Category Ranking
98%
Total Visits
921
Avg Visit Duration
2 minutes
Citations
20
Article Abstract
Zerumbone is a phytochemical with diverse biological activities ranging from anti-inflammatory to anti-cancer properties; however, to date the cellular targets of this important compound have remained elusive. Here we report the global protein target spectrum of zerumbone in living cancer cells using competitive activity-based protein profiling of a novel cell-permeable clickable probe, combined with quantitative mass spectrometry.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1039/c4cc09527h | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Development of cell-permeable and plasma-stable peptidomimetic inhibitors against PSD-95/nNOS interaction as potential anti-ischemic stroke agents.
Eur J Med Chem
December 2025
Department of Medicinal Chemistry, School of Pharmacy, Qingdao University, Qingdao, 266021, China. Electronic address:
The N-methyl-d-aspartate receptor (NMDAR)-neuronal nitric oxide synthase (nNOS)-postsynaptic density-95 (PSD-95) ternary complex represents a promising therapeutic target for acute ischemic stroke treatment. Although the shortest peptide ETAV targeting the PDZ2 domain of PSD-95 shows therapeutic potential, its limit in vivo stability restricts its broad application. Therefore, we herein systematically optimized and developed a series of novel peptidomimetics based on ETAV.
View Article and Find Full Text PDFA Chimeric Peptide Derived from a Bacterial Effector Protein Attenuates TLR-2/4-Mediated Production of Pro-Inflammatory Cytokines and Enhances the Cellular Availability of Gentamicin.
J Inflamm Res
August 2025
Laboratory of Bacterial Pathogenesis, National Institute of Animal Biotechnology, Hyderabad, Telangana, 500032, India.
Introduction: Toll-like receptors (TLRs) are critical components of innate immunity, recognizing microbe-derived molecules and triggering pro-inflammatory cytokine production for pathogen clearance. However, TLR hyperactivation can cause excessive inflammation, contributing to disorders such as sepsis. Thus, modulating TLR signalling is a promising therapeutic strategy.
View Article and Find Full Text PDFC-Arg9-APCR3-VHL promotes β-catenin degradation via the VHL-mediated ubiquitin-proteasome system in APC-mutant colorectal cancer.
Int J Biol Macromol
September 2025
Colorectal surgery department, The Third Affiliated Hospital of Kunming Medical University, Kunming 650106, Yunnan, China. Electronic address:
Mutations in the adenomatous polyposis coli (APC) gene are common in colorectal cancer (CRC) and result in deregulation of β-catenin, a key driver of tumor initiation and progression. Despite its central role, targeted degradation of β-catenin remains an unmet therapeutic need in APC-mutant CRC. This study introduces and evaluates C-Arg9-APCR3-VHL, a novel PROTAC designed to promote β-catenin degradation via the VHL-Mediated ubiquitin-proteasome pathway.
View Article and Find Full Text PDFDimethyl-2-oxoglutarate but not antioxidants prevents glucose hypometabolism induced neural cell death: implications in the pathogenesis and therapy of Alzheimer's disease.
Biochem Biophys Rep
September 2025
Department of Biochemistry, Dr B. C. Roy Multi-Speciality Medical Research Centre, Indian Institute of Technology, Kharagpur, West Bengal, India.
Cerebral glucose hypometabolism is a cardinal molecular signature of Alzheimer's disease, and its role in the pathogenesis of this disorder is under intensive study in both animal and cell-based models. In the current study, we exposed SH-SY5Y cells (human neuroblastoma cell line) over a period of 48 h to DRB18, an inhibitor of multiple glucose transporters, in different concentrations to develop a state of glucose hypometabolism. Under this metabolic insult, in SH-SY5Y cells a profound dose-dependent neural cell death, an increased production of reactive oxygen radicals, mitochondrial membrane depolarization and a depletion of cellular ATP content were noted; these effects were not prevented by lipid-soluble novel antioxidants such as ferrostatin-1 and liproxstatin-1 or by a general water-soluble antioxidant like N-acetylcysteine.
View Article and Find Full Text PDFHigh-Throughput Evaluation of Cryoprotective Agents for Mixture Effects That Reduce Toxicity.
bioRxiv
May 2025
School of Chemical, Biological and Environmental Engineering, Oregon State University.
Vitrification is a promising approach for cryopreserving complex biological structures such as organs. However, to prevent ice formation, high concentrations of cell-permeable cryoprotective agents (CPAs) are required, which can be highly toxic. The current reliance on a small number of CPAs limits optimization of low-toxicity compositions for vitrification.
View Article and Find Full Text PDF