Inhibition of discoidin domain receptor (DDR)-1 with nilotinib alters CSF miRNAs and is associated with reduced inflammation and vascular fibrosis in Alzheimer ’s disease
Discoidin Domain Receptor (DDR)-1 is activated by collagen. Nilotinib is a tyrosine kinase inhibitor that is FDA-approved for leukemia and potently inhibits DDR-1. Individuals diagnosed with mild –moderate Alzh... (Source: Journal of Neuroinflammation)
Source: Journal of Neuroinflammation - May 16, 2023 Category: Neurology Authors: Max Stevenson, Rency Varghese, Michaeline L. Hebron, Xiaoguang Liu, Nick Ratliff, Amelia Smith, R. Scott Turner and Charbel Moussa Tags: Research Source Type: research
Exploration of imatinib and nilotinib-derived templates as the P2-Ligand for HIV-1 protease inhibitors: Design, synthesis, protein X-ray structural studies, and biological evaluation
Eur J Med Chem. 2023 Apr 21;255:115385. doi: 10.1016/j.ejmech.2023.115385. Online ahead of print.ABSTRACTStructure-based design, synthesis, X-ray structural studies, and biological evaluation of a new series of potent HIV-1 protease inhibitors are described. These inhibitors contain various pyridyl-pyrimidine, aryl thiazole or alkylthiazole derivatives as the P2 ligands in combination with darunavir-like hydroxyethylamine sulfonamide isosteres. These heterocyclic ligands are inherent to kinase inhibitor drugs, such as nilotinib and imatinib. These ligands are designed to make hydrogen bonding interactions with the backbone...
Source: European Journal of Medicinal Chemistry - May 7, 2023 Category: Chemistry Authors: Arun K Ghosh Jennifer L Mishevich Satish Kovela Ryan Shaktah Ajay K Ghosh Megan Johnson Yuan-Fang Wang Andres Wong-Sam Johnson Agniswamy Masayuki Amano Yuki Takamatsu Shin-Ichiro Hattori Irene T Weber Hiroaki Mitsuya Source Type: research
Exploration of imatinib and nilotinib-derived templates as the P2-Ligand for HIV-1 protease inhibitors: Design, synthesis, protein X-ray structural studies, and biological evaluation
Eur J Med Chem. 2023 Apr 21;255:115385. doi: 10.1016/j.ejmech.2023.115385. Online ahead of print.ABSTRACTStructure-based design, synthesis, X-ray structural studies, and biological evaluation of a new series of potent HIV-1 protease inhibitors are described. These inhibitors contain various pyridyl-pyrimidine, aryl thiazole or alkylthiazole derivatives as the P2 ligands in combination with darunavir-like hydroxyethylamine sulfonamide isosteres. These heterocyclic ligands are inherent to kinase inhibitor drugs, such as nilotinib and imatinib. These ligands are designed to make hydrogen bonding interactions with the backbone...
Source: European Journal of Medicinal Chemistry - May 7, 2023 Category: Chemistry Authors: Arun K Ghosh Jennifer L Mishevich Satish Kovela Ryan Shaktah Ajay K Ghosh Megan Johnson Yuan-Fang Wang Andres Wong-Sam Johnson Agniswamy Masayuki Amano Yuki Takamatsu Shin-Ichiro Hattori Irene T Weber Hiroaki Mitsuya Source Type: research
