Results 81 to 90 of about 11,341 (256)

Fibrates Inhibit PLTP‐induced M2 Macrophage Infiltration and Increase the Sensitivity of Hepatocellular Carcinoma to ICIs

Advanced Science, EarlyView.
Phospholipid transfer protein(PLTP) plays a critical role in forming a complex with kinase A (AURKA) and P65. This interaction facilitates phosphorylation of P65 at Ser536, leading to the activation of the NF‐κB signaling pathway. Ultimately, this leads to the upregulation of downstream cytokines, including IL‐6, IL‐8, and CSF‐1, which promotes M2 ...
Xinyue Liang, Yaning Li, Jianxun Cai, Lisi Luo, Pengfei Yang, Yutong Chen, Jiancong Zhou, Yan Zeng, Jiaping Yu, Weiyu Zhang, Wenzheng Pang, Yufang Li, Chunhua Wen, Jian Li, Linjuan Zeng   +14 more
wiley   +1 more source

Interpretable PROTAC Degradation Prediction With Structure‐Informed Deep Ternary Attention Framework

Advanced Science
Proteolysis Targeting Chimeras (PROTACs) are heterobifunctional ligands bridging Proteins‐Of‐Interest (POIs) and E3 ligases for ubiquitin‐proteasome degradation, promising to target the ‘undruggable’.
Zhenglu Chen, Chunbin Gu, Shuoyan Tan, Xiaorui Wang, Yuquan Li, Mutian He, Ruiqiang Lu, Shijia Sun, Chang‐Yu Hsieh, Xiaojun Yao, Huanxiang Liu, Pheng‐Ann Heng   +11 more
doaj   +1 more source

Homo-PROTACs:bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation [PDF]

, 2017
E3 ubiquitin ligases are key enzymes within the ubiquitin proteasome system which catalyze the ubiquitination of proteins, targeting them for proteasomal degradation.
A Grosfeld, A Hergovich, A Rapisarda, A Schoenfeld, AC Lai, AC Lai, AR Schoenfeld, B Vu, C Galdeano, C Galdeano, C Loenarz, CE Stebbins, CH Arrowsmith, CM Pickart, CM Robinson, D Komander, DC Swinney, DE Feldman, DL Buckley, DL Buckley, DM Spencer, DP Bondeson, E Bulatov, EF Douglass, EK Schrader, ES Fischer, ET Mack, FE Morreale, G Chessari, G Lu, G Minervini, G Nalepa, G Petzold, GE Winter, H Lebraud, H Sun, I Molle Van, IJ Frew, J Frost, J Krönke, J Lu, JR Skaar, K Raina, L Gossage, LT Vassilev, M Li, M Tanaka, M Toure, M Zengerle, MD Petroski, ME Matyskiela, MR Arkin, MS Gadd, N Ohoka, N Zheng, PH Maxwell, RE Barry, T Han, T Ito, T Kamura, T Uehara, TA Soucy, TB Durham, TG Davies, TK Oost, TW Corson, V Bangiyeva, V Wittmann, WG Kaelin, X Huang, X Lucas, X Tan, Y Itoh, Z-Y Jiang   +73 more
core   +3 more sources

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

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

Understanding and Overcoming Antibody‐Drug Conjugate Resistance: Biological Mechanisms and Emerging Analytical Frameworks in Breast Cancer

Advanced Science, EarlyView.
Antibody–drug conjugates (ADCs) transform breast cancer therapy, yet resistance limits their durability. Emerging evidence reveals that ADC failure is not solely tumor‐intrinsic but shaped by dynamic tumor–microenvironment interactions that alter drug delivery, processing, and response.
Minji Seo, Jangsoon Lee, Naoto T. Ueno
wiley   +1 more source

Design and development of PROTACs: A new paradigm in anticancer drug discovery

Medicine in Drug Discovery
PROTAC (Proteolysis targeting chimera) is a potential revolutionary strategy in cancer drug development focusing on their ability to target specific receptors like androgen and BRD4, which are vital for the progression and development of several cancers.
Vishal Mathur, Mukund Jha, Iqra Zai, Moksh Mahajan, Shagufi Nazar, Shaheen Ali, Anam Ilyas, Sana Tanweer, Javed Ali, Ozair Alam   +9 more
doaj   +1 more source

Proteasomal and lysosomal degradation for specific and durable suppression of immunotherapeutic targets

Cancer Biology & Medicine, 2020
Cancer immunotherapy harness the body’s immune system to eliminate cancer, by using a broad panel of soluble and membrane proteins as therapeutic targets.
Yungang Wang, Shouyan Deng, Jie Xu
doaj   +1 more source

VHL-recruiting PROTAC attenuates renal fibrosis and preserves renal function via simultaneous degradation of Smad3 and stabilization of HIF-2α

Cell & Bioscience, 2022
Background Renal fibrosis is the pathological foundation of various chronic kidney diseases progressing to end stage renal failure. However, there are currently no nephroprotective drugs targeted to the fibrotic process in clinical practice.
Jiayi Yang, Yuyi Ruan, Dan Wang, Jinjin Fan, Ning Luo, Huiting Chen, Xiaoyan Li, Wei Chen, Xin Wang   +8 more
doaj   +1 more source

Halofuginone is a Molecular Glue Degrader of Integrin β4

Advanced Science, EarlyView.
Integrin β4 overexpression is linked to aggressive tumors and poor prognosis, but targeted therapies are lacking. We identified halofuginone (HF) as a molecular glue degrader that promotes integrin β4 degradation via the CRL4BWDR18 E3 ligase. HF suppresses tumor progression in vitro and in vivo, offering a new strategy for targeting oncogenic ...
Wei Gong, Di Yang, Junrui Tian, Yufei Chai, Tiantian Yu, Qingnan Wu, Yan Wang, Weimin Zhang, Qimin Zhan   +8 more
wiley   +1 more source