Ontology highlight
ABSTRACT:
INSTRUMENT(S): Orbitrap Fusion Lumos
ORGANISM(S): Homo Sapiens (human)
SUBMITTER: Travis Ruan
LAB HEAD: Mark Larance
PROVIDER: PXD027300 | Pride | 2022-02-17
REPOSITORIES: Pride
Ashhurst Anneliese S AS Tang Arthur H AH Fajtová Pavla P Yoon Michael C MC Aggarwal Anupriya A Bedding Max J MJ Stoye Alexander A Beretta Laura L Pwee Dustin D Drelich Aleksandra A Skinner Danielle D Li Linfeng L Meek Thomas D TD McKerrow James H JH Hook Vivian V Tseng Chien-Te CT Larance Mark M Turville Stuart S Gerwick William H WH O'Donoghue Anthony J AJ Payne Richard J RJ
Journal of medicinal chemistry 20211103 4
Cathepsin L is a key host cysteine protease utilized by coronaviruses for cell entry and is a promising drug target for novel antivirals against SARS-CoV-2. The marine natural product gallinamide A and several synthetic analogues were identified as potent inhibitors of cathepsin L with IC<sub>50</sub> values in the picomolar range. Lead molecules possessed selectivity over other cathepsins and alternative host proteases involved in viral entry. Gallinamide A directly interacted with cathepsin L ...[more]