Yasutomi Asano
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View article: Gram-scale preparation of the antibiotic lead compound salicyl-AMS, a potent inhibitor of bacterial salicylate adenylation enzymes
Gram-scale preparation of the antibiotic lead compound salicyl-AMS, a potent inhibitor of bacterial salicylate adenylation enzymes Open
View article: Identification of Novel, Potent, and Orally Available GCN2 Inhibitors with Type I Half Binding Mode
Identification of Novel, Potent, and Orally Available GCN2 Inhibitors with Type I Half Binding Mode Open
General control nonderepressible 2 (GCN2) is a master regulator kinase of amino acid homeostasis and important for cancer survival in the tumor microenvironment under amino acid depletion. We initiated studies aiming at the discovery of no…
View article: Development of human cGAS-specific small-molecule inhibitors for repression of dsDNA-triggered interferon expression
Development of human cGAS-specific small-molecule inhibitors for repression of dsDNA-triggered interferon expression Open
Cyclic GMP-AMP synthase (cGAS) is the primary sensor for aberrant intracellular dsDNA producing the cyclic dinucleotide cGAMP, a second messenger initiating cytokine production in subsets of myeloid lineage cell types. Therefore, inhibitio…
View article: Discovery of novel serine palmitoyltransferase inhibitors as cancer therapeutic agents
Discovery of novel serine palmitoyltransferase inhibitors as cancer therapeutic agents Open
View article: CCDC 1511207: Experimental Crystal Structure Determination
CCDC 1511207: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 1511402: Experimental Crystal Structure Determination
CCDC 1511402: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Publisher Correction: Small molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice
Publisher Correction: Small molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice Open
View article: Small molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice
Small molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice Open
View article: Discovery of an Orally Bioavailable, Brain-Penetrating, in Vivo Active Phosphodiesterase 2A Inhibitor Lead Series for the Treatment of Cognitive Disorders
Discovery of an Orally Bioavailable, Brain-Penetrating, in Vivo Active Phosphodiesterase 2A Inhibitor Lead Series for the Treatment of Cognitive Disorders Open
Herein, we describe the discovery of a potent, selective, brain-penetrating, in vivo active phosphodiesterase (PDE) 2A inhibitor lead series. To identify high-quality leads suitable for optimization and enable validation of the physiologic…