Development and therapeutic potential of adaptor-associated kinase 1 inhibitors in human multifaceted diseases

X Xin, Y Wang, L Zhang, D Zhang, L Sha, Z Zhu… - European Journal of …, 2023 - Elsevier
Abstract Adaptor-Associated Kinase 1 (AAK1), a Ser/Thr protein kinase, responsible for
regulating clathrin-mediated endocytosis, is ubiquitous in the central nervous system (CNS) …

Reductive catalytic difluorocarbene transfer via palladium catalysis

XY Zhang, SP Sun, YQ Sang, XS Xue… - Angewandte …, 2023 - Wiley Online Library
A palladium‐catalyzed reductive difluorocarbene transfer reaction that tames
difluorocarbene to couple with two electrophiles has been developed, representing a new …

Recent progress in discovery of novel AAK1 inhibitors: from pain therapy to potential anti-viral agents

YH Yuan, ND Mao, JL Duan, H Zhang… - Journal of Enzyme …, 2023 - Taylor & Francis
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 …

Asymmetric Phase-Transfer Alkylation of Readily Available Aryl Aldehyde Schiff Bases of Amino Acid Ethyl Esters

J Lu, L Huang, H Liang, Z Wang, T Kato, Y Liu… - Organic …, 2024 - ACS Publications
Asymmetric phase-transfer alkylation of the N-(arylmethylene)-α-alkylamino acid ethyl esters
and N-(arylmethylene) glycine ethyl esters was found to be catalyzed by the (R)-or (S) …

Discovery of (S)-1-((2′,6-Bis(difluoromethyl)-[2,4′-bipyridin]-5-yl)oxy)-2,4-dimethylpentan-2-amine (BMS-986176/LX-9211): A Highly Selective, CNS Penetrable …

G Luo, L Chen, WA Kostich, B Hamman… - Journal of Medicinal …, 2022 - ACS Publications
Recent mouse knockout studies identified adapter protein-2 associated kinase 1 (AAK1) as
a viable target for treating neuropathic pain. Potent small-molecule inhibitors of AAK1 have …

M2 microglia extracellular vesicle mir-124 regulates neural stem cell differentiation in ischemic stroke via aak1/notch

Y Song, R Shi, Y Liu, F Cui, L Han, C Wang, T Chen… - Stroke, 2023 - Am Heart Assoc
BACKGROUND: Small extracellular vesicles (sEVs) derived from M2 microglia (M2-
microglia–derived small extracellular vesicles [M2-sEVs]) contribute to central nervous …

Discovery and Characterization of Selective, First-in-Class Inhibitors of Citron Kinase

JJ Maw, JA Coker, T Arya, CM Goins… - Journal of Medicinal …, 2024 - ACS Publications
Citron kinase (CITK) is an AGC-family serine/threonine kinase that regulates cytokinesis.
Despite knockdown experiments implicating CITK as an anticancer target, no selective CITK …

Carrier-Mediated Delivery of Low-Molecular-Weight N-Containing Drugs across the Blood–Brain Barrier or the Blood–Retinal Barrier Using the Proton-Coupled …

T Tashima - Future Pharmacology, 2023 - mdpi.com
While it is true that pharmacotherapy has achieved desired health outcomes, significant
unmet medical needs persist in the field of central nervous system (CNS) drugs, particularly …

Discovery of 4-(1, 2, 4-Oxadiazol-5-yl) azepan-2-one Derivatives as a New Class of Cannabinoid Type 2 Receptor Agonists for the Treatment of Inflammatory Pain

J Nan, J Liu, G Lin, S Zhang, A Xia, P Zhou… - Journal of Medicinal …, 2023 - ACS Publications
Selectively targeting the cannabinoid receptor CB2 is an attractive therapeutic strategy for
the treatment of inflammatory pain without psychiatric side effects mediated by the …

Development of a novel AAK1 inhibitor via Kinobeads-based screening

A Yoshida, S Ohtsuka, F Matsumoto, T Miyagawa… - Scientific reports, 2024 - nature.com
A chemical proteomics approach using Ca2+/calmodulin-dependent protein kinase kinase
(CaMKK) inhibitor–immobilized sepharose (TIM-063-Kinobeads) identified main targets …