Results 21 to 30 of about 11,341 (256)

PROTACs in gastrointestinal cancers

Molecular Therapy - Oncolytics, 2022
Proteolysis targeting chimera (PROTAC) presents a powerful strategy for targeted protein degradation (TPD). The heterobifunctional PROTAC molecule consists of an E3 ligase ligand covalently linked to a protein of interest (POI) via a linker. PROTAC can induce ubiquitinated proteasomal degradation of proteins by hijacking the ubiquitin-proteasome ...
Yu Chen, Qingfan Yang, Jinrun Xu, Liyao Tang, Yan Zhang, Fukuan Du, Yueshui Zhao, Xu Wu, Mingxing Li, Jing Shen, Ruilin Ding, Hongying Cao, Wanping Li, Xiaobing Li, Meijuan Chen, Zhigui Wu, Chi Hin Cho, Yu Du, Qinglian Wen, Zhangang Xiao   +19 more
openaire   +3 more sources

Degradation of proteins by PROTACs and other strategies

Acta Pharmaceutica Sinica B, 2020
Blocking the biological functions of scaffold proteins and aggregated proteins is a challenging goal. PROTAC proteolysis-targeting chimaera (PROTAC) technology may be the solution, considering its ability to selectively degrade target proteins.
Yang Wang, Xueyang Jiang, Feng Feng, Wenyuan Liu, Haopeng Sun   +4 more
doaj   +1 more source

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

Sci Data
Proteolysis-targeting chimeras (PROTAC) are emerging and promising molecules for targeted protein degradation which have the potential to overcome critical bottlenecks in traditional small molecule drug development. However, the scarcity of publicly available data on molecular compound structures has significantly hindered computational drug discovery ...
Cai H, Yao G, Shi Y, Zhang T, Hu Y.
europepmc   +3 more sources

From classic medicinal chemistry to state‐of‐the‐art interdisciplinary medicine: Recent advances in proteolysis‐targeting chimeras technology

Interdisciplinary Medicine, 2023
Proteolysis‐targeting chimeras (PROTACs) is a targeted protein degradation (TPD) technique effected by hijacking the ubiquitin‐proteasome system (UPS) of the cells.
Xuyang Zhao, Yifan Chen, Huang Su, Liqin Zhang   +3 more
doaj   +1 more source

Novel approaches for the rational design of PROTAC linkers

Exploration of Targeted Anti-tumor Therapy, 2020
Proteolysis targeting chimeras (PROTACs) represent a promising class of hetero-bivalent molecules that facilitate ubiquitination of a target protein by simultaneously binding and bringing together both the E3 enzyme and the target.
Almaz Zagidullin, Vasili Milyukov, Albert Rizvanov, Emil Bulatov   +3 more
doaj   +1 more source

PROTAC-Design-Evaluator (PRODE): An Advanced Method for In-Silico PROTAC Design

ACS Omega, 2023
Abstract PROTAC (proteolysis-targeting chimeras) is a rapidly evolving technology to target undruggable targets. The mechanism by which this happens is when a bifunctional molecule binds to a target protein and also brings in proximity an E3 ubiquitin ligase to trigger ubiquitination and degradation of the target protein.
Ben Geoffrey A S, Deepak Agrawal, Nagaraj M. Kulkarni, Rajappan Vetrivel, Kishan Gurram   +4 more
openaire   +3 more sources

Development of Protacs to Target Cancer-promoting Proteins for Ubiquitination and Degradation [PDF]

, 2003
The proteome contains hundreds of proteins that in theory could be excellent therapeutic targets for the treatment of human diseases. However, many of these proteins are from functional classes that have never been validated as viable candidates for the ...
Crews, Craig M., Deshaies, Raymond J., Kim, Kyung B., Ransick, Andy, Sakamoto, Kathleen M., Stein, Bernd, Verma, Rati   +6 more
core   +1 more source

BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design [PDF]

, 2019
Targeting subunits of BAF/PBAF chromatin remodeling complexes has been proposed as an approach to exploit cancer vulnerabilities. Here, we develop proteolysis targeting chimera (PROTAC) degraders of the BAF ATPase subunits SMARCA2 and SMARCA4 using a ...
Arnhof, Heribert, Bader, Gerd, Boehmelt, Guido, Ciulli, Alessio, Dank, Christian, Diers, Emelyne, Ehrenhöfer-Wölfer, Katharina, Ettmayer, Peter, Farnaby, William, Galant, Michael, Gerstberger, Thomas, Gmaschitz, Teresa, Greb, Peter, Karolyi-Oezguer, Jale, Koegl, Manfred, McConnell, Darryl B., Owen-Hughes, Tom, Pearson, Mark, Petermann, Oliver, Riedmueller, Carina, Rinnenthal, Joerg, Roy, Michael J., Rumpel, Klaus, Schnitzer, Renate, Sharps, Bernadette, Steurer, Steffen, Trainor, Nicole, Traxler, Elisabeth, Wachter, Johannes, Weinstabl, Harald, Weiss-Puxbaum, Alexander, Whitworth, Claire, Wiechens, Nicola, Wu, Meng-Ying, Wöhrle, Simon, Zoephel, Andreas, Zollman, David   +36 more
core   +2 more sources

BRD4-targeting PROTAC as a unique tool to study biomolecular condensates

Cell Discovery, 2023
Biomolecular condensates play key roles in various biological processes. However, specific condensation modulators are currently lacking. PROTAC is a new technology that can use small molecules to degrade target proteins specifically.
Yi Shi, Yuan Liao, Qianlong Liu, Zhihao Ni, Zhenzhen Zhang, Minglei Shi, Pilong Li, Haitao Li, Yu Rao   +8 more
doaj   +1 more source

FAK PROTAC Inhibits Ovarian Tumor Growth and Metastasis by Disrupting Kinase Dependent and Independent Pathways

Frontiers in Oncology, 2022
Focal adhesion kinase (FAK) is highly expressed in a variety of human cancers and is a target for cancer therapy. Since FAK kinase inhibitors only block the kinase activity of FAK, they are not highly effective in clinical trials. FAK also functions as a
Xueyun Huo, Xueyun Huo, Xueyun Huo, Wenjing Zhang, Guannan Zhao, Guannan Zhao, Zhenwen Chen, Peixin Dong, Hidemichi Watari, Ramesh Narayanan, Ramesh Narayanan, Todd D. Tillmanns, Lawrence M. Pfeffer, Lawrence M. Pfeffer, Junming Yue, Junming Yue   +15 more
doaj   +1 more source