based PROTACs

Communications Chemistry
PROteolysis-Targeting Chimeras (PROTACs) are an emerging class of molecules capable of inducing a forced approximation between a protein of interest (POI) and an E3 ligase enzyme (e.g., Cereblon), leading to the degradation of the POI by the cell’s own ...
André T. S. Vicente, Sara P. S. P. Moura, Jorge A. R. Salvador   +2 more
doaj   +2 more sources

Linker-free PROTACs efficiently induce the degradation of oncoproteins

Nature Communications
Proteolysis-targeting chimeras (PROTACs) present a potentially effective strategy against various diseases via selective proteolysis. How to increase the efficacy of PROTACs remains challenging.
Jianchao Zhang, Congli Chen, Xiao Chen, Kefan Liao, Fengming Li, Xiaoxiao Song, Chaowei Liu, Ming-Yuan Su, Huiyong Sun, Tingjun Hou, Chris Soon Heng Tan, Lijing Fang, Hai Rao   +12 more
doaj   +2 more sources

Estrogen Receptor-α Targeting: PROTACs, SNIPERs, Peptide-PROTACs, Antibody Conjugated PROTACs and SNIPERs

Pharmaceutics, 2022
Targeting selective estrogen subtype receptors through typical medicinal chemistry approaches is based on occupancy-driven pharmacology. In occupancy-driven pharmacology, molecules are developed in order to inhibit the protein of interest (POI), and their popularity is based on their virtue of faster kinetics.
Arvind Negi, Kavindra Kumar Kesari, Anne Sophie Voisin-Chiret   +2 more
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PROTAC-DB: an online database of PROTACs [PDF]

Nucleic Acids Research, 2020
Abstract Proteolysis-targeting chimeras (PROTACs), which selectively degrade targeted proteins by the ubiquitin-proteasome system, have emerged as a novel therapeutic technology with potential advantages over traditional inhibition strategies.
Gaoqi Weng, Chao Shen 0008, Dong-Sheng Cao 0001, Junbo Gao, Xiaowu Dong, Qiaojun He, Bo Yang 0023, Dan Li 0013, Jian Wu 0001, Tingjun Hou   +9 more
openaire   +2 more sources