Seeking heterocyclic scaffolds as antivirals against dengue virus
Dengue is one of the most typical viral infection categorized in the Neglected Tropical
Diseases (NTDs). It is transmitted via the female Aedes aegypti mosquito to humans and …
Diseases (NTDs). It is transmitted via the female Aedes aegypti mosquito to humans and …
Structural properties and interaction partners of familial ALS-associated SOD1 mutants
J Huai, Z Zhang - Frontiers in neurology, 2019 - frontiersin.org
Amyotrophic lateral sclerosis (ALS) is the most common motor neuron degenerative disease
in adults and has also been proven to be a type of conformational disease associated with …
in adults and has also been proven to be a type of conformational disease associated with …
Family-wide structural analysis of human numb-associated protein kinases
The highly diverse Numb-associated kinase (NAK) family has been linked to broad cellular
functions including receptor-mediated endocytosis, Notch pathway modulation, osteoblast …
functions including receptor-mediated endocytosis, Notch pathway modulation, osteoblast …
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) …
regulating clathrin-mediated endocytosis, is ubiquitous in the central nervous system (CNS) …
WNT activates the AAK1 kinase to promote clathrin-mediated endocytosis of LRP6 and establish a negative feedback loop
MJ Agajanian, MP Walker, AD Axtman… - Cell reports, 2019 - cell.com
Summary β-Catenin-dependent WNT signal transduction governs development, tissue
homeostasis, and a vast array of human diseases. Signal propagation through a WNT …
homeostasis, and a vast array of human diseases. Signal propagation through a WNT …
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 …
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 …
a viable target for treating neuropathic pain. Potent small-molecule inhibitors of AAK1 have …
Depletion of endogenously biotinylated carboxylases enhances the sensitivity of TurboID-mediated proximity labeling in Caenorhabditis elegans
Proximity-dependent protein labeling provides a powerful in vivo strategy to characterize the
interactomes of specific proteins. We previously optimized a proximity labeling protocol for …
interactomes of specific proteins. We previously optimized a proximity labeling protocol for …
Chemical probes for understudied kinases: challenges and opportunities
RAM Serafim, JM Elkins, WJ Zuercher… - Journal of Medicinal …, 2021 - ACS Publications
Over 20 years after the approval of the first-in-class protein kinase inhibitor imatinib, the
biological function of a significant fraction of the human kinome remains poorly understood …
biological function of a significant fraction of the human kinome remains poorly understood …
Identification of pyrimidine-based lead compounds for understudied kinases implicated in driving neurodegeneration
The pyrimidine core has been utilized extensively to construct kinase inhibitors, including
eight FDA-approved drugs. Because the pyrimidine hinge-binding motif is accommodated …
eight FDA-approved drugs. Because the pyrimidine hinge-binding motif is accommodated …
SGC-AAK1-1: a chemical probe targeting AAK1 and BMP2K
Inhibitors based on a 3-acylaminoindazole scaffold were synthesized to yield potent dual
AAK1/BMP2K inhibitors. Optimization furnished a small molecule chemical probe (SGC …
AAK1/BMP2K inhibitors. Optimization furnished a small molecule chemical probe (SGC …