Results 111 to 120 of about 13,155 (273)

Unraveling the Role of Linker Design in Proteolysis Targeting Chimeras.

Journal of medicinal chemistry, 2021
A current bottleneck in the development of proteolysis targeting chimeras (PROTACs) is the empirical nature of linker length structure-activity relationships (SARs). A multidisciplinary approach to alleviate the bottleneck is detailed here. First, we examine four published synthetic approaches that have been developed to increase synthetic throughput ...
Bemis, Troy A, La Clair, James J, Burkart, Michael D   +2 more
openaire   +3 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

“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

Different Flour Microbial Communities Drive to Sourdoughs Characterized by Diverse Bacterial Strains and Free Amino Acid Profiles [PDF]

, 2016
This work aimed to investigate whether different microbial assemblies in flour may influence the microbiological and biochemical characteristics of traditional sourdough.
Fabio Minervini, Giuseppe Celano, Marco Gobbetti, Maria De Angelis   +3 more
core   +2 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

ZDHHC18‐Mediated Palmitoylation of ORF3a Promotes SARS‐CoV‐2 Pathogenesis by Antagonizing TRIM16‐Mediated Ubiquitination and Proteasomal Degradation

Advanced Science, EarlyView.
Palmitoylation by ZDHHC18 blocks ORF3a K27‐linked ubiquitination mediated by TRIM16, thereby preventing its proteasomal degradation and strengthening viral pathogenesis. Targeting palmitoylation through a pharmacological inhibitor (2‐BP), a competitive inhibitory peptide (OPIP), or adenovirus‐mediated knockdown of ZDHHC18 expression presents a ...
Sidi Yang, Kun Li, Lihong Liu, Linsen Zeng, Qifeng Deng, Jiacheng Huang, Xiaoran Dong, Xin Wang, Jianwei Liang, Hongchao Liu, Hong Peng, Yuxin Lin, Xiaolu Xie, Yuzhen Ye, Tiefeng Xu, Zhaohuan Wang, Chun‐Mei Li, Deyin Guo   +17 more
wiley   +1 more source

Developmental biology of the pancreas [PDF]

, 2018
In this review, I summarize some aspects of murine pancreas development, with particular emphasis on the analysis of the ontogenetic relationships between different pancreatic cell types.
Merino, Pedro
core  

Pathophysiology of acute experimental pancreatitis: Lessons from genetically engineered animal models and new molecular approaches [PDF]

, 2005
The incidence of acute pancreatitis is growing and worldwide population-based studies report a doubling or tripling since the 1970s. 25% of acute pancreatitis are severe and associated with histological changes of necrotizing pancreatitis. There is still
Anne Barbara Tietz, Arnush M, Bhagat L, Bhatia M, Bhatia M, Bockman DE, Burkhard Göke, Claus Schäfer, Demols A, Ebert MP, Frossard JL, Gardner JD, Gerard C, Grady T, Grisham M, Gu D, Gukovskaya AS, Gukovsky I, Hahm KB, Halangk W, Halangk W, Korc M, Lee MS, Leser HG, Massague J, Meda P, Norman J, Ohnishi H, Ohnishi H, Ohnishi H, Roberts AB, Saluja A, Schafer C, Schafer C, Schmid RM, Song AM, Steinle A, Van Acker GJD, Vogelmann R   +38 more
core   +1 more source

T‐Cell Exhaustion in the Tumor Microenvironment: Subcellular Dysfunction, Pan‐Cancer Characteristics, and Therapeutic Interventions

Advanced Science, EarlyView.
This study elucidates the mechanisms of subcellular multidimensional collapse in exhausted T cells. By specifically targeting the nucleus, mitochondria, and endoplasmic reticulum, strategic interventions can effectively remodel the compromised organelle network. This integrated approach drives comprehensive T cell resuscitation, ultimately establishing
Mingxing Wang, Wanhui Dong, Jian Chen, Zhangjie Zhou, Shujuan Fu, Tingting Wu, Haiyan Jiang, Zhiying Wang, Zhixian Zhong, Yi Zhong   +9 more
wiley   +1 more source