SHIP1 therapeutic target enablement: Identification and evaluation of inhibitors for the treatment of late‐onset Alzheimer's disease
Alzheimer s & Dementia Translational Research & Clinical Interventions2023Vol. 9(4), pp. e12429–e12429
Citations Over TimeTop 13% of 2023 papers
Cynthia D. Jesudason, Emily R. Mason, Shaoyou Chu, Adrian L. Oblak, June Javens‐Wolfe, Mustapha Moussaif, Greg Durst, Philip A. Hipskind, Daniel E. Beck, Jiajun Dong, Ovini Amarasinghe, Zhong‐Yin Zhang, Adam Hamdani, Kratika Singhal, Andrew D. Mesecar, Sarah Souza, Marlene Jacobson, Jerry Di Salvo, Disha Soni, Murugesh Kandasamy, Andrea R. Masters, Sara K. Quinney, Suzanne Doolen, Hasi Huhe, Stacey J. Sukoff Rizzo, Bruce T. Lamb, Alan D. Palkowitz, Timothy I. Richardson
Abstract
Cellular thermal shift assay (CETSA) and signaling (pAKT) assays were developed to provide evidence of src homology 2 (SH2) domain-contaning inositol phosphatase 1 (SHIP1) target engagement and on-target activity in cellular assays.A phenotypic high-content imaging assay with simultaneous measures of phagocytosis, cell number, and nuclear intensity was developed to explore cellular pharmacology and monitor cell health.SHIP1 inhibitors demonstrate a wide range of activity and cellular pharmacology, and many reported inhibitors are cytotoxic.The chemical probe 3-((2,4-dichlorobenzyl)oxy)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl) pyridine is recommended to explore SHIP1 pharmacology.
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