Results 111 to 120 of about 11,341 (256)

BRD4-BRD2 isoform switching coordinates pluripotent exit and Smad2-dependent lineage specification [PDF]

, 2017
Pluripotent Stem Cells (PSCs) hold great clinical potential, as they possess the capacity to differentiate into fully specialised tissues such as pancreas, liver, neurons and cardiac muscle.
Ciulli, Alessio, Davidson, Lindsay, Fernandez-Alonso, Rosalia, Findlay, Greg M., Hukelmann, Jens, Lamond, Angus, Prescott, Alan R., Sapkota, Gopal P., Zengerle, Michael   +8 more
core   +3 more sources

“Membrane‐Guided” Repair Strategy: Precision Delivery of GGT1 Degrader for Targeted Repair and Regeneration of Spinal Cord Neurons

Advanced Science, EarlyView.
This study confirms that GGT1 is a key driver of neuronal ferroptosis following spinal cord injury. We developed NSCm@EA, a biomimetic delivery system coated with neural stem cell membranes, for precise delivery of enocyanin to injured neurons. By combining targeted delivery with ubiquitination degradation mechanisms, this system promotes MGRN1 ...
Tao Yang, Lei Ye, Peigen Xie, Tao Song, Jian Chen, Heng Zhao, Zhengshan Liu, Xi Chen, Jianing Ding, Xintian Ding, Ao Shao, Miaomiao Wu, Fengdong Zhao, Siyue Tao, Tao You   +14 more
wiley   +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

PROTAC-DB 3.0: an updated database of PROTACs with extended pharmacokinetic parameters

Nucleic Acids Research
Abstract Proteolysis-targeting chimera (PROTAC) is an emerging therapeutic technology that leverages the ubiquitin-proteasome system to target protein degradation. Due to its event-driven mechanistic characteristics, PROTAC has the potential to regulate traditionally non-druggable targets.
Jingxuan Ge, Shimeng Li, Gaoqi Weng, Huating Wang, Meijing Fang, Huiyong Sun, Yafeng Deng, Chang- Yu Hsieh, Dan Li, Tingjun Hou   +9 more
openaire   +2 more sources

A Plug‐and‐Play Platform for Customizing Multivalent Degraders and Degrader‐Drug Conjugates

Advanced Science, EarlyView.
Membrane proteins remain challenging targets for conventional TPD approaches. Here, the authors develop UPTAB, a modular platform leveraging ultrahigh‐affinity orthogonal Im/CL protein pairs for lysosomal degradation of membrane proteins. Mono‐targeted (Type‐I), dual‐targeted (Type‐II), and tri‐targeted (Type‐III) UPTABs enable simultaneous degradation
Mengqing Zhao, Yan Deng, Jianjian Han, Yong Xie, Kai Bao, Lixin Ma, Lilong Liu, Wuxiang Mao   +7 more
wiley   +1 more source

Application of PROTACs in target identification and validation

Acta Materia Medica
Proteolysis targeting chimeras (PROTACs), as a novel therapeutic drug model, has received widespread attention from academia and the pharmaceutical industry.
Yang Liu, Jing Liang, Rui Zhu, Yueying Yang, Yali Wang, Wenyi Wei, Hua Li, Lixia Chen   +7 more
doaj   +1 more source

Selectivity on-target of bromodomain chemical probes by structure-guided medicinal chemistry and chemical biology [PDF]

, 2016
Targeting epigenetic proteins is a rapidly growing area for medicinal chemistry and drug discovery. Recent years have seen an explosion of interest in developing small molecules binding to bromodomains, the readers of acetyl-lysine modifications.
Alessio Ciulli, Carles Galdeano, Chiang C-M, Lejeune P   +3 more
core   +2 more sources

Effect of carbamazepine on the pharmacokinetics of vepdegestrant, a PROteolysis TArgeting Chimera estrogen receptor degrader, in healthy adults

British Journal of Clinical Pharmacology, EarlyView.
Aim To evaluate the effects of carbamazepine, a strong cytochrome P450 (CYP)3A4 inducer, on the pharmacokinetics and safety of vepdegestrant, a PROteolysis TArgeting Chimera estrogen receptor degrader. Methods This was a phase 1, open‐label, fixed‐sequence, two‐period study in healthy adult participants.
Hechuan Wang, Jennifer A. Winton, Kyle T. Matschke, Alexandre Stouffs, Kimberly C. Lee, Yuanyuan Zhang, Wenlian Qiao, Weiwei Tan   +7 more
wiley   +1 more source

Selective modulation of protein C affinity for EPCR and phospholipids by Gla domain mutation [PDF]

, 2005
Uniquely amongst vitamin K-dependent coagulation proteins, protein C interacts via its Gla domain both with a receptor, the endothelial cell protein C receptor (EPCR), and with phospholipids.
Bangalore, Cheng, Christiansen, Christiansen, Domotor, Edgell, Esmon, Esmon, Faioni, Falls, Fay, Freedman, Freedman, Fukudome, Fukudome, Fukudome, Fukudome, Hermida, Huang, Ido, Jalbert, Kalafatis, Kalafatis, Kalafatis, Kisiel, Liaw, Marshall, McDonald, Nelsestuen, Nicolaes, Nishioka, Norstrom, Norstrom, Oganesyan, Regan, Regan, Reitsma, Rezende, Riewald, Sala, Shen, Shen, Shen, Simioni, Simmonds, Simmonds, Soriano-Garcia, Soriano-Garcia, Stearns-Kurosawa, Stearns-Kurosawa, Sun, Suzuki, Villoutreix, Walker, Wojcik, Xu, Yang, Zhang, Zhang   +58 more
core   +1 more source

Engineering Murine Cross‐Reactivity Into an Affibody to Human Death Receptor 5

Biotechnology and Bioengineering, EarlyView.
ABSTRACT Interspecies cross‐reactive protein therapeutics that target conserved epitopes across species are critical for translational research. The present study showcases the engineering of an affibody molecule, originally discovered for binding to human death receptor 5 (hDR5) with 94 nM affinity, to simultaneously acquire cross‐reactivity to murine
Tse‐Han Kuo, Nagamani Vunnam, Jonathan N. Sachs, Benjamin J. Hackel   +3 more
wiley   +1 more source