Remove 2024 Remove Fragment Screening Remove Treatment
article thumbnail

Covalent Fragment Screening and Optimization Identifies the Chloroacetohydrazide Scaffold as Inhibitors for Ubiquitin C-terminal Hydrolase L1

Covalent Modifiers

Flaherty Journal of Medicinal Chemistry 2024 DOI: 10.1021/acs.jmedchem.3c01661 Thus, UCHL1 inhibitors could serve as a viable treatment strategy against these aggressive cancers. Herein, we describe a covalent fragment screen that identified the chloroacetohydrazide scaffold as a covalent UCHL1 inhibitor. Muli, Aaron D.

article thumbnail

Advancements in hit identification for membrane protein drug discovery

Drug Target Review

This receptor is also expressed in the brain, where it helps to regulate dopamine release, making it a therapeutic target for the treatment of insomnia, pain, depression and Parkinson’s disease. Available at: [link] (Accessed: 23 September 2024). References Sun D, et al. Jones EM, et al. doi:10.7554/elife.54895.