Results 101 to 110 of about 827,025 (271)

Biomimetic Scaffold‐Based 3D Models for Decoding Cancer Biology and Advancing Therapy

Advanced Science, EarlyView.
A timeline of the research history of 3D biomimetic scaffold materials and platforms. With advances in biomimetic materials and 3D scaffold technologies, their functional scope has expanded from mimicking basic physical and biochemical properties to increasingly replicating complex pathophysiological processes.
Haitao Zhao, Yuechen Han, Jie Li, Peng Luo, Lin Qi, Zhiwei Xia, Xiaosong Li, Quan Cheng, Chenshen Huang, Wantao Wu, Hao Zhang   +10 more
wiley   +1 more source

Discovery of ARD-2051 as a Potent and Orally Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor for the Treatment of Advanced Prostate Cancer

We report the discovery of ARD-2051 as a potent and orally efficacious androgen receptor (AR) proteolysis-targeting chimera degrader. ARD-2051 achieves DC50 values of 0.6 nM and Dmax >90% in inducing AR protein degradation in both the LNCaP and VCaP ...
Sun, D, Xiang, W, Wang, Y, Metwally, H, Takyi-Williams, J, Mckean, R, Han, X, Lu, J, Qin, C, Zhao, L, Xu, T, McEachern, D, Yang, CY, Kirchhoff, PD, Miao, B, Wang, L, Ator, M, Wang, M, Wen, B, Matvekas, A, Wang, S   +20 more
core   +1 more source

Palmitoyl Acyltransferase Zdhhc17 Promotes Functional Recovery After Spinal Cord Injury by Targeting the Nuclear Transport Factors Kpna2 and Ipo9

Advanced Science, EarlyView.
In this study, we demonstrate that Zdhhc17, acting as a PAT, suppresses neuronal apoptosis and promotes axon regeneration after injury, thereby enhancing functional recovery following SCI. In this context, Kpna2 and Ipo9 serve as novel palmitoylation substrates of Zdhhc17, whose palmitoylation prevents the injury‐induced degradation of their proteins ...
Meixuan Chen, Huan Chen, Sining Ding, Fan Liu, Xiaofei Zheng, Yuan Wang, Ruitu Tian, Huan Li, Peilin Liu, Le Hu, Bin Liu, Limin Rong, Mangmang Li   +12 more
wiley   +1 more source

Degrading GPX4 via Biomimetic Nanoparticle‐Mediated In Situ Synthesis of Deep‐Learning‐Designed Binder‐Degron Chimeras for Prostate Cancer Therapy

Advanced Science, EarlyView.
A deep‐learning‐designed binder is fused to a combinatorial degron to create a binder‐degron chimera (bdC) that recruits the CUL2‐RING ubiquitin ligase complex. Encapsulation in a prostate‐cancer‐targeted, CD47‐camouflaged nanocarrier enables tumor‐specific in situ bdC expression, triggering GPX4 degradation and ferroptosis, thereby establishing a ...
Si‐Han Zhang, Ye An, Na Zeng, Mei‐Cheng Liu, Jian‐Xuan Sun, Xi Gong, Jin‐Zhou Xu, Shao‐Gang Wang, Qi‐Dong Xia   +8 more
wiley   +1 more source

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

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

Methylated Nucleotide-Based Proteolysis-Targeting Chimera Enables Targeted Degradation of Methyl-CpG-Binding Protein 2

Methyl-CpG-binding protein 2 (MeCP2), a reader of DNA methylation, has been extensively investigated for its function in neurological and neurodevelopmental disorders. Emerging evidence indicates that MeCP2 exerts an oncogenic function in cancer; however,
Li Chen (5749), Wenyi Wei (6911471), Zhen Wang (72451), Xing Qiu (560143), Hiroyuki Inuzuka (12378227), He Chen (104732), Xian Chen (107385), Dingpeng Zhang (6052529), Jing Liu (38537), Ling Xie (2026981), H. Ümit Kaniskan (1476325), Jian Jin (351142)   +11 more
core   +1 more source

In Situ Bioorthogonal Synthesis of PROTACs via Dual‐Responsive Cleavage for Synergistic Photo‐Immunotherapy

Advanced Science, EarlyView.
A bioactive self‐delivering SNAP‐TAC platform responds to tumor‐associated cathepsin B and glutathione, enabling in situ bioorthogonal synthesis of a BRD4‐degrading proteolysis‐targeting chimera within the tumor microenvironment. The resulting BRD4 degradation and PD‐L1 downregulation synergize with photodynamic therapy‐induced immunogenic cell death ...
Shiqin Jian, Jiasha Wu, Fusheng Xu, Yan Zuo, Huaxing Shen, Rui Ji, Luyi Wang, Na Li, Yanting Sun, Yongsheng Yu, Yejiao Shi, Honggang Hu, Feng Xu, Dan Huang, Xiaochun Hu   +14 more
wiley   +1 more source

AI‐Designed TREM1‐Targeted LYTAC Nanoparticles Reprogram the Neuroimmune Microenvironment in Traumatic Brain Injury

Advanced Science, EarlyView.
AI‐enabled de novo design of a TREM1 binder, integrated into a BBB‐crossing and macrophage‐targeted nanoplatform, enables TREM1 degradation and attenuates neuroinflammation, thereby promoting neuroprotection and tissue repair after traumatic brain injury. ABSTRACT Secondary neuroinflammation drives progressive damage after traumatic brain injury (TBI),
Yimin Huang, Yuan Liu, Huan Peng, Yu Ni, Zhengqiao Jiang, Chenxuan Yu, Xincheng Zhang, Huayu Kang, Yanchao Liu, Juan Chen, Kai Zhao, Lin Han, Xin Zou, Kai Shu, Xiaochuan Wang, Jian‐Zhi Wang, Ting Lei, Chao Gan, Jianfeng Liu, Huaqiu Zhang   +19 more
wiley   +1 more source

PROteolysis TArgeting Chimeras (PROTACs) — Past, present and future

Drug Discovery Today: Technologies, 2019
The majority of currently used therapeutics are small molecule-based and utilize occupancy-driven pharmacology as the mode of action (MOA), in which the protein function is modulated via temporary inhibition. New modalities that operate using alternative MOAs are essential for tapping into the "undruggable" proteome.
Mariell Pettersson, Craig M. Crews
openaire   +2 more sources