Results 91 to 100 of about 13,155 (273)

Potent and Selective IGF‐IIR‐Recruiting Bifunctional Molecules for Targeted Lysosomal Degradation of Extracellular and Membrane Proteins

Advanced Science, EarlyView.
Lysosome‐targeting chimeras (LYTACs) enable degradation of extracellular and membrane proteins via lysosomal trafficking. We report a novel IGF‐II mutant (Del1–7, Y27L) that selectively engages IGF‐IIR while avoiding IGF‐IR and IR‐A. mutIGF‐II–based LYTACs enhance target internalization and degradation and support a genetically encodable, all‐protein ...
Yuan Zhao, Yaxian Liao, Pengyun Li, Regina Stasser de Gonzalez, Xuankun Chen, Nicholas S. Nieto, Florence M. Brunel, Nick Cox, Joseph Stock, Matthew McHenry, Guangsen Fu, Penghsuan Huang, Wenxin Wu, Deqin Cai, Lingjun Li, Alexander N. Zaykov, Weiping Tang   +16 more
wiley   +1 more source

Specificity for deubiquitination of monoubiquitinated FANCD2 is driven by the N-terminus of USP1 [PDF]

, 2018
The Fanconi anemia pathway for DNA interstrand crosslink repair and the translesion synthesis pathway for DNA damage tolerance both require cycles of monoubiquitination and deubiquitination.
Arkinson, Connor, Chaugule, Viduth K, Toth, Rachel, Walden, Helen   +3 more
core   +3 more sources

PSMA8‐Containing 20S Proteasome Regulates Spermiogenesis and Male Fertility

Advanced Science, EarlyView.
PSMA8 assembles s20S proteasome that degrades specific substrates in elongating spermatids. Degradation of s20S‐substrates activates translation of FXR1‐target mRNAs, which are essential for mitochondrial sheath formation and sperm morphogenesis.
Huiwen Cao, Qianting Zhang, Wei Xu, Anxuan Fang, Haomang Xu, Cheng Qiu, Lugeng He, Chao Yu   +7 more
wiley   +1 more source

PTGES3 proteolysis using the liposomal peptide-PROTAC approach

Biology Direct
Background Hepatocellular carcinoma (HCC) is the leading cause of cancer-related deaths worldwide, and the lack of effective biomarkers for early detection leads to poor therapeutic outcomes.
Shiwei Liu, Fukang Yuan, Hui Dong, Jiaqi Zhang, Xinyu Mao, Yangsui Liu, Huansong Li   +6 more
doaj   +1 more source

Leveraging Macrophage Metabolic Reprogramming for Enhanced Anti‐Tumor Immunity

Advanced Science, EarlyView.
Tumor‐associated macrophages (TAMs) are key regulators of the tumor microenvironment (TME), with their metabolic states playing a critical role in tumor progression or regression. This review summarizes current understanding of TAM metabolic plasticity alongside cutting‐edge bioengineering innovations, outlining a roadmap for transforming the ...
Zhiyun Liu, Lingyao Zeng, Xulin Gan, Yilin Zhou, Han Shen, Dan Wu, Xin Shou, Minmin Jiang, Liyun Shi   +8 more
wiley   +1 more source

Design and applications of bifunctional small molecules: Why two heads are better than one [PDF]

, 2008
Induction of protein−protein interactions is a daunting challenge, but recent studies show promise for small molecules that specifically bring two or more protein molecules together for enhanced or novel biological effect.
Aberle, Nicholas, Corson, Timothy W., Crews, Craig M   +2 more
core   +1 more source

First Generation Proteolysis Targeting Chimeras (PROTACs) for the Treatment of Progeria

Advanced Science, EarlyView.
We report the first PROTACs designed to degrade progerin, introducing a novel therapeutic approach for progeria. The best compound, UCM‐18142, significantly reduces progerin levels and improves key disease phenotypes in patient‐derived cells and in the LmnaG609G/G609G mouse model, paving the way for new treatment strategies targeting the root cause of ...
Jon Macicior‐Michelena, Marcelino Telechea, Daniel Fernández, Alba García‐Martín, Ángeles Canales, Silvia Ortega‐Gutiérrez   +5 more
wiley   +1 more source

Galectins as New Prognostic Markers and Potential Therapeutic Targets for Advanced Prostate Cancers [PDF]

, 2013
A better understanding of multimolecular interactions involved in tumor dissemination is required to identify new effective therapies for advanced prostate cancer (PCa).
Compagno, Daniel Georges, Gentilini, Lucas Daniel, Jaworski, Felipe Martín, Laderach, Diego Jose   +3 more
core   +3 more sources

ESCRT‐Mimetic Nanodegrader Targets STING for Anti‐Inflammatory Therapy

Advanced Science, EarlyView.
A nanoplatform‐enabled targeted protein degradation strategy is presented to regulate aberrant STING signaling. STING‐ATTEC induces selective autophagic degradation of STING via formation of a STING–ATTEC–LC3 ternary complex, while the cationic FA‐LNP+ system enhances LC3 generation and targeted delivery. Together, this synergistic approach efficiently
Fuyuan Zhou, Qiming Zhai, Zhihao Yao, Qing Li, Yan Yang, Si Wang, Chao Huang, Liangjing Xin, Tao Chen, Jinlin Song   +9 more
wiley   +1 more source

Crystal Structure of the Cul2-Rbx1-EloBC-VHL Ubiquitin Ligase Complex [PDF]

, 2017
Cullin RING E3 ubiquitin ligases (CRLs) function in the ubiquitin proteasome system to catalyze the transfer of ubiquitin from E2 conjugating enzymes to specific substrate proteins.
Adams, Alessio Ciulli, Angers, Babon, Buckley, Buetow, Bulatov, Bulatov, Bullock, Cai, Calabrese, Canning, Cavadini, Chen, Deshaies, Duda, Duda, Duda, Emsley, Evans, Fischer, Fraczkiewicz, Frost, Fulcher, Galdeano, Goldenberg, Hershko, Hon, Jia, Kamura, Kamura, Keegan, Kelsall, Kim, Lai, Lamsoul, Lee, Liu, Liu, Liu, Lu, Lucas, Lydeard, Mahrour, Matthews, Maxwell, McCoy, Min, Morgan S. Gadd, Mosadeghi, Muchnik, Muniz, Nguyen, Nicholls, Onel, Pause, Petroski, Pettersen, Petzold, Prabhu, Salter, Scott, Semenza, Spratt, Stebbins, Teresa A.F. Cardote, Thomas, Vagin, Van Molle, Winn, Winter, Yasgar, Zengerle, Zhao, Zheng   +74 more
core   +2 more sources