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Proteomic Profiling of Medullary Thyroid Cancer Identifies CAPN1 as a Key Regulator of NF1 and RET Fueled Growth.
Thyroid
January 2025
Department of Cancer Biology and Genetics, The Ohio State University, Columbus, Ohio, USA.
Medullary thyroid cancer (MTC) is a frequently metastatic tumor of the thyroid that develops from the malignant transformation of C-cells. These tumors most commonly have activating mutations within the RET or RAS proto-oncogenes. Germline mutations within RET result in C-cell hyperplasia, and cause the MTC pre-disposition disorder, multiple endocrine neoplasia, type 2A (MEN2A).
View Article and Find Full Text PDFDendritic Antifungal Peptides as Potent Agents against Drug-Resistant and Biofilm.
J Med Chem
January 2025
College of Animal Science and Technology, Northeast Agricultural University, Harbin 150030, P. R. China.
infection is a major public health problem, exacerbated by the emergence of drug-resistant fungi with the widespread use of antifungal drugs. Therefore, the development of novel antifungal drugs for drug-resistant infections is crucial. We constructed a series of dendritic antifungal peptides (AFPs) with different chain lengths of fatty acids as hydrophobic ends and 2 or 3 protease-stable repeats (Arg-Pro) as dendritic peptide branches.
View Article and Find Full Text PDFProtease-activated receptor 2 (PAR2) is a central regulator of intestinal barrier function, inflammation and pain. Upregulated intestinal proteolysis and PAR2-signaling are implicated in inflammatory bowel diseases (IBDs) and irritable bowel syndrome (IBS). To identify potential bacterial regulators of PAR2 activity, we developed a functional assay for PAR2 processing and used it to screen conditioned media from a library of diverse gut commensal microbes.
View Article and Find Full Text PDFRA-0002034 ( ) is a potent covalent inhibitor targeting the alphavirus nsP2 cysteine protease. The species-dependent pharmacokinetics and metabolism of were investigated to evaluate its therapeutic potential. Pharmacokinetic profiling revealed rapid clearance in mice, predominantly mediated by glutathione -transferase (GST)-catalyzed conjugation.
View Article and Find Full Text PDFMitigating dithiothreitol interference to gold/thiol interface in electrochemical detection of cathepsin B activity toward multiplex protease analysis.
Biosens Bioelectron
January 2025
Department of Chemistry, Kansas State University, Manhattan, KS, 66502, USA. Electronic address:
Proteases are overexpressed at various stages of conditions such as cancers and thus can serve as biomarkers for disease diagnosis. Electrochemical techniques to detect the activity of extracellular proteases have gained attraction due to their multiplexing capability. Here we employ an electrochemical approach based on a 3 × 3 gold (Au) microelectrode array (MEA) functionalized with (2-aminoethyl)ferrocene (AEF) tagged specific peptide substrates to monitor cathepsin B (CB) protease activity.
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