Results 81 to 90 of about 7,362 (230)

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

Synthesis, biological evaluation and clinical trials of Cereblon-based PROTACs

Communications Chemistry
PROteolysis-Targeting Chimeras (PROTACs) are an emerging class of molecules capable of inducing a forced approximation between a protein of interest (POI) and an E3 ligase enzyme (e.g., Cereblon), leading to the degradation of the POI by the cell’s own ...
André T. S. Vicente, Sara P. S. P. Moura, Jorge A. R. Salvador   +2 more
doaj   +1 more source

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

PROTAC-based protein degradation: a window of opportunity for melanoma therapy

Journal of Biomedical Science
The key small molecule-based modalities for inducing targeted protein degradation have seen explosive growth over the past decade. They include heterobifunctional degraders such as PROteolysis TArgeting Chimeras (PROTACs): molecules working as protein ...
Giulia Gentile, Simona D’Aguanno, Marta Di Martile, Adele Petricca, Elisabetta Valentini, Stefano Scalera, Donatella Del Bufalo   +6 more
doaj   +1 more source

Advancing cancer immunotherapy: Small-Molecule, biomacromolecular, and nanoscale PROTACs targeting PD-L1 for degradation

Materials Today Advances
Programmed death-ligand 1 (PD-L1) is a key immune checkpoint protein that enables tumor immune evasion by engaging PD-1 on T cells, thereby inhibiting their cytotoxic function.
Yang Meng, Yujing Zhang, Wanpeng Yu, Dongming Xing, Chao Wang   +4 more
doaj   +1 more source

Mitochondria‐endoplasmic reticulum organelle glue as maturation promoter for origination/dimensional dual‐cross cardiomyocytes

BMEMat, EarlyView.
Mitochondria‐endoplasmic reticulum contact sites (MERCS) are areas where the mitochondria and endoplasmic reticulum closely interact. In this study, we utilize synthetic organelle glues to artificially engineer MERCS for regulating cardiomyocyte development, through which the immature and chemo‐plasticity issues of undifferentiated cells are addressed.
Wei Tang, Hao Sun, Chenqi Duan, Jiajia Chang, Yuxing Wang, Ming Zhao, Huiyue Zhao, Shan Lu, Yang Yang, Da Huo   +9 more
wiley   +1 more source

Crystal structures of DCAF1-PROTAC-WDR5 ternary complexes provide insight into DCAF1 substrate specificity

Nature Communications
Proteolysis-targeting chimeras (PROTACs) have been explored for the degradation of drug targets for more than two decades. However, only a handful of E3 ligase substrate receptors have been efficiently used. Downregulation and mutation of these receptors
Mark F. Mabanglo, Brian Wilson, Mahmoud Noureldin, Serah W. Kimani, Ahmed Mamai, Chiara Krausser, Héctor González-Álvarez, Smriti Srivastava, Mohammed Mohammed, Laurent Hoffer, Manuel Chan, Jamie Avrumutsoae, Alice Shi Ming Li, Taraneh Hajian, Sarah Tucker, Stuart Green, Magdalena Szewczyk, Dalia Barsyte-Lovejoy, Vijayaratnam Santhakumar, Suzanne Ackloo, Peter Loppnau, Yanjun Li, Almagul Seitova, Taira Kiyota, Jue George Wang, Gilbert G. Privé, Douglas A. Kuntz, Bhashant Patel, Vaibhavi Rathod, Anand Vala, Bhimsen Rout, Ahmed Aman, Gennady Poda, David Uehling, Jailall Ramnauth, Levon Halabelian, Richard Marcellus, Rima Al-awar, Masoud Vedadi   +38 more
doaj   +1 more source

Fibrilpaint: A Class of Amyloid‐Targeting Peptides

Chemistry – A European Journal, EarlyView.
FibrilPaints are modular peptides engineered to recognize amyloid fibrils. By systematically varying charge, sequence, and termini, their binding behavior can be tuned while retaining recognition. Successful binding ″paints″ fibrils for visualization and opens routes toward targeted degradation and diagnostic applications.
Júlia Aragonès Pedrola, Françoise A. Dekker, Katrin Guttmann, Litske M. van Leeuwen, Shalini Singh, Guy Mayer, Tommaso Garfagnini, Assaf Friedler, Stefan G. D. Rüdiger   +8 more
wiley   +1 more source

Cellular parameters shaping pathways of targeted protein degradation

Communications Biology
In recent years the development of proteolysis-targeting chimeras (PROTACs) has enhanced the field of ubiquitin signalling through advancing therapeutic targeted protein degradation (TPD) strategies and generating tools to explore the ubiquitin landscape.
Annabel Cardno, Bryony Kennedy, Catherine Lindon   +2 more
doaj   +1 more source