Results 201 to 210 of about 11,335 (243)

PROTAC Technology as a New Tool for Modern Pharmacotherapy

Molecules
The publication focuses on the innovative applications of PROTAC (proteolysis-targeting chimera) technology in modern pharmacotherapy, with particular emphasis on cancer treatment. PROTACs represent an advanced therapeutic strategy that enables selective
Natalia Kubryń, Łukasz Fijałkowski, J. Nowaczyk, A. Jamil, A. Nowaczyk   +4 more
semanticscholar   +1 more source

Annual review of PROTAC degraders as anticancer agents in 2022.

European journal of medicinal chemistry
Following nearly two decades of development, significant advancements have been achieved in PROTAC technology. As of the end of 2022, more than 20 drugs have entered clinical trials, with ARV-471 targeting estrogen receptor (ER) showing remarkable ...
Xiao Wang, Zhao-Long Qin, Na Li, Meiqi Jia, Qiuge Liu, Yi-Ru Bai, Jian Song, Shuo Yuan, Sai-Yang Zhang   +8 more
semanticscholar   +1 more source

PROTAC Shrinks Mutated Prostate Tumors

Cancer Discovery, 2022
Abstract The most clinically advanced proteolysis-targeting chimera, bavdegalutamide, seems to work best against two molecularly defined subtypes of advanced prostate cancer. According to phase I/II trial data presented at the 2022 American Society of Clinical Oncology Genitourinary Cancers Symposium, the androgen receptor degrader most ...
openaire   +2 more sources

PROTAC Prodrug‐Integrated Nanosensitizer for Potentiating Radiation Therapy of Cancer

Advances in Materials
Radiation therapy (RT) is one of the primary options for clinical cancer therapy, in particular advanced head and neck squamous cell carcinoma (HNSCC).
Shunan Zhang, Yi Lai, Jiaxing Pan, Madiha Saeed, Shiqin Li, Huiling Zhou, Xingyu Jiang, Jing Gao, Yun Zhu, Haijun Yu, Wen Zhang, Zhiai Xu   +11 more
semanticscholar   +1 more source

PROTAC technology: From drug development to probe technology for target deconvolution.

European journal of medicinal chemistry
Drug development remains a critical focus within the global pharmaceutical industry. To date, more than 80 % of disease targets are considered difficult to target. The emergence of PROTAC technology has, to some extent, alleviated this challenge.
Si Yan, Guangshuai Zhang, Wei Luo, Mengwei Xu, Rui Peng, Ziwei Du, Yan Liu, Zhaofang Bai, Xiaohe Xiao, Shuanglin Qin   +9 more
semanticscholar   +1 more source

Selective degradation of multimeric proteins by TRIM21-based molecular glue and PROTAC degraders.

Cell
Targeted protein degradation (TPD) utilizes molecular glues or proteolysis-targeting chimeras (PROTACs) to eliminate disease-causing proteins by promoting their interaction with E3 ubiquitin ligases.
Panrui Lu, Yalong Cheng, Lei Xue, Xintong Ren, Xilong Xu, Chenglong Chen, Longzhi Cao, Jiao Li, Qingcui Wu, Shan Sun, Junjie Hou, Wei Jia, Wei Wang, Yan Ma, Zhaodi Jiang, Chao Li, Xiangbing Qi, Niu Huang, Ting Han   +18 more
semanticscholar   +1 more source

Light‐Triggered PROTAC Nanoassemblies for Photodynamic IDO Proteolysis in Cancer Immunotherapy

Advances in Materials
While proteolysis‐targeting chimeras (PROTACs) hold great potential for persistently reprogramming the immunosuppressive tumor microenvironment via targeted protein degradation, precisely activating them in tumor tissues and preventing uncontrolled ...
Jiwoong Choi, Byeongmin Park, Jung Yeon Park, Dongwon Shin, Sangmin Lee, H. Y. Yoon, Kwangmeyung Kim, Sun Hwa Kim, Yongju Kim, Yoosoo Yang, M. Shim   +10 more
semanticscholar   +1 more source

Dual-Action-Only PROTACs

Journal of the American Chemical Society
Proteolysis targeting chimera (PROTAC)-based degraders are highly potent pseudocatalytic drugs, but on-target off-site homing could yield undesirable consequences. We report here a generalizable AND-logic gated PROTAC, where the concurrent presence of two different disease-relevant endogenous stimuli liberates an active protein degrader. We design Dual-
Ranit Dutta, Anirudh Devarajan, Amelia Talluri, Ritam Das, S. Thayumanavan   +4 more
openaire   +2 more sources

Discovery of a PROTAC degrader for METTL3-METTL14 complex.

Cell Chemical Biology
N6-methyladenosine (m6A) methylation is the most abundant type of RNA modification that is mainly catalyzed by the METTL3-METTL14 methyltransferase complex. This complex has been linked to multiple cancers and is considered a promising therapeutic target
Wenhao Du, Yuting Huang, Xiaoai Chen, Yue Deng, Yaoliang Sun, Hong-Dou Yang, Qiongyu Shi, Feifei Wu, Guobin Liu, He Huang, Jian Ding, Xun Huang, Shilin Xu   +12 more
semanticscholar   +1 more source

Targeted protein degradation by PROTACs

Pharmacology & Therapeutics, 2017
Targeted protein degradation using the PROTAC technology is emerging as a novel therapeutic method to address diseases driven by the aberrant expression of a disease-causing protein. PROTAC molecules are bifunctional small molecules that simultaneously bind a target protein and an E3-ubiquitin ligase, thus causing ubiquitination and degradation of the ...
Taavi K, Neklesa, James D, Winkler, Craig M, Crews   +2 more
openaire   +2 more sources