Results 131 to 140 of about 14,786 (290)

SUMOylation regulates tumorigenesis and progression: Molecular mechanisms and therapeutic applications

Interdisciplinary Medicine, EarlyView.
SUMOylation, a dynamic post‐translational modification, acts as a master regulator at the heart of tumor malignancy. Our work delineates how the SUMOylation cycle—mediated by E1/E2/E3 enzymes and reversed by SENPs—orchestrates multiple hallmarks of cancer. The central pathway converges on three critical pathological axes: 1.
Yimao Wu, Zichang Chen, Yinting Hu, Gokhan Zengin, Qian Zhang, Meng‐Yao Li, Wenlong Sun   +6 more
wiley   +1 more source

Degraders in epigenetic therapy: PROTACs and beyond

Theranostics
Epigenetics refers to the reversible process through which changes in gene expression occur without changing the nucleotide sequence of DNA. The process is currently gaining prominence as a pivotal objective in the treatment of cancers and other ailments.
Xing-Jie Dai, Shi-Kun Ji, Meng-Jie Fu, Gao Liu, Hui-Min Liu, Shao-Peng Wang, Liang Shen, Ning Wang, Piet Herdewijn, Yichao Zheng, Sai-Qi Wang, Xiao-Bing Chen   +11 more
semanticscholar   +1 more source

Optimization of a “Bump-and-Hole” Approach to Allele-Selective BET Bromodomain Inhibition [PDF]

, 2018
Allele-specific chemical genetics enables selective inhibition within families of highly-conserved proteins. The four BET (bromodomain & extra-terminal domain) proteins – BRD2, BRD3, BRD4 and BRDT bind acetylated chromatin via their bromodomains and ...
Albrecht, Amorim, Anders, Andrieu, Arrowsmith, Bamborough, Bamborough, Baud, Baud, Bishop, Bolden, Bunnage, Cheung, Clackson, Conery, Dawson, Deeney, Delmore, Dubocovich, Filippakopoulos, Filippakopoulos, Gacias, Gadd, Galdeano, Gamsjaeger, Huang, Islam, Lamonica, Li, Lin, Lu, Miller, Mirguet, Muller, Nassar, Nguyen, Nicholls, Nicodeme, Philpott, Picaud, Raina, Raux, Runcie, Sander, Schroder, Shi, Shi, Smith, Stathis, Stonestrom, Tanaka, Theodoulou, Theodoulou, Wang, Winter, Yang, Zengerle, Zhou, Zou, Zuber   +59 more
core   +2 more sources

PROTACs in cancer immunotherapy: a minireview

Biochemical Society Transactions
The discovery of immune checkpoint blockade as a therapeutic strategy to induce immunogenic cancer cell elimination has shown great success in the treatment of various cancers. However, limited response rates highlight the need for further development in this field. Promising new preclinical developments include the discoveries of proteolysis-targeting
Köckenberger J. E., Cardenas Alcoser E. S., Chang E. T., Gutkind J. S., Ferguson F. M.   +4 more
openaire   +2 more sources

Advantages of PROTACs in achieving selective degradation of homologous protein families

Beilstein Journal of Organic Chemistry
Proteolysis-targeting chimeras (PROTACs) have emerged as a promising therapeutic modality and now represent an important addition to the toolkit of medicinal chemists.
Luxi Yang, Xinfei Mao, Jingyi Zhang, Jing Shu, Wenhai Huang, Xiaowu Dong, Yinqiao Chen, Mingfei Wu   +7 more
doaj   +1 more source

The ubiquitin-proteasome system in neurodegeneration [PDF]

, 2014
SIGNIFICANCE: Impairment of the ubiquitin-proteasome system (UPS) has been implicated in the pathogenesis of a wide variety of neurodegenerative disorders, including Alzheimer's, Parkinson's, and Huntington's diseases.
McKinnon, C, Tabrizi, SJ
core   +1 more source

Development of miRNA-based PROTACs targeting Lin28 for breast cancer therapy

Science Advances
Lin28, a highly conserved carcinogenic protein, plays an important role in the generation of cancer stem cells, contributing to the unfavorable prognosis of cancer patients. This RNA binding protein specifically binds to pri/pre-microRNA (miRNA) lethal-7
Jianfei Xu, Xiaoran Zhao, Xingxing Liang, Dongyang Guo, Jing Wang, Qian Wang, Xinjing Tang   +6 more
semanticscholar   +1 more source

Smart Integration of Structural Biology and Medicinal Chemistry to Unlock Target‐Driven Drug Discovery

Medicinal Research Reviews, EarlyView.
ABSTRACT To enhance drug discovery efforts, medicinal chemists should evaluate, filter, and utilize relevant structural information about target proteins. Acquiring and interpreting protein structures is crucial for elucidating ligand‐receptor interactions and addressing ADME‐related considerations, making it an essential aspect of medicinal chemistry.
Matteo Rossi Sebastiano, Giulia Apprato, Serena Francisco, Giuseppe Ermondi, Giulia Caron   +4 more
wiley   +1 more source

G protein-coupled receptor kinase 2 (GRK2) as a potential therapeutic target in cardiovascular and metabolic diseases [PDF]

, 2019
G protein-coupled receptor kinase 2 (GRK2) is a central signaling node involved in the modulation of many G protein-coupled receptors (GPCRs) and also displaying regulatory functions in other cell signaling routes.
Arcones, Alba C., Briones, Ana M., Cruces-Sande, Marta, Mayor, Federico, Murga, Cristina, Salaices, Mercedes   +5 more
core   +3 more sources

Deciphering the mechanism of E3 ubiquitin ligases in plant responses to abiotic and biotic stresses and perspectives on PROTACs for crop resistance

Plant Biotechnology Journal
Summary With global climate change, it is essential to find strategies to make crops more resistant to different stresses and guarantee food security worldwide.
Yingying Su, Guillaume Legrand Ngolong Ngea, Kaili Wang, Yuchun Lu, Esa Abiso Godana, Michael Ackah, Qiya Yang, Hongyin Zhang   +7 more
semanticscholar   +1 more source