Results 71 to 80 of about 8,212 (230)

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

Selective Modulation of OTUB1 Noncanonical Function via a bioPhosTAC Strategy

Advanced Science, EarlyView.
This work positions the versatile performance of the peptide‐based bioPhosTAC platform for dissecting phosphorylation‐dependent biology and expanding the scope of induced‐proximity technologies. We demonstrated that selective manipulation of a tyrosine phosphorylation site is sufficient to propagate coordinated cellular consequences.
Seung Un Seo, Seon Min Woo, Minhyeong Choi, Soeun Rhee, Simmyung Yook, Donghyuk Shin, Kwang‐Su Park, Taeg Kyu Kwon   +7 more
wiley   +1 more source

Multi‐Technique Integration Identifies O‐GlcNAc Transferase in Fibroblast‐Like Synoviocytes as a Therapeutic Target for Rheumatoid Arthritis

Advanced Science, EarlyView.
AI‑guided single‑cell transcriptomics identifies OGT as a key regulator enriched in rheumatoid arthritis fibroblast‑like synoviocytes (RA‐FLSs). Inflammatory stimuli activate the OGT–SAP130 axis, which modulates the H3K27ac/H3K27me3 balance and epigenetically silences BTG2, promoting aggressive transformation of RA‑FLSs.
Duoli Xie, Jie Huang, Chunhao Cao, Zhenchao Tang, Xingchen Li, Jianmin Guo, Xinxin Chen, Fang Wang, Dongyi He, Jie Li, Yu Du, Bing He, Jianhua Yao, Aiping Lu, Chao Liang   +14 more
wiley   +1 more source

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

Glucose and Glutamine Deprivation Promotes Breast Cancer Lung Metastasis via BRD4‐Dependent Enhancer Activation

Advanced Science, EarlyView.
To model a nutrient‐restricted tumor microenvironment, breast cancer cells were adapted to low glucose and glutamine levels. In the adapted cells, BRD4‐driven enhancer activation increases pro‐invasive EDN1 expression, facilitated by ATF3/c‐JUN and reinforced by enhancer RNA.
Poshan Yugal Bhattarai, Arathy Vasukutty, Yujin Na, Sung‐Chul Lim, Hong Seok Choi   +4 more
wiley   +1 more source

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

YX-112, a novel celastrol-derived PROTAC, inhibits the development of triple-negative breast cancer by targeting the degradation of multiple proteins

Frontiers in Pharmacology
BackgroundCelastrol is an effective component of the plant Tripterygium wilfordii Hook. f., which has a high inhibitory effect on triple-negative breast cancer.
Yongxue Gu, Mengmeng Yang, Wenbin Wang, Lihua Li, Ying Ma, Wenshan Liu, Wenshan Liu, Qiang Zhao   +7 more
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

Site‐Specific Protein Bioconjugation Through Cellular Incorporation of Noncanonical Amino Acids

Angewandte Chemie, EarlyView.
Genetic code expansion (GCE) enables site‐specific installation of noncanonical amino acids containing bioorthogonal conjugation handles, allowing precise, homogeneous protein modification. This review examines the principles of orthogonal translation, surveys the chemistries available for chemoselective labeling, and highlights emerging multi‐site ...
Rahul Sarkar, Manas Joshi, Abhishek Chatterjee   +2 more
wiley   +2 more sources

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