Results 61 to 70 of about 11,335 (243)

PROTAC the protein [PDF]

Science-Business eXchange, 2012
GSK and Yale researchers have announced a collaboration to develop a platform that selectively tags disease-associated proteins with an E3 ubiquitin ligase ligand, thus targeting them to a cell's protein degradation machinery. GSK hopes the platform could be a cornerstone for a new Discovery Performance Unit at the pharma and the partners are aiming to
openaire   +1 more source

RIPK3 Orchestrates Scar‐Associated Macrophage Dysfunction to Drive Pulmonary Fibrosis

Advanced Science, EarlyView.
Beyond signaling cell death, RIPK3 emerges as a critical metabolic regulator in pulmonary fibrosis. This research reveals that RIPK3 promotes PI3K‐AKT signaling in scar‐associated macrophages to fuel polyamine synthesis, independent of its kinase activity.
Tao Yang, Xiao Li, Shuyue Lei, Qingqing Li, Yi Zhang, Zhizhen Hui, Jinjin Ren, Xuelian Yang, Xiaoqian Yang, Chunlan Feng, Yousheng Xu, Dongxin Zhao, Wei Tang   +12 more
wiley   +1 more source

A novel ROR1-targeting antibody-PROTAC conjugate promotes BRD4 degradation for solid tumor treatment

Theranostics
Rationale: Proteolysis Targeting Chimeras (PROTACs) are bifunctional compounds that have been extensively studied for their role in targeted protein degradation (TPD).
Lei Wang, Yong Ke, Qunye He, Pameila Paerhati, Weiliang Zhuang, Yali Yue, Junjun Liu, Jiawei Zhang, Lulu Huang, Qiang Yin, Huifang Zong, Jianwei Zhu, Baohong Zhang   +12 more
semanticscholar   +1 more source

Protacs for Treatment of Cancer [PDF]

Pediatric Research, 2010
Protein degradation is the cell's mechanism of eliminating misfolded or unwanted proteins. The pathway by which proteins are degraded occurs through the ubiquitin-proteasome system. Ubiquitin is a small 9-kD (kDa) protein that is attached to proteins. A minimum of four ubiquitins are required for proteins to be recognized by the degradation machinery ...
openaire   +2 more sources

Coacervate‐Mediated Lysosome‐Targeting Antibody Delivery for Protein Degradation

Advanced Science, EarlyView.
Targeting coacervates to the lysosome in the cytoplasm is a challenge. Here, we convert a tetrapeptide into lysosome‐targeting, membrane‐translocating coacervates. The lysosome‐sorting peptide coacervates facilitate coacervate‐mediated delivery of antibody antigen complexes and a PROTAC compound to the lysosome for the targeted degradation of cancer ...
Dingdong Yuan, Yishu Bao, Zhiyi Xu, Zhong Zheng, Yongxu Han, Kai Cheng, Yuan‐Di Zhao, Jiang Xia   +7 more
wiley   +1 more source

From PROTAC to TPD: Advances and Opportunities in Targeted Protein Degradation

Pharmaceuticals
PROTAC is a rapidly developing engineering technology for targeted protein degradation using the ubiquitin–proteasome system, which has promising applications for inflammatory diseases, neurodegenerative diseases, and malignant tumors. This paper gives a
Siqi Wang, Fuchu He, Chunyan Tian, Aihua Sun   +3 more
doaj   +1 more source

Proteasomal and lysosomal degradation for specific and durable suppression of immunotherapeutic targets

Cancer Biology & Medicine, 2020
Cancer immunotherapy harness the body’s immune system to eliminate cancer, by using a broad panel of soluble and membrane proteins as therapeutic targets.
Yungang Wang, Shouyan Deng, Jie Xu
doaj   +1 more source

De Novo Design of an Androgen Receptor DNA Binding Domain‐Targeted peptide PROTAC for Prostate Cancer Therapy

Advanced Science, 2022
Androgen receptor splice variant‐7 (AR‐V7), one of the major driving factors, is the most attractive drug target in castration‐resistant prostate cancer (CRPC). Currently, no available drugs efficiently target AR‐V7 in clinical practice.
Bohan Ma, Yizeng Fan, Dize Zhang, Yi Wei, Yanlin Jian, Donghua Liu, Zixi Wang, Yang Gao, Jian Ma, Yule Chen, Shan Xu, Lei Li   +11 more
doaj   +1 more source

Linker-Determined Folding and Hydrophobic Interactions Explain a Major Difference in PROTAC Cell Permeability

ACS Medicinal Chemistry Letters
The ability to adopt folded conformations that have a low solvent-accessible 3D polar surface area has been found to be important for PROTACs to display a high passive cell permeability. We have studied two VHL PROTACs that differ only by the replacement
Vasanthanathan Poongavanam, Stefan Peintner, Y. Abeje, Florian Kölling, D. Meibom, M. Erdélyi, Jan Kihlberg   +6 more
semanticscholar   +1 more source

Targeted Degradation of eEF2K by a Structure‐Guided PROTAC Strategy for the Treatment of Triple‐Negative Breast Cancer

Advanced Science, EarlyView.
This study developed an eEF2K‐targeting PROTAC, A6, that efficiently degrades eEF2K in TNBC cells, inhibiting tumor growth in vitro and in vivo. To enhance tumor‐specific delivery, we engineered A6@ZIF‐8, a pH‐sensitive nanocarrier, which improved drug accumulation at tumor sites, offering a promising therapeutic strategy for TNBC through targeted ...
Shijun Cao, Changxin Zhong, Shilong Jiang, Yungui Li, Yang Xi, Mingxuan Xiao, Ting Jiang, Xiaoya Wan, Zonglin Chen, Xiaohui Yu, Yan Cheng   +10 more
wiley   +1 more source