Results 91 to 100 of about 135,650 (305)

Multifunctional Gold Nanocluster‐Based PROTAC System for Targeted Degradation of Phosphorylated Tau and Modulation of Neuroinflammation in Alzheimer's Disease

Advanced Functional Materials, EarlyView.
We present a novel proteolysis‐targeting chimera (PROTAC) system conjugated to lipoic acid gold nanoclusters (PLANC), designed to degrade pTau, regulate inflammatory signaling, and effectively traverse the blood‐brain barrier (BBB). PLANC degraded pTau at various phosphorylation sites, with mechanistic studies confirming proteasome‐mediated degradation
Sarah Nevins, Callan D. McLoughlin, Wan‐Kyu Ko, Hye Kyu Choi, Brandon Conklin, Joshua B. Stein, Yannan Hou, Hongwon Kim, Rohan Khulbe, Ki‐Bum Lee   +9 more
wiley   +1 more source

E3 ligase activity of XIAP RING domain is required for XIAP-mediated cancer cell migration, but not for its RhoGDI binding activity. [PDF]

PLoS ONE, 2012
Although an increased expression level of XIAP is associated with cancer cell metastasis, the underlying molecular mechanisms remain largely unexplored.
Jinyi Liu, Dongyun Zhang, Wenjing Luo, Jianxiu Yu, Jingxia Li, Yonghui Yu, Xinhai Zhang, Jingyuan Chen, Xue-Ru Wu, Chuanshu Huang   +9 more
doaj   +1 more source

LMO7 Suppresses Tumor‐Associated Macrophage Phagocytosis of Tumor Cells Through Degradation of LRP1

Advanced Science, EarlyView.
LMO7 in tumor‐associated macrophages suppresses phagocytosis of tumor cells and limits cytotoxic T lymphocytes infiltration, fostering tumor progression. Mechanistically, LMO7 mediates the ubiquitination and degradation of the phagocytic receptor LRP1, impairing its ability to engulf tumor cells and driving macrophages toward an antitumor phenotype ...
Mengkai Li, Tao Wang, Yuwen Zhong, Zhiming Wang, Wei Li, Zejian Wang, Xinyi Yang, Yu Qiao, Jianfeng Xiang, Wei Gu, Zishu Wang, Lei Sun, Feng Qian   +12 more
wiley   +1 more source

Dynamic control of selectivity in the ubiquitination pathway revealed by an ASP to GLU substitution in an intra-molecular salt-bridge network

, 2012
Ubiquitination relies on a subtle balance between selectivity and promiscuity achieved through specific interactions between ubiquitin-conjugating enzymes (E2s) and ubiquitin ligases (E3s).
Bonvin, Alexandre M. J. J., Sjoerd J de Vries, Adrien S. J. Melquiond (122976), H Th Marc Timmers, Alexandre M. J. J. Bonvin (18079), Adrien S J Melquiond, Wijk, Sjoerd van, Alexandre M J J Bonvin, Melquiond, Adrien S. J., Timmers, H. Th. Marc, Sjoerd J. de Vries (110976), H. Th. Marc Timmers (10936), Sjoerd J. L. van Wijk (122975), Vries, Sjoerd J. de, Sjoerd J L van Wijk   +14 more
core   +1 more source

Natural Products Inspired Scaffold Diversification Leads to Unnatural Molecular Warhead and Covalent Strategy to Modulating Protein Function through Electrophilic Bromine Transfer

Advanced Science, EarlyView.
We report a new thiolate‐reactive α,α‐gem‐dibromo lactam warhead that activates transcription factor Nrf2 and demonstrates anti‐inflammatory activities, which have implications in cancer, neurodegeneration, and cardiovascular diseases. RNA‐seq illuminated detailed transcriptional profiles, and chemical reactions with cysteine‐containing compounds ...
Beau R. Brummel, Sofia Kokkaliari, Qiwen Gao, Jinjing Chen, Larissa Costa de Almeida, Srinivasarao Tenneti, Derek A. Leas, Eli Levit, Lewis S. Alexander, Khalil A. Abboud, Pingrong Wei, Michael D. Cameron, James R. Rocca, Ranjala Ratnayake, Donna D. Zhang, Hendrik Luesch, Robert W. Huigens III   +16 more
wiley   +1 more source

Characterisation of the ubiquitin E3 ligase COP1 [PDF]

, 2018
Constitutive photomorphogenic 1 (COP1) is a ubiquitin E3 ligase that has been implicated in development of a variety cancers. The goal was to characterise the ubiquitin E3 ligase activity of COP1 and the relationship between COP1 and its interaction ...
Curry, Jack Richard
core   +1 more source

A Caged E3 Ligase Ligand for PROTAC-Mediated Protein Degradation with Light

, 2019
A caging group has been appended to a widely used Von Hippel Lindau (VHL) E3 ligase ligand for targeted protein degradation with PROTACs. Proteolysis is triggered only after a short irradiation time allowing spatiotemporal control of the protein’s ...
Maria M., Shchepinova, Edward, Tate, Cyrille, Kounde   +2 more
core   +1 more source

SIAH1 (siah E3 ubiquitin protein ligase 1) [PDF]

, 2013
Review on SIAH1 (siah E3 ubiquitin protein ligase 1), with data on DNA, on the protein encoded, and where the gene is ...
Nagano, Y, Matsuzawa, SI
core   +1 more source

Targeting Lactate and Lactylation in Cancer Metabolism and Immunotherapy

Advanced Science, EarlyView.
Lactate, once deemed a metabolic waste, emerges as a central regulator of cancer progression. This review elucidates how lactate and its epigenetic derivative, protein lactylation, orchestrate tumor metabolism, immune suppression, and therapeutic resistance.
Jiajing Gong, Yuhang Xie, Zhijie Weng, Yongzhi Wu, Longjiang Li, Bo Li   +5 more
wiley   +1 more source

DOT1L Drives Endothelial‐to‐Mesenchymal Transition and Fibrotic Vascular Remodeling via H3K79 Methylation

Advanced Science, EarlyView.
DOT1L as a central epigenetic regulator of EndoMT and pulmonary fibrosis. Acting as an early epigenetic switch, it translates TGFβ–SMAD signaling into H3K79me2‐mediated chromatin remodeling, selectively activates fibrosis‐related genes, and primes ECs for rapid mesenchymal transition.
Yaofeng Wang, Xing Peng, Jingjing Chen, Yun Zhang, Tinghong Zhang, Jingyuan Zhang, Jiaying Fan, Hui Zheng, Qiaoyuan Liu, Zhimin Song, Zhan‐Peng Huang, Shu Meng   +11 more
wiley   +1 more source