Document Report Card

ID: ALA2321771

Journal: ACS Med Chem Lett

Title: Inhibition of Ebola Virus Infection: Identification of Niemann-Pick C1 as the Target by Optimization of a Chemical Probe.

Authors: Lee K, Ren T, Côté M, Gholamreza B, Misasi J, Bruchez A, Cunningham J.

Abstract: A high throughput screen identified adamantane dipeptide 1 as an inhibitor of Ebola virus (EboV) infection. Hit-to-lead optimization to determine the structure-activity relationship (SAR) identified the more potent EboV inhibitor 2 and a photoaffinity labeling agent 3. These anti-viral compounds were employed to identify the target as Niemann-Pick C1 (NPC1), a host protein that binds the EboV glycoprotein and is essential for infection. These studies establish NPC1 as a promising target for anti-viral therapy.

CiteXplore: 23526644

DOI: 10.1021/ml300370k