AI Article Synopsis
- AAK1 is a crucial kinase that controls the phosphorylation of a specific protein subunit (μ2) involved in important biological processes and is being researched for therapeutic applications in neuropathic pain and various viral diseases, including COVID-19.
- The text reviews recent advancements in drug discovery targeting AAK1 inhibitors, focusing on design, pharmacological properties, safety, and synthesis methods.
- The goal is to inform medicinal chemists and expedite the development of new small molecule inhibitors for clinical use.
Article Abstract
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.
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Source |
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10653628 | PMC |
| http://dx.doi.org/10.1080/14756366.2023.2279906 | DOI Listing |
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