Results 81 to 90 of about 823,777 (226)

Near‐Infrared Fluorescent PROTAC Enables Theranostic Imaging and Selective Tau Degradation in Alzheimer's Disease

Advanced Science, EarlyView.
Here, we report a novel NIR fluorescent PROTAC platform that enables real‐time imaging and targeted degradation of Alzheimer's p‐Tau. Our lead compound effectively clears p‐Tau, reduces APP/Aβ, and alleviates cognitive deficits in AD mice. This work demonstrates a theranostic strategy for visualizing degradation and developing next‐generation AD ...
Ziwei Ren, Qian Yue, Ning Gao, Qiu‐Lian Hao, Yan Huo, Chuchu Li, Xinyue Leng, Lu‐Lu Sun, Maggie Pui Man Hoi, Hai‐Hao Han, Mingliang Ma, Xu‐Wen Li   +11 more
wiley   +1 more source

Telomerase Reverse Transcriptase Degradation via a Rationally Designed Covalent Proteolysis Targeting Chimera [PDF]

Expression of telomerase reverse transcriptase (TERT) is a hallmark of cancer, maintaining telomere length and integrity to enable replicative immortality.
Karl, Scheidt, Grant, Frost, Stephen, Kron, Yue, Liu   +3 more
core   +2 more sources

Nano-Proteolysis Targeting Chimeras (Nano-PROTACs) in Cancer Therapy

International Journal of Nanomedicine
Proteolysis-targeting chimeras (PROTACs) are heterobifunctional molecules that have the capability to induce specific protein degradation. While playing a revolutionary role in effectively degrading the protein of interest (POI), PROTACs encounter certain limitations that impede their clinical translation. These limitations encompass off-target effects,
Yue Song, Qing-Qing Dong, Yi-Ke Ni, Xiao-Ling Xu, Chao-Xiang Chen, Wei Chen   +5 more
openaire   +5 more sources

Discovery of a KLHL41 Ligand for Muscle Specific Protein Degradation

Nature Communications
Despite the recent advancement of proteolysis-targeting chimera (PROTAC) development, they remain predominantly dependent on two E3 ligases, CRBN and VHL, which are ubiquitously expressed in all types of cells.
Junhyeong Yim, Jaeseok Lee, Solbi Kim, Jieun Choi, Soyoung Yoon, Hana Cho, Sunbin Jung, GaYeon Yoo, Sanghee Lee, Hankum Park, Juyong Lee, Jongmin Park   +11 more
doaj   +1 more source

PROTAC^® technology and potential for its application in infection control

Тонкие химические технологии
Objectives. To describe the pharmaceutical technology of controlled degradation of protein molecules (PROTAC®, Proteolysis Targeting Chimera), approaches to the design of the PROTAC® molecule, methods of ligand and linker selection and synthesis, as well
M. A. Zakharova, M. V. Chudinov
doaj   +1 more source

Molecular Glue Degraders Enhance CAPRIN1‐Dependent Lysosomal Degradation of APP and Reduce Amyloid β in Alzheimer's Disease

Advanced Science, EarlyView.
A new class of lysosome‐directed molecular glue degraders selectively enhance CAPRIN1–APP interactions, driving APP degradation and reducing amyloid‐β production in human neurons and Alzheimer's disease mouse models. This CAPRIN1‐dependent targeted protein degradation strategy reveals a previously unrecognized therapeutic approach for disrupting the ...
Sunghan Jung, Xu Wang, Bin Liu, Raktim Roy, Nancy Jaiswal, Ratan K. Rai, Yuichiro Takagi, Cen Gao, Lifan Zeng, Ho‐Yin Lo, Reagan K. Wohlford, Ryan K. Higgins, Bruce T. Lamb, Anantha Shekhar, Anita C. Bellail, Chunhai Hao   +15 more
wiley   +1 more source

Bridged Proteolysis Targeting Chimera (PROTAC) Enables Degradation of Undruggable Targets

Proteolysis Targeting Chimeras (PROTACs) are attractive therapeutic modalities for degrading disease-causing proteins. While many PROTACs have been developed for numerous protein targets, current small-molecule PROTAC approaches cannot target undruggable
Hyerin Yim (9740528), Kwang-Su Park (10151730), Xiaobao Yang (2313229), Xian Chen (107385), Yue Zhong (1285050), Xiaoran Han (8299770), Yan Xiong (197517), Ling Xie (2026981), Jing Liu (38537), Poulikos I. Poulikakos (13265292), Jian Jin (351142)   +10 more
core   +1 more source

Targeted Lysosomal Degradation of Extracellular and Membrane Proteins: From Receptor Hijacking to Programmable Endolysosomal Routing

Advanced Science, EarlyView.
Targeted chimeric degraders engage extracellular or membrane proteins and endocytosable cell‐surface receptors, forming ternary complexes that induce receptor‐mediated internalization. Following endocytosis, post‐endocytic sorting—not internalization alone—determines target fate.
Ke Liu, Xiyan Wang, Xiaozhen Liu, Chaoqi He, Da Qian, Xuli Meng, Liquan Zhu   +6 more
wiley   +1 more source

Discovery of Selective Proteolysis-Targeting Chimera Degraders Targeting PTP1B as Long-Term Hypoglycemic Agents

PTP1B, a promising target for insulin sensitizers in type 2 diabetes treatment, can be effectively degraded using proteolysis-targeting chimera (PROTAC). This approach offers potential for long-acting antidiabetic agents.
Yuqi Ying (14434974), Shaobing Cheng (10094194), Ziwei Zhang (2029975), Zhifang Cai (785093), Zunhua Yang (544464), Yulin Feng (117705), Pei Hu (1489597), Jian Xiong (531582), Jiamin Wu (1987333), Yuanying Fang (544463), Qing Zeng (494174), Huilan Li (7489379)   +11 more
core   +4 more sources

BRAFV600E‐PROTAC versus inhibitors in melanoma cells: Deep transcriptomic characterization

Clinical and Translational Medicine
Aims This study compares the suppression of Mitogen‐activated protein kinase (MAPK) signalling and early resistance potential between a proteolysis‐targeting chimera (PROTAC) and inhibitors targeting BRAFV600E.
Solomon O. Alhassan, Zakaria Y. Abd Elmageed, Youssef Errami, Guangdi Wang, Joe A. Abi‐Rached, Emad Kandil, Mourad Zerfaoui   +6 more
doaj   +1 more source