Fiche publication
Date publication
décembre 2023
Journal
Journal of enzyme inhibition and medicinal chemistry
Auteurs
Membres identifiés du Cancéropôle Est :
Dr GARRIDO Carmen
,
Pr LIRUSSI Frédéric
Tous les auteurs :
Yuan YH, Mao ND, Duan JL, Zhang H, Garrido C, Lirussi F, Gao Y, Xie T, Ye XY
Lien Pubmed
Résumé
Adaptor associated kinase 1 (AAK1), a member of the Ark1/Prk1 family of Ser/Thr kinases, is a specific key kinase regulating Thr156 phosphorylation at the μ2 subunit of the adapter complex-2 (AP-2) protein. Due to their important biological functions, AAK1 systems have been validated in clinics for neuropathic pain therapy, and are being explored as potential therapeutic targets for diseases caused by various viruses such as Hepatitis C (HCV), Dengue, Ebola, and COVID-19 viruses and for amyotrophic lateral sclerosis (ALS). Centreing on the advances of drug discovery programs in this field up to 2023, AAK1 inhibitors are discussed from the aspects of the structure-based rational molecular design, pharmacology, toxicology and synthetic routes for the compounds of interest in this review. The aim is to provide the medicinal chemistry community with up-to-date information and to accelerate the drug discovery programs in the field of AAK1 small molecule inhibitors.
Mots clés
Adaptor associated kinase 1 (AAK1), inhibitor, medicinal chemistry, therapeutic application
Référence
J Enzyme Inhib Med Chem. 2023 12;38(1):2279906
