Results 71 to 80 of about 64,058 (295)

Dual Covalent Targeting of STING Cysteines 292/309 Disrupts Functional Oligomerization and Enables Potent Antagonist Development

Advanced Science, EarlyView.
We report a rational design strategy for STING antagonists by dual covalent targeting of Cys292/309 in its C‐terminal domain, directly preventing functional oligomerization. Through covalent warhead repurposing, we identified P005091 and revealed its unique dual‐cysteine mechanism.
Yuxuan Zhao, Ling Huang, Wenjing Qin, Bin Zhang, Yang Yang, Xue Chen, Xiaoquan Wang, Weilin Zhou, Feiyang Chen, Zhenyu Li, Liyuan Le, Yiqiu Zhang, Zhen Xiang, Lu Zhang, Fei Wang, Dan Lei, Zi‐zhe Cai, Ying Gao, Yong Chen, Xuecen Wang, Junmin Quan, Shuixing Zhang, Xianzhang Bu, Xin Yue   +23 more
wiley   +1 more source

A systematic review of p53 regulation of oxidative stress in skeletal muscle

Redox Report, 2018
Background: p53 is a tumor suppressor protein involved in regulating a wide array of signaling pathways. The role of p53 in the cell is determined by the type of imposed oxidative stress, its intensity and duration.
Kaitlyn Beyfuss, David A. Hood
doaj   +1 more source

Nanomedicine Meets Immunotherapy: Advancing Adoptive Cell Therapy with Nanoparticles in the Treatment of Cancer with Sustainability Perspectives

Advanced Science, EarlyView.
This review surveys nanoparticle‐based strategies to enhance adoptive cell therapy, particularly CAR‐T cell approaches, in solid tumor treatment. It describes how nanoparticles can improve tumor immunogenicity and T‐cell infiltration while reducing toxicity, and how they enable in vivo CAR‐T cell generation.
Erica Frostegård, Tatiana Bobrova, Amalie Leinebø, Thibault Leray, Shayamita Ghosh, Lorena García‐Hevia, Chiara Puccinelli, Lorenzo Riccio, Jacopo Sorani, Davide Bonifazi, Julien Caumartin, Emmanuel Donnadieu, Florence Gazeau, Roland Hischier, Else Marit Inderberg, Mónica L. Fanarraga, Maria Loustau, Bernd Nowack, Sébastien Wälchli, Cécilia Ménard‐Moyon   +19 more
wiley   +1 more source

Activation of Ciona sperm motility: phosphorylation of dynein polypeptides and effects of a tyrosine kinase inhibitor [PDF]

, 1991
A high molecular mass dynein ATPase polypeptide and a 18–20 kDa dynein light chain of Ciona sperm flagella are phosphorylated during in vivo activation of motility or in vitro activation of motility by incubation with cyclic AMP.
Brokaw, Charles J., Dey, Chinmoy S.
core  

THE CONCISE GUIDE TO PHARMACOLOGY 2017/18:Enzymes [PDF]

, 2017
The Concise Guide to PHARMACOLOGY 2017/18 provides concise overviews of the key properties of nearly 1800 human drug targets with an emphasis on selective pharmacology (where available), plus links to an open access knowledgebase of drug targets and ...
,, Alexander, Stephen Ph, Davies, Jamie A, Fabbro, Doriano, Faccenda, Elena, Harding, Simon D, Kelly, Eamonn, Marrion, Neil V, Pawson, Adam J, Peters, John A, Sharman, Joanna L, Southan, Christopher   +11 more
core   +15 more sources

Regulation of transcription by cyclic AMP-dependent protein kinase. [PDF]

Proceedings of the National Academy of Sciences, 1989
cAMP-dependent protein kinase (PKA; ATP: protein phosphotransferase; EC 2.7.1.37) appears to be the major mediator of cAMP responses in mammalian cells. We have investigated the role of PKA subunits in the regulation of specific genes in response to cAMP by cotransfection of wild-type or mutant subunits of PKA together with cAMP-inducible reporter ...
P L, Mellon, C H, Clegg, L A, Correll, G S, McKnight   +3 more
openaire   +2 more sources

Nano‐Enabled Systemic Delivery of STING Agonist by Engineered Silicasome for Potent Antitumor Immunotherapy

Advanced Science, EarlyView.
Engineered mesoporous silica nanoparticles (Silicasomes) enable systemic delivery of the STING agonist ADU‐S100, overcoming the instability and toxicity that limit cyclic dinucleotides to local administration. By enhancing tumor accumulation, activating systemic antitumor immunity, and remodeling the tumor immune microenvironment, these nanoparticles ...
Wenjing Zhou, Yuting Li, Xudong Sun, Honghong Yang, Xiayu Shi, Lijia Yao, Jinhong Jiang, Erli Wang, Haoyang Wang, Yi Wei, Xiangsheng Liu   +10 more
wiley   +1 more source

Very large G protein-coupled receptor 1 regulates myelin-associated glycoprotein via Gαs/Gαq-mediated protein kinases A/C. [PDF]

, 2013
VLGR1 (very large G protein-coupled receptor 1), also known as MASS1 (monogenic audiogenic seizure susceptible 1), is an orphan G protein-coupled receptor that contains a large extracellular N terminus with 35 calcium-binding domains.
Fu, Ying-Hui, Lin, Shu-Ting, Ptácek, Louis J, Shin, Daesung   +3 more
core   +1 more source

T‐Cell Exhaustion in the Tumor Microenvironment: Subcellular Dysfunction, Pan‐Cancer Characteristics, and Therapeutic Interventions

Advanced Science, EarlyView.
This study elucidates the mechanisms of subcellular multidimensional collapse in exhausted T cells. By specifically targeting the nucleus, mitochondria, and endoplasmic reticulum, strategic interventions can effectively remodel the compromised organelle network. This integrated approach drives comprehensive T cell resuscitation, ultimately establishing
Mingxing Wang, Wanhui Dong, Jian Chen, Zhangjie Zhou, Shujuan Fu, Tingting Wu, Haiyan Jiang, Zhiying Wang, Zhixian Zhong, Yi Zhong   +9 more
wiley   +1 more source

Nucleic Acid Therapeutics for “Undruggable” Cancer Targets: Mechanisms, Challenges, and Prospects

Advanced Science, EarlyView.
Nucleic acid therapeutics bypass the structural limitations of conventional drugs by targeting mRNA rather than proteins. This review examines how antisense oligonucleotides, siRNAs, miRNAs, aptamers, and mRNA vaccines intervene against historically undruggable oncoproteins including Ras, MYC, and p53, highlighting mechanistic advances, delivery ...
Feng Xu, Ke Wang, Kaizhong Lu, Tianlun Hou, Yuan Chen, Xian Wang, Hongchuan Jin   +6 more
wiley   +1 more source