Results 11 to 20 of about 11,335 (243)

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

A region-confined PROTAC nanoplatform for spatiotemporally tunable protein degradation and enhanced cancer therapy

Nature Communications
The antitumor performance of PROteolysis-TArgeting Chimeras (PROTACs) is limited by its insufficient tumor specificity and poor pharmacokinetics. These disadvantages are further compounded by tumor heterogeneity, especially the presence of cancer stem ...
Jing Gao, Xingyu Jiang, Shumin Lei, Wenhao Cheng, Yi Lai, Min Li, Lei Yang, Peifeng Liu, Xiao-hua Chen, Min Huang, Haijun Yu, Huixiong Xu, Zhiai Xu   +12 more
doaj   +2 more sources

Drugtamer‐PROTAC Conjugation Strategy for Targeted PROTAC Delivery and Synergistic Antitumor Therapy

Advanced Science
Proteolysis‐targeting chimeras (PROTACs) have emerged as a promising strategy for targeted protein degradation and drug discovery. To overcome the inherent limitations of conventional PROTACs, an innovative drugtamer‐PROTAC conjugation approach is ...
Shipeng He, Yuxin Fang, Yaojin Zhu, Ziyang Ma, Guoqiang Dong, Chunquan Sheng   +5 more
doaj   +3 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
  +8 more sources

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, Dongsheng Cao, Junbo Gao, Xiaowu Dong, Qiaojun He, Bo Yang, Dan Li, Jian Wu, Tingjun Hou   +9 more
openaire   +2 more sources

PROTAC targeted protein degraders: the past is prologue

Nature reviews. Drug discovery, 2022
Targeted protein degradation (TPD) is an emerging therapeutic modality with the potential to tackle disease-causing proteins that have historically been highly challenging to target with conventional small molecules.
M. Békés, D. Langley, C. Crews
semanticscholar   +1 more source

Frontiers in PROTACs

Drug Discovery Today, 2021
Targeting protein-protein interactions (PPI) is a key focus in the development of new and emerging small-molecule therapeutics. Shallow interacting surfaces can render PPI targeting notoriously difficult. This leaves many therapeutically captivating targets 'undruggable'.
Gregory R. Hughes, Ashley P. Dudey, Andrew M. Hemmings, Andrew Chantry   +3 more
openaire   +4 more sources

PROTAC-DB 2.0: an updated database of PROTACs

Nucleic Acids Research, 2022
AbstractProteolysis targeting chimeras (PROTACs), which harness the ubiquitin-proteasome system to selectively induce targeted protein degradation, represent an emerging therapeutic technology with the potential to modulate traditional undruggable targets.
Gaoqi Weng, Xuanyan Cai, Dongsheng Cao, Hongyan Du, Chao Shen, Yafeng Deng, Qiaojun He, Bo Yang, Dan Li, Tingjun Hou   +9 more
openaire   +2 more sources

PROTAC-PatentDB: A PROTAC Patent Compound Dataset. [PDF]

Sci Data
Cai H, Yao G, Shi Y, Zhang T, Hu Y.
europepmc   +2 more sources

Non-small molecule PROTACs (NSM-PROTACs): Protein degradation kaleidoscope

Acta Pharmaceutica Sinica B, 2022
The proteolysis targeting chimeras (PROTACs) technology has been rapidly developed since its birth in 2001, attracting rapidly growing attention of scientific institutes and pharmaceutical companies. At present, a variety of small molecule PROTACs have entered the clinical trial.
Sinan Ma, Jianai Ji, Yuanyuan Tong, Yuxuan Zhu, Junwei Dou, Xian Zhang, Shicheng Xu, Tianbao Zhu, Xiaoli Xu, Qidong You, Zhengyu Jiang   +10 more
openaire   +3 more sources