Results 41 to 50 of about 5,184,182 (156)

Site‐Specific Protein Bioconjugation Through Cellular Incorporation of Noncanonical Amino Acids

Angewandte Chemie, EarlyView.
Genetic code expansion (GCE) enables site‐specific installation of noncanonical amino acids containing bioorthogonal conjugation handles, allowing precise, homogeneous protein modification. This review examines the principles of orthogonal translation, surveys the chemistries available for chemoselective labeling, and highlights emerging multi‐site ...
Rahul Sarkar, Manas Joshi, Abhishek Chatterjee   +2 more
wiley   +2 more sources

Targeted Degradation of Picornaviral 3C Protease via PROTACs Confers High Barrier to Viral Resistance and Broad‐Spectrum Antiviral Activity

Advanced Science, EarlyView.
This study reports D34 as the first PROTAC degrader that targets the 3C protease of picornaviruses. D34 effectively degrades EV71 3C protease via the ubiquitin‐proteasome pathway. More importantly, D34 exhibits a high resistance barrier and shows broad‐spectrum antiviral activity against multiple picornaviruses, highlighting its potential as a novel ...
Weilong Deng, Junyu Chen, Yingyue Pang, Yuanyuan Zhang, Siqian Chen, Guoliang You, Xiaoman Tian, Zhongxin Xu, Jing Wang, Luqing Shang   +9 more
wiley   +1 more source

Targeted Protein Degradation in the Mitochondrial Matrix and Its Application to Chemical Control of Mitochondrial Morphology [PDF]

Dysfunction of mitochondria is implicated in various diseases, including cancer and neurodegenerative disorders, but drug discovery targeting mitochondria and mitochondrial proteins has so far made limited progress.
Shinichi, Sato, Minoru, Ishikawa, Shusuke, TOMOSHIGE, Sho, Nakamura, Wakana, Yamada   +4 more
core   +2 more sources

A Single‐Amino‐Acid Ligand for LAT1: A Minimalist and Modular Platform for Lysosome‐Targeted Degradation of Membrane Proteins

Advanced Science, EarlyView.
LA‐LYTAC repurposes the cancer‐enriched amino acid transporter LAT1 as a lysosomal trafficking receptor for targeted membrane‐protein degradation. A single phenylalanine‐derived ligand, modularly linked to antibodies or small‐molecule binders, recruits PD‐L1, EGFR, or integrins to LAT1, triggering transporter‐mediated internalization, lysosomal ...
Liquan Zhu, Ke Liu, Haotian Liu, Chaoqi He, Xiaozhen Liu, Xin Zeng, Misha Mao, Yuxiao Mu, Ying Li, Qinghui Zheng, Hongchao Tang, Da Qian, Xuli Meng   +12 more
wiley   +1 more source

Small molecule degraders of the hepatitis C virus protease reduce susceptibility to resistance mutations

Nature Communications, 2019
Targeted protein degradation (TPD) is a promising strategy for drug development. In this proof-of-concept study, the authors use telaprevir, which binds hepatitis C virus (HCV) NS3/4A protease, to target the protease for protein degradation, and show ...
Mélissanne de Wispelaere, Guangyan Du, Katherine A. Donovan, Tinghu Zhang, Nicholas A. Eleuteri, Jingting C. Yuan, Joann Kalabathula, Radosław P. Nowak, Eric S. Fischer, Nathanael S. Gray, Priscilla L. Yang   +10 more
doaj   +1 more source

Multimodal Bioinspired Self‐Healing Composites Enabling Durable and High‐Efficiency Wearable Perovskite Light‐Emitting Diodes

Advanced Science, EarlyView.
Butterfly wing–inspired intrinsically self‐healing polymer interlayers enable flexible perovskite optoelectronics with high luminance, strain‐insensitive stability, and environmental resilience. These hierarchically structured films redistribute mechanical stress, suppress defect formation, and maintain performance under repeated bending, paving the ...
Loganathan Veeramuthu, Yu‐Chen Wang, Chun‐Tse Tsai, Yen‐Lin Tseng, Xuan Ting King, Tzu‐Ming Hsu, Zhen‐Li Yan, Fang‐Cheng Liang, Pei‐Yin Chen, Georgy Dosovitskiy, Yehonadav Bekenstein, Hyunjin Lee, Tao Zhou, Chi‐Ching Kuo   +13 more
wiley   +1 more source

GPC3-mediated lysosome-targeting chimeras (GLTACs) for targeted degradation of membrane proteins

Acta Pharmaceutica Sinica B
Membrane protein degradation is a cutting-edge field in targeted protein degradation (TPD). Herein, we developed glypican-3 (GPC3)-mediated lysosome-targeting chimeras (GLTACs) as a novel strategy for the targeted degradation of tumor-specific membrane ...
Yuxin Fang, Yaojin Zhu, Wei Wang, Zhewei Xia, Shipeng He, Guoqiang Dong, Chunquan Sheng   +6 more
doaj   +1 more source

Synthetic protein degradation circuits using programmable cleavage and ligation by Sortase A

Nature Communications
BioPROTACs are heterobifunctional proteins designed for targeted protein degradation (TPD). They are useful not only for probing protein functions but also offer a therapeutic avenue for modulating disease-related proteins.
Hopen K. Yang, Pragati K. Muthukumar, Wilfred Chen   +2 more
doaj   +1 more source

Molecular Glue Degraders Enhance CAPRIN1‐Dependent Lysosomal Degradation of APP and Reduce Amyloid β in Alzheimer's Disease

Advanced Science, EarlyView.
A new class of lysosome‐directed molecular glue degraders selectively enhance CAPRIN1–APP interactions, driving APP degradation and reducing amyloid‐β production in human neurons and Alzheimer's disease mouse models. This CAPRIN1‐dependent targeted protein degradation strategy reveals a previously unrecognized therapeutic approach for disrupting the ...
Sunghan Jung, Xu Wang, Bin Liu, Raktim Roy, Nancy Jaiswal, Ratan K. Rai, Yuichiro Takagi, Cen Gao, Lifan Zeng, Ho‐Yin Lo, Reagan K. Wohlford, Ryan K. Higgins, Bruce T. Lamb, Anantha Shekhar, Anita C. Bellail, Chunhai Hao   +15 more
wiley   +1 more source

Inhibition of Mitogen-Activated Protein Kinase Erk1/2 Promotes Protein Degradation of ATP Binding Cassette Transporters A1 and G1 in CHO and in HuH7 cells. [PDF]

, 2013
Signal transduction modulates expression and activity of cholesterol transporters. We recently demonstrated that the Ras/mitogen-activated protein kinase (MAPK) signaling cascade regulates protein stability of Scavenger Receptor BI (SR-BI) through ...
Enrich Bastús, Carles, Enrich Carlos, Karen Cecilia Chan, Monira Hoque, Darabi, Masoud, Reverter Martín, Meritxell, Hoque, Monira, Rentero Alfonso, Carles, Meritxell Reverter, Rentero Carles, Melanie Manetsch, Masoud Darabi, Mulay, Vishwaroop, Peta Wood, Grewal Thomas, Álvarez-Guaita, Anna, Heeren, Joerg, Anna Alvarez-Guaita, Kerry-Anne Rye, Darabi Masoud, Rye Kerry-Anne, Chan, Karen Cecilia, Manetsch, Melanie, Mulay Vishwaroop, Manetsch Melanie, Heeren Joerg, Carlos Enrich, Cairns, Rose, Reverter Meritxell, Joerg Heeren, Carles Rentero, Vishwaroop Mulay, Rose Cairns, Wood Peta, Wood, Peta, Grewal, Thomas, Rye, Kerry-Anne, Chan Karen Cecilia, Álvarez-Guaita Anna, Thomas Grewal, Hoque Monira, Cairns Rose   +41 more
core   +2 more sources