Results 101 to 110 of about 823,777 (226)

H4K12 Lactylation Regulates NDUFS7 to Drive Microglia Reverse Electron Transport in Spinal Cord Injury

Advanced Science, EarlyView.
Lactate accumulation after SCI promotes H4K12la lactylation, which upregulates NDUFS7, triggering mitochondrial RET and ROS, enforcing pro‐inflammatory microglial polarization. MM@mPTC, a biomimetic nanotherapeutic, degrades LDHA in activated microglia, reducing H4K12la lactylation and blocking RET, thus curbing ROS, fostering a reparative phenotype ...
Chenglong Hong, Zhichen Jiang, Zhouwei Wu, Chenyu Wu, Jiang Liu, Kaijie Guo, Yihui Liang, Shaobo Xu, Yuchen Jin, Yong Xiao, Lei Guo, Hui Xu, Sunren Sheng, Chenggui Wang   +13 more
wiley   +1 more source

Orthogonal Light‐ and Enzyme‐Triggered and‐Gate Prodrugs for Senolytic Therapy

Advanced Science, EarlyView.
An orthogonal AND‐gate prodrug platform combines 390 nm near‐UV photocleavage with SA‐β‐gal activation to control payload release in senescent cells. Its modular architecture enables 4‐MU fluorescence, doxorubicin‐mediated cytotoxicity, and ARV‐771‐driven BRD4 degradation, supporting stimulus‐controlled senolytic design in cellular and organoid models.
Mengyang Chang, Kaixue Zhang, Junwei Wang, Fangchao Bi, Zhuoxin Dai, Miao Yang, Ming Liu, Huanzhi Peng, Franklin Zhang, Yuan Guo, Jigang Dai, Quanxing Liu, Wei Wang   +12 more
wiley   +1 more source

From Inhibition to Degradation: Targeting the Anti-apoptotic Protein Myeloid Cell Leukemia 1(MCL1) [PDF]

, 2019
Here we show the development of heterobifunctional small molecules capable of selectively targeting MCL1 using a Proteolysis Targeting Chimera (PROTAC) methodology leading to successful degradation. We have confirmed the involvement of the
Ranjan, Maity, James, Papatzimas, Paola, Neri, Nizar J., Bahlis, Evgueni, Gorobets, Justin L., MacCallum, Darren, Derksen, Mir Ishruna, Muniyat   +7 more
core   +1 more source

Generalizable Strategies for the Synthesis of Cereblon-Recruiting PROTAC Prodrugs. [PDF]

Angew Chem Int Ed Engl
Cereblon‐recruiting PROTACs remain challenging to derivatize for prodrug‐based delivery. In this study, three complementary conjugation strategies enabled the efficient synthesis of cleavable PROTAC prodrugs with tunable release kinetics that can be incorporated into a library of PEGylated constructs and bottlebrush prodrugs.
Wang AX, Liu B, Ackerman EM, Xiang Y, Nguyen HV, Jiang Y, Koehler AN, Johnson JA.   +7 more
europepmc   +3 more sources

Tackling cancer stemness with nanotechnology in the era of precision medicine

BMEMat, EarlyView.
Precise customization of nanoparticles (NPs) enables active targeting of cancer stem cells (CSCs), thereby improving drug delivery and therapeutic efficacy. NP‐based probing enhances CSC detection through imaging and liquid biopsy, whereas diverse therapeutic payloads improve therapeutic outcomes.
Shaolei Guo, Shun Yao, Lihui Meng, Chunyuan Chen, Yuechu Lucinda Lu, Rong Lu, Kashif Rafiq Zahid, Umar Raza, Qingzhi Wu, Wenli Chen   +9 more
wiley   +1 more source

HSP70 Interactome‐Mediated Proteolysis Targeting Chimera (HSP70‐PROTAC) for Ferroptosis‐Driven Cancer Treatment

Targeted protein degradation (TPD) represents a transformative therapeutic paradigm that harnesses the cellular degradation machinery to pharmacologically eliminate disease‐causing proteins with aberrant expression.
Shiqun Wang, Jinyun Dong, Lan, Yanning, Yichao Wang, Chen, Zhe\u2010Sheng, Jieyu Xu, Miao, Kai, Guangzhao Pan, Zhe‐Sheng Chen, Hui Liang, Qin, Jiang\u2010Jiang, Yanning Lan, Haiyan Yang, Jiang‐Jiang Qin, Cai, Maohua, Li, Yulong, Pan, Guangzhao, Maohua Cai, Ma, Xuelei, Fangfang Tao, Xuelei Ma, Wu, Zumei, Zumei Wu, Yang, Haiyan, Wang, Shiqun, Xu, Jieyu, Wang, Yichao, Dong, Jinyun, Liang, Hui, Yulong Li, Tao, Fangfang, Kai Miao   +31 more
core   +1 more source

Multi‐omics–driven precision medicine

iMeta, EarlyView.
Multi‐omics‐driven precision medicine (MODPM) provides a multiscale, continuously learnable framework that integrates genomics, epigenomics, transcriptomics, proteomics, metabolomics, microbiome profiles, and clinical data. Powered by artificial intelligence and foundation models, MODPM enables cross‐modal representation learning, contextual modeling ...
Huibo Li, Zhe Zhao, Yifan Zhang, Yao Ma, Gaofei Hu, Min Zeng, Zhanqun Yang, Zixuan Zhao, Xin Zhou, Wei Hu, Yuxuan Sun, Meng Su, Jun Li, Matthew Whiteman, Wei Fu, Chao Zhong, Lemin Zheng, Long Chen, Hairong Lv, Rongsheng Zhao, Yi Zhun Zhu   +20 more
wiley   +1 more source

Data for: Discovery of Potent Proteolysis Targeting Chimera Degrader of IDO1

, 2020
Supplementary Information for Discovery of Potent Proteolysis Targeting Chimera Degrader of ...
Yongmei Xie (5162336), Tinghong Ye (506838), Yijie Wang (90004), Dongping Yao (8598066), Yuqin Yao (2279452), Mingxing Hu (8598063), Xifei Yang (323243), Wei Wang (17594), Bin Chen (63682), Weilin Zhou (1981888), Gong-Ping Liu (636544)   +10 more
core   +1 more source

PROTACs therapeutically target the polyglutamine androgen receptor in spinal and bulbar muscular atrophy models

Neurotherapeutics
Spinal and bulbar muscular atrophy (SBMA) is a CAG/polyglutamine (polyQ) repeat expansion disorder in which the mutant androgen receptor (AR) protein triggers progressive degeneration of the neuromuscular system in men.
Agamjot Sangotra, Satya L. Reddy, Curtis J. Kuo, Weiguo Xiang, Diane E. Merry, Christopher Grunseich, Shaomeng Wang, Andrew P. Lieberman   +7 more
doaj   +1 more source

Specific MHC-I Peptides Are Induced Using PROTACs

Frontiers in Immunology, 2018
Peptides presented by the class-I major histocompatibility complex (MHC-I) are important targets for immunotherapy. The identification of these peptide targets greatly facilitates the generation of T-cell-based therapeutics.
Stephanie M. Jensen, Gregory K. Potts, Damien B. Ready, Melanie J. Patterson   +3 more
doaj   +1 more source