Comb Chem High Throughput Screen
January 2025
Background: Cisplatin is an effective anti-cancer drug with limited clinical applications due to ototoxicity. Resveratrol, known for its antioxidant and anti-inflammatory properties, has been reported to mitigate these adverse effects, although the underlying mechanism remains under-researched.
Objective: This study aimed to investigate the effects and underlying mechanisms of resveratrol on cisplatin-induced ototoxicity.
The bromination of α-oxo ketene dithioacetals using KBr/HO, catalyzed by vanadium chloroperoxidase (VCPO), has been successfully demonstrated. A comparative study of enzymatic processes "on water" "in water", using 2 wt% of the surfactant TPGS-750-M revealed that the in-water protocol not only provides higher yields but also accommodates a broader substrate scope. This bromination method in an aqueous micellar medium enabled the preparation of brominated α-oxo ketene dithioacetals in fair to excellent yields (23 examples).
View Article and Find Full Text PDFResearch (Wash D C)
January 2025
Immune recognition and activation by the peptide-laden major histocompatibility complex-T cell receptor (TCR)-CD3 complex is essential for anti-tumor immunity. Tumors may escape immune surveillance by dissembling the complex. Here, we report that transferrin, which is overexpressed in patients with liver metastasis, disassociates TCR from the CD3 signaling apparatus by targeting the constant domain (CD) of T cell receptor α (TCRα), consequently suppresses T cell activation, and inhibits anti-metastatic and anti-tumor immunity.
View Article and Find Full Text PDFBackground: There are no approved oral disease-modifying treatments for Alzheimer's disease (AD).
Objectives: The objective of this study was to assess efficacy and safety of blarcamesine (ANAVEX®2-73), an orally available small-molecule activator of the sigma-1 receptor (SIGMAR1) in early AD through restoration of cellular homeostasis including autophagy enhancement.
Design: ANAVEX2-73-AD-004 was a randomized, double-blind, placebo-controlled, 48-week Phase IIb/III trial.