Results 111 to 120 of about 823,777 (226)

Hsp90 Inhibition on the Western Blot: N‐Terminal Versus C‐Terminal Inhibitors in Breast Cancer

Medicinal Research Reviews, EarlyView.
ABSTRACT Heat shock protein 90 (Hsp90) is an established and clinically validated anticancer target. By regulating the folding and maturation of diverse client proteins, it is indirectly involved in carcinogenesis. Key breast cancer oncogenic drivers, including estrogen receptor, progesterone receptor, and human epidermal growth factor receptor 2, are ...
Jaka Dernovšek, Jernej Cingl, Urša Pečar Fonović, Tihomir Tomašič   +3 more
wiley   +1 more source

PROTAC-Induced Glycogen Synthase Kinase 3β Degradation as a Potential Therapeutic Strategy for Alzheimer’s Disease

Glycogen synthase kinase 3β (GSK-3β) is a serine/threonine kinase and an attractive therapeutic target for Alzheimer’s disease. Based on proteolysis-targeting chimera (PROTAC) technology, a small set of novel GSK-3β degraders was designed and ...
Valle Palomo (356637), Vincenza Andrisano (1417069), Melissa Guardigni (15844121), Matteo Bersani (15844127), Paula Fernández-Gómez (15844133), Andrea Tarozzi (2259433), Angela De Simone (1417054), Barbara Pagliarani (15844130), Elisa Uliassi (1730821), Andrea Milelli (2332678), Letizia Pruccoli (6828539), Francesca Spyrakis (68226), Alan Santini (15844124), Maria Laura Bolognesi (102185), Flavia Frabetti (73321)   +14 more
core   +1 more source

Molecular Glue Degraders in Early Development for Cancer Therapy

Medicinal Research Reviews, EarlyView.
ABSTRACT Molecular glue degraders are an emerging class of small molecule allosteric modulators that induce or stabilize protein‐protein interactions, enabling targeted degradation of previously intractable proteins. By redirecting E3 ligases to recognize neosubstrates, proteins that are not typically recognized by a specific E3 ubiquitin ligase, they ...
E. Sila Ozdemir, Hyunbum Jang, Ozlem Keskin, Attila Gursoy, Ruth Nussinov   +4 more
wiley   +1 more source

Perspectives of autophagy-tethering compounds (ATTECs) in drug discovery

Medicine Plus
Degrader technologies provide unprecedented strategies to tackle diseases caused by pathogenic proteins that are difficult to target by the traditional inhibitor approach.
Yu Ding, Dong Xing, Yiyan Fei, Shouqing Luo, Boxun Lu   +4 more
doaj   +1 more source

Innovation in pest management: can the past inform the future?

Pest Management Science, EarlyView.
Progress in pest management occurred incrementally, but occasionally, transformative discoveries introduced disruptive technologies. Looking ahead, generative artificial intelligence is expected to accelerate agricultural discovery by integrating vast datasets from mechanization, genetics, and chemistry.
Eric Moog, Franck E. Dayan
wiley   +1 more source

Proteolysis targeting chimeras (PROTACs) in oncology: a review of patents and regulatory considerations

Pharmaceutical Patent Analyst
Proteolysis Targeting Chimeras (PROTACs) represents a groundbreaking advancement in drug discovery and targeted protein degradation. Unlike traditional small-molecule inhibitors, PROTACs leverage the cell’s natural protein degradation machinery to selectively degrade pathogenic proteins, offering significant therapeutic potential for previously ...
M, Sowndharya, Joga, Ramesh, Gandhi, Kajal, Yerram, Sravani, Raghuvanshi, Rajeev Singh, Srivastava, Saurabh   +5 more
openaire   +2 more sources

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, Jacek Nowaczyk, Amer Jamil, Alicja Nowaczyk   +4 more
doaj   +1 more source

Artificial intelligence empowers targeted protein degradation: Core technological innovations, multi‐scenario applications, and translational prospects

Smart Molecules, EarlyView.
AI is transforming TPD by improving the design, prediction, and optimization of degraders such as PROTACs, molecular glues, and LYTACs. This review summarizes key AI‐driven advances, highlights applications across drug discovery stages, and discusses remaining challenges and future directions for accelerating the development of therapies against ...
Shuanglin Qin, Rui Peng, Guangshuai Zhang, Si Yan, Jin Xiao, Zishu Liu, Ziyu Tan, Qingqing Xie, Shangjie Li, Wei Luo, Xiaohe Xiao   +10 more
wiley   +1 more source

Molecular glues: Recent advances in cereblon substrate identification and mechanistic insights

Smart Molecules, EarlyView.
Molecular glues exert diverse core biological functions by inducing or stabilizing protein–protein interactions, extending far beyond the traditional scope of targeted protein degradation. Key breakthroughs include expanded cereblon substrate recognition, sustained G protein‐coupled receptor megacomplex signaling, and the first orthosteric molecular ...
Qingyun Guan, Xiaoyu Shi, Qian Yang, Xiangyi Jiang, Xinyong Liu, Peng Zhan   +5 more
wiley   +1 more source

Methylated Nucleotide-Based Proteolysis-Targeting Chimera Enables Targeted Degradation of Methyl-CpG-Binding Protein 2

Methyl-CpG-binding protein 2 (MeCP2), a reader of DNA methylation, has been extensively investigated for its function in neurological and neurodevelopmental disorders. Emerging evidence indicates that MeCP2 exerts an oncogenic function in cancer; however,
Li Chen (5749), Wenyi Wei (6911471), Zhen Wang (72451), Xing Qiu (560143), Hiroyuki Inuzuka (12378227), He Chen (104732), Xian Chen (107385), Dingpeng Zhang (6052529), Jing Liu (38537), Ling Xie (2026981), H. Ümit Kaniskan (1476325), Jian Jin (351142)   +11 more
core   +1 more source