Results 31 to 40 of about 823,777 (226)

Proteolysis targeting chimeras (PROTACs) for epigenetics research

Current Opinion in Chemical Biology, 2020
Proteolysis targeting chimeras (PROTACs) are heterobifunctional molecules and allow selective protein degradation by addressing the natural ubiquitin proteasome system. As this new strategy of chemically induced protein degradation can serve as a biological tool and provides new possibilities for drug discovery, it has been applied to a variety of ...
Anja Vogelmann, Dina Robaa, Wolfgang Sippl, Manfred Jung   +3 more
openaire   +3 more sources

Proteolysis targeting chimeras (PROTACs) are emerging therapeutics for hematologic malignancies [PDF]

Journal of Hematology & Oncology, 2020
AbstractProteolysis targeting chimeras (PROTACs) are heterobifunctional small molecules that utilize the ubiquitin proteasome system (UPS) to degrade proteins of interest (POI). PROTACs are potentially superior to conventional small molecule inhibitors (SMIs) because of their unique mechanism of action (MOA, i.e., degrading POI in a sub-stoichiometric ...
Yonghan He, Sajid Khan, Zhiguang Huo, Dongwen Lv, Xuan Zhang, Xingui Liu, Yaxia Yuan, Robert Hromas, Mingjiang Xu, Guangrong Zheng, Daohong Zhou   +10 more
openaire   +3 more sources

Current Status of Oligonucleotide-Based Protein Degraders

Pharmaceutics, 2023
Transcription factors (TFs) and RNA-binding proteins (RBPs) have long been considered undruggable, mainly because they lack ligand-binding sites and are equipped with flat and narrow protein surfaces. Protein-specific oligonucleotides have been harnessed
Po-Chang Shih, Miyako Naganuma, Yosuke Demizu, Mikihiko Naito   +3 more
doaj   +1 more source

Proteolysis-Targeting Chimeras (PROTACs) in Cancer Therapy: Present and Future

Molecules, 2022
The PROteolysis TArgeting Chimeras (PROTACs) is an innovative technique for the selective degradation of target proteins via the ubiquitin–proteasome system. Compared with traditional protein inhibitor drugs, PROTACs exhibit advantages in the efficacy and selectivity of and in overcoming drug resistance in cancer therapy, providing new insights into ...
Rui Li, Miao Liu, Zhenya Yang, Jiao Li, Yuxin Gao, Ruirong Tan   +5 more
openaire   +3 more sources

PROteolysis TArgeting Chimeras (PROTACs) as emerging anticancer therapeutics

Oncogene, 2020
Using PROteolysis TArgeting Chimeras (PROTACs) to degrade proteins that are important for tumorigenesis has emerged as a potential therapeutic strategy for cancer. PROTACs are heterobifunctional molecules consisting of one ligand for binding to a protein of interest (POI) and another to an E3 ubiquitin (E3) ligase, connected via a linker.
Sajid Khan, Yonghan He, Xuan Zhang, Yaxia Yuan, Shaoyan Pu, Qingpeng Kong, Guangrong Zheng, Daohong Zhou   +7 more
openaire   +3 more sources

Radiotherapy-Triggered Proteolysis Targeting Chimera Prodrug Activation in Tumors

, 2022
Proteolysis targeting chimera (PROTAC) is an emerging protein degradation strategy, which shows excellent advantages in targeting those so-called “undruggable” proteins.
Yujie Li (294983), Jinghong Li (219583), Chunrong Yang (294274), Yujie Li, Qiankun Ni, Yuchen Yang, Chunrong Yang, Jinghong Li, Yuchen Yang (21709), Qiankun Ni (8574846)   +9 more
core   +1 more source

Small-Molecule PROTACs for Cancer Immunotherapy

Molecules, 2022
Unsatisfactory physicochemical properties of macromolecular drugs seriously hinder their application in tumor immunotherapy. However, these problems can be effectively solved by small-molecule compounds.
Zefan Liu, Yajun Zhang, Yucheng Xiang, Xin Kang   +3 more
doaj   +1 more source

In Situ Bioorthogonal Synthesis of PROTACs via Dual-Responsive Cleavage for Synergistic Photo-Immunotherapy. [PDF]

Adv Sci (Weinh)
A bioactive self‐delivering SNAP‐TAC platform responds to tumor‐associated cathepsin B and glutathione, enabling in situ bioorthogonal synthesis of a BRD4‐degrading proteolysis‐targeting chimera within the tumor microenvironment. The resulting BRD4 degradation and PD‐L1 downregulation synergize with photodynamic therapy‐induced immunogenic cell death ...
Jian S, Wu J, Xu F, Zuo Y, Shen H, Ji R, Wang L, Li N, Sun Y, Yu Y, Shi Y, Hu H, Xu F, Huang D, Hu X.   +14 more
europepmc   +2 more sources

Newly Emerging Strategies in Antiviral Drug Discovery: Dedicated to Prof. Dr. Erik De Clercq on Occasion of His 80th Anniversary

Molecules, 2022
Viral infections pose a persistent threat to human health. The relentless epidemic of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has become a global health problem, with millions of infections and fatalities so far.
Shujing Xu, Dang Ding, Xujie Zhang, Lin Sun, Dongwei Kang, Boshi Huang, Xinyong Liu, Peng Zhan   +7 more
doaj   +1 more source

Proteolysis Targeting Chimeras (PROTACs) of Anaplastic Lymphoma Kinase (ALK) [PDF]

European Journal of Medicinal Chemistry, 2018
Anaplastic lymphoma kinase (ALK) activation has been associated with many types of human cancer. Significant efforts have been devoted to the development of ALK inhibitors to antagonize the kinase activity of ALK. Four ALK inhibitors have been approved by the FDA to date for treating patients with ALK-positive non-small cell lung cancers (NSCLC ...
Chengwei Zhang, Xiao-Ran Han, Xiaobao Yang, Biao Jiang, Jing Liu, Yue Xiong, Jian Jin   +6 more
openaire   +2 more sources