Results 111 to 120 of about 13,195 (282)

Activatable PROTAC nanoassembly for photodynamic PTP1B proteolysis enhances glioblastoma immunotherapy

Acta Pharmaceutica Sinica B
In light of the burgeoning successes of cancer immunotherapy, glioblastoma (GBM) remains refractory due to an immunosuppressive microenvironment originating from its molecular heterogeneity.
Yeongji Jang, Jiwoong Choi, Byeongmin Park, Jung Yeon Park, Jae-Hyeon Lee, Jagyeong Goo, Dongwon Shin, Sun Hwa Kim, Yongju Kim, Hyun Kyu Song, Jooho Park, Kwangmeyung Kim, Yoosoo Yang, Man Kyu Shim   +13 more
doaj   +1 more source

Effective targeting of the survivin dimerization interface with small molecule inhibitors [PDF]

, 2016
Many oncoproteins are considered undruggable because they lack enzymatic activities. In this study, we present a small-molecule–based anticancer agent that acts by inhibiting dimerization of the oncoprotein survivin, thereby promoting its degradation ...
Dong, Zizheng, Liu, Jianguo, Liu, Jingyuan, Peery, Robert C., Qi, Jing, Zhang, Jian-Ting, Zhang, Shaobo   +6 more
core   +1 more source

Scalable Engineering of Bio‐Manufactured Extracellular Vesicles for Selective Delivery in Ovarian Cancer Patient‐Derived Models

Advanced Science, EarlyView.
Engineered extracellular vesicles displaying Ephrin‐B2 selectively target Ephrin‐B4–expressing ovarian cancer cells, enabling precise delivery in patient‐derived models. This scalable bio‐manufacturing platform reveals a versatile strategy to exploit Ephrin signaling for highly specific therapeutic payload delivery and motivates exploration of tailored
Nihar Godbole, Andrew Lai, Alexander Quinn, Marianne Gillard, Dominic Guanzon, Katherin Scholz‐Romero, Alexis Salas‐Burgos, Bastián Lillo Dapremont, Rohan Lourie, Naven Chetty, Richard Lobb, Kate Beecher, Amy E. McCart Reed, Kaltin Ferguson, Biao Sun, Yaowu He, John D. Hooper, Carlos Salomon   +17 more
wiley   +1 more source

Iterative design and optimization of initially inactive Proteolysis Targeting Chimeras (PROTACs) identify VZ185 as a potent, fast and selective von Hippel-Lindau (VHL)-based dual degrader probe of BRD9 and BRD7 [PDF]

, 2018
Developing PROTACs to redirect the ubiquitination activity of E3 ligases and potently degrade a target protein within cells can be a lengthy and unpredictable process, and it remains unclear whether any combination of E3 and target might be productive ...
Ciulli, Alessio, Daniels, Danette L., Gmaschitz, Teresa, Hughes, Scott J., Koegl, Manfred, Maniaci, Chiara, Riching, Kristin M., Spallarossa, Andrea, Testa, Andrea, Wieshofer, Corinna, Zoppi, Vittoria   +10 more
core   +6 more sources

Proteolysis Targeting Chimeras (PROTACs) in Breast Cancer Therapy

ChemMedChem
AbstractBreast cancer (BC) accounts for 30 % of cancer cases among women cancer patients globally, indicating the urgent need for the development of selective therapies targeting BCs. Recently, proteolysis‐targeting chimera (PROTAC) has emerged as a promising strategy to target breast cancer. PROTAC is a chimeric molecule consisting of a target protein
Yerim Jin, Yeongju Lee
openaire   +2 more sources

Genetic Code Expanded T Cell for Controllable Immunotherapy

Advanced Science, EarlyView.
Our GCE‐CAR‐T cells enables tight, dose‐dependent, and function‐preserving control of CAR expression at the translational level through amber codon suppression and genetic incorporation of ncAA. ABSTRACT Chimeric antigen receptor (CAR)‐T cell therapy has demonstrated curative potential against hematologic malignancies, but its clinical application ...
Xue Wang, Yingao Gao, Yeyu Su, Yong Wang, Tao Liu   +4 more
wiley   +1 more source

The Interplay among PINK1/PARKIN/Dj-1 Network during Mitochondrial Quality Control in Cancer Biology: Protein Interaction Analysis [PDF]

, 2018
PARKIN (E3 ubiquitin ligase PARK2), PINK1 (PTEN induced kinase 1) and DJ-1 (PARK7) are proteins involved in autosomal recessive parkinsonism, and carcinogenic processes.
Lucas, Millikin, Narendra, Santel, Zhang
core   +2 more sources

“Membrane‐Guided” Repair Strategy: Precision Delivery of GGT1 Degrader for Targeted Repair and Regeneration of Spinal Cord Neurons

Advanced Science, EarlyView.
This study confirms that GGT1 is a key driver of neuronal ferroptosis following spinal cord injury. We developed NSCm@EA, a biomimetic delivery system coated with neural stem cell membranes, for precise delivery of enocyanin to injured neurons. By combining targeted delivery with ubiquitination degradation mechanisms, this system promotes MGRN1 ...
Tao Yang, Lei Ye, Peigen Xie, Tao Song, Jian Chen, Heng Zhao, Zhengshan Liu, Xi Chen, Jianing Ding, Xintian Ding, Ao Shao, Miaomiao Wu, Fengdong Zhao, Siyue Tao, Tao You   +14 more
wiley   +1 more source

Development of an orally bioavailable CDK12/13 degrader and induction of synthetic lethality with AKT pathway inhibition

Cell Reports Medicine
Summary: Cyclin-dependent kinases 12/13 play pivotal roles in orchestrating transcription elongation, DNA damage response, and maintenance of genomic stability. Biallelic CDK12 loss has been documented in various malignancies.
Yu Chang, Xiaoju Wang, Jianzhang Yang, Jean Ching-Yi Tien, Rahul Mannan, Gabriel Cruz, Yuping Zhang, Josh N. Vo, Brian Magnuson, Somnath Mahapatra, Hanbyul Cho, Saravana Mohan Dhanasekaran, Cynthia Wang, Zhen Wang, Licheng Zhou, Kaijie Zhou, Yang Zhou, Pujuan Zhang, Weixue Huang, Lanbo Xiao, Weihuang Raymond Liu, Rudana Hamadeh, Fengyun Su, Rui Wang, Stephanie J. Miner, Xuhong Cao, Yunhui Cheng, Rohit Mehra, Ke Ding, Arul M. Chinnaiyan   +29 more
doaj   +1 more source

Multiple stable conformations account for reversible concentration-dependent oligomerization and autoinhibition of a metamorphic metallopeptidase [PDF]

, 2010
© 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim. Molecular plasticity controls enzymatic activity: the native fold of a protein in a given environment is normally unique and at a global free-energy minimum. Some proteins, however, spontaneously undergo
López-Pelegrín, Mar, Cerdà-Costa, Núria, Cintas-Pedrola, Anna, Herranz-Trillo, Fátima, Bernadó, Pau, Peinado, Juan Ramón, Arolas, Joan L., Gomis-Rüth, F. Xavier   +7 more
core   +1 more source