Results 121 to 130 of about 504,547 (295)

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

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

Recognition of phylogenetically diverse pathogens through enzymatically amplified recruitment of RNF213

EMBO Reports
Innate immunity senses microbial ligands known as pathogen-associated molecular patterns (PAMPs). Except for nucleic acids, PAMPs are exceedingly taxa-specific, thus enabling pattern recognition receptors to detect cognate pathogens while ignoring others.
Ana Crespillo-Casado, Prathyush Pothukuchi, Katerina Naydenova, Matthew C J Yip, Janet M Young, Jerome Boulanger, Vimisha Dharamdasani, Ceara Harper, Pierre-Mehdi Hammoudi, Elsje G Otten, Keith Boyle, Mayuri Gogoi, Harmit S Malik, Felix Randow   +13 more
doaj   +1 more source

CRBN E3 ligase modulators (CELMoDs) as potential alternative for immunomodulatory drug (IMiD) resistance in CRBN-based targeted therapy

Results in Chemistry
Cereblon (CRBN), a promising substrate receptor of the CRL4 E3 ubiquitin ligase complex is recruited by small-molecule ligands to mediate the selective degradation of target proteins in cancer therapy. Immunomodulatory drugs (IMiDs) are the most commonly
E. Rosette Celsiya Mary, C. Sudandiradoss   +1 more
doaj   +1 more source

Tumor‐Intrinsic HEXB Drives Endothelial‐To‐Mesenchymal Transition and Confers Resistance to Anti‐Angiogenic Therapy in Glioblastoma

Advanced Science, EarlyView.
This study elucidates how glioblastoma tumors develop resistance to anti‐VEGF therapy through endothelial‐to‐mesenchymal transition (Endo‐MT). The researchers identify a novel signaling pathway where tumor‐derived HEXB stabilizes HSP60 to drive this vascular reprogramming.
Tianqi Liu, Xin Chen, Tao Sun, Jianqi Wu, Haixu Yan, Xing Liu, Hongda Lin, Xiangyu Wang, Ziao Xiao, Yang Xu, Qiang Fu, Peng Cheng, Wen Cheng, Anhua Wu   +13 more
wiley   +1 more source

Mitochondrial Quality Control in Degenerative Musculoskeletal Diseases: Signaling Networks and Therapeutic Landscapes

Advanced Science, EarlyView.
Mitochondrial quality control (MQC) collapse redefines osteoarthritis, intervertebral disc degeneration, and osteoporosis as disorders of organelle dysfunction. Damaged mitochondria leak mtDNA and metabolites, driving cGAS‐STING inflammation, epigenetic reprogramming, and metabolic memory.
Haiyang Gao, Zhangrong Cheng, Xianglong Chen, Wenbo Wu, Wang Wu, Zimu Yu, Cao Yang, Yukun Zhang   +7 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

Advances in KEAP1-based PROTACs as emerging therapeutic modalities: Structural basis and progress

Redox Biology
Kelch-like ECH-associated protein 1 (KEAP1) functions as a substrate adaptor for the Cullin 3-RING E3 ligase complex, mediating the ubiquitination and subsequent proteasomal degradation of nuclear factor erythroid 2-related factor 2 (NRF2).
Jing Chen, Disheng Feng, Rui Zhu, Hua Li, Lixia Chen   +4 more
doaj   +1 more source

FKBP51 and FKBP12.6-Novel and tight interactors of Glomulin.

PLoS ONE, 2019
The protein factor Glomulin (Glmn) is a regulator of the SCF (Skp1-CUL1-F-box protein) E3 ubiquitin-protein ligase complex. Mutations of Glmn lead to glomuvenous malformations.
Andreas Hähle, Thomas M Geiger, Stephanie Merz, Christian Meyners, Mao Tianqi, Jürgen Kolos, Felix Hausch   +6 more
doaj   +1 more source

Tubocapsenolide A Overcomes Oxaliplatin Resistance in Colorectal Cancer by Targeting PLK1 to Impair CEP55–ESCRT‐Associated Vesicular Damage Clearance

Advanced Science, EarlyView.
Oxaliplatin‐resistant colorectal cancer cells utilize a previously unappreciated PLK1‐CEP55‐ESCRT‐driven vesicular extrusion mechanism to clear L‐OHP‐induced cellular damage. The natural withanolide Tubocapsenolide A directly targets and inhibits PLK1 to disrupt this specific damage‐clearance machinery. This blockade induces severe nucleolar stress and
Yueying Yang, Jing Liang, Lu Wang, Hongyan Zhang, Zhiruo Zhang, Yang Liu, Rui Zhu, Wen Xu, Shaohua Xu, Dejuan Sun, Ke Xiang, Yali Wang, Zhimin Fan, Zheng Wang, Hua Li, Lixia Chen   +15 more
wiley   +1 more source