Results 71 to 80 of about 11,335 (243)

BRAFV600E‐PROTAC versus inhibitors in melanoma cells: Deep transcriptomic characterization

Clinical and Translational Medicine
Aims This study compares the suppression of Mitogen‐activated protein kinase (MAPK) signalling and early resistance potential between a proteolysis‐targeting chimera (PROTAC) and inhibitors targeting BRAFV600E.
Solomon O. Alhassan, Zakaria Y. Abd Elmageed, Youssef Errami, Guangdi Wang, Joe A. Abi‐Rached, Emad Kandil, Mourad Zerfaoui   +6 more
doaj   +1 more source

Dual Aptamers‐Based SETDB1 PROTACs as Effective Anti‐Tumor Strategies for Breast Cancer

Advanced Science, EarlyView.
This study establishes dual‐aptamer PROTACs targeting SETDB1 using a SETDB1‐specific aptamer conjugated to AS1411. The designed PROTACs penetrate cells, recruit MDM2 to degrade SETDB1, and inhibit cancer cell proliferation and migration. Remarkably, they also overcome tamoxifen resistance and enhance CD8+ T cell cytotoxicity, suppressing tumor growth ...
Yanxuan Guo, Yingge Lv, Shuyu Huang, Chang Liu, Yan Ouyang, Bei Lan, Chenghao Xuan   +6 more
wiley   +1 more source

VERITAC-2: a Phase III study of vepdegestrant, a PROTAC ER degrader, versus fulvestrant in ER+/HER2- advanced breast cancer

Future Oncology
Vepdegestrant (ARV-471) is an oral PROTAC ER degrader that binds an E3 ubiquitin ligase and ER to directly trigger ubiquitination of ER and its subsequent proteasomal degradation.
E. Hamilton, Cynthia X. Ma, M. Laurentiis, H. Iwata, S. Hurvitz, Seth A. Wander, M. Danso, Dongrui R Lu, Julia Perkins Smith, Yuan Liu, L. Tran, Sibyl Anderson, M. Campone   +12 more
semanticscholar   +1 more source

G4‐Ligand‐Directed PROTACs Unveil DR1 as a Novel Ligand‐Co‐Binding G4‐Protein and Reshape G4‐Dependent Transcription

Advanced Science, EarlyView.
G4‐binding proteins (G4BPs) that specifically co‐bind G4s in the presence of small‐molecule ligands represent a critical but unexplored class of proteins. We introduce G4‐Ligand‐Directed PROTACs (G4L‐TACs), a chemical platform that couples G4 ligands (PDS) to E3 recruiters to selectively degrade these ligand‐co‐binding G4BPs.
Mao‐Lin Li, Shu‐Min Xu, Xin‐Chen Jiang, Le‐Tian Dai, Yu‐Tao Hu, Kai‐Bo Wang, Jia‐Heng Tan, Zhi‐Shu Huang, Shuo‐Bin Chen   +8 more
wiley   +1 more source

A Spatiotemporally Controlled Nanoplatform for Photothermal BRD4 Degradation Enables Synergistic Cancer Immunotherapy

Advanced Science, EarlyView.
A GSH‐responsive MOF nanoplatform acts as a Photothermolysis‐Targeting Conjugate (PTTAC). Through sophisticated step‐wise nuclear delivery, it enables NIR‐II light‐triggered photothermal degradation of BRD4. This precise strategy induces robust immunogenic cell death (ICD) and powerfully synergizes with anti‐PD‐L1 blockade to elicit a potent systemic ...
Luyi Wang, Jiasha Wu, Rui Ji, Sufeng Qiang, Yulin Shen, Yan Zuo, Shiqin Jian, Siyao Liu, Fusheng Xu, Honggang Hu, Xiaochun Hu   +10 more
wiley   +1 more source

Rational Design of PROTAC Linkers Featuring Ferrocene as a Molecular Hinge to Enable Dynamic Conformational Changes

Journal of the American Chemical Society
Proteolysis Targeting Chimeras (PROTACs) are bifunctional molecules that induce ubiquitination and degradation of a target protein via recruitment to an E3 ligase.
Alessandra Salerno, L. Wieske, Claudia J Diehl, A. Ciulli   +3 more
semanticscholar   +1 more source

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

Microtopography enhances intestinal drug absorption via Piezo1‐mediated tight junction modulation

BMEMat, EarlyView.
Microtopography‐driven enhancement of oral peptide drug delivery by activating Piezo1 channels significantly improves paracellular permeability and bioavailability, offering a novel approach for optimizing macromolecule absorption in pharmaceutical formulations.
Yu Hu, Nan Xu, Xin Li, Xiaowo Kang, Tieyuan Bian, Junsheng Lin, Hao Tang, Yinyin Bao, Lu Zhang, Hongyan Yuan, Mingxi Yao, Xingyu Jiang, Zhi Luo   +12 more
wiley   +1 more source

A RIPK1-specific PROTAC degrader achieves potent antitumor activity by enhancing immunogenic cell death.

Immunity
Receptor-interacting serine/threonine-protein kinase 1 (RIPK1) functions as a critical stress sentinel that coordinates cell survival, inflammation, and immunogenic cell death (ICD).
Jonathan Mannion, Valentina Gifford, Benjamin Bellenie, Winnie Fernando, Laura Ramos Garcia, R. Wilson, Sidonie Wicky John, Savita Udainiya, E. Patin, C. Tiu, Angèle Smith, Maria Goicoechea, A. Craxton, Nathalia Moraes de Vasconcelos, Naomi Guppy, Kwai-Ming J. Cheung, Nicholas J Cundy, Olivier A. Pierrat, Alfie Brennan, T. Roumeliotis, Graeme Benstead-Hume, J. Alexander, Gareth Muirhead, S. Layzell, Wenxin Lyu, V. Roulstone, Mark Allen, H. Baldock, Arnaud Legrand, Florian Gabel, Natalia Serrano-Aparicio, C. Starling, Hongyan Guo, Jason W. Upton, M. Gyrd-Hansen, Marion MacFarlane, Benedict Seddon, Florence I Raynaud, I. Roxanis, K. Harrington, Syed Haider, Jyoti S. Choudhary, S. Hoelder, T. Tenev, Pascal Meier   +44 more
semanticscholar   +1 more source

Shedding Light on Synthetic Autocatalysis: From Conventional Closed‐Shell Chemistries to Overlooked Open‐Shell Occurrences

Chemistry – A European Journal, EarlyView.
Why add another catalyst when the product itself holds the power to catalyze its own formation? Autocatalysis in synthetic chemistry enhances reaction efficiency and uncovers novel catalytic behavior across both closed‐shell and open‐shell systems, expanding reactivity and enabling innovative design strategies.
Jaspreet Kaur, Joshua P. Barham
wiley   +1 more source