Timothy A. Subashi
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View article: Cryo-EM structures of the human glutamine transporter SLC1A5 (ASCT2) in the outward-facing conformation
Cryo-EM structures of the human glutamine transporter SLC1A5 (ASCT2) in the outward-facing conformation Open
Alanine-serine-cysteine transporter 2 (ASCT2, SLC1A5) is the primary transporter of glutamine in cancer cells and regulates the mTORC1 signaling pathway. The SLC1A5 function involves finely tuned orchestration of two domain movements that …
View article: Author response: Cryo-EM structures of the human glutamine transporter SLC1A5 (ASCT2) in the outward-facing conformation
Author response: Cryo-EM structures of the human glutamine transporter SLC1A5 (ASCT2) in the outward-facing conformation Open
Article Figures and data Abstract Introduction Results Discussion Materials and methods Data availability References Decision letter Author response Article and author information Metrics Abstract Alanine-serine-cysteine transporter 2 (ASC…
View article: Structural basis for the transport mechanism of the human glutamine transporter SLC1A5 (ASCT2)
Structural basis for the transport mechanism of the human glutamine transporter SLC1A5 (ASCT2) Open
Alanine-serine-cysteine transporter 2 (ASCT2, SLC1A5) is the primary transporter of glutamine in cancer cells and regulates the mTORC1 signaling pathway. The SLC1A5 function involves finely tuned orchestration of two domain movements that …
View article: Discovery of PF-06928215 as a high affinity inhibitor of cGAS enabled by a novel fluorescence polarization assay
Discovery of PF-06928215 as a high affinity inhibitor of cGAS enabled by a novel fluorescence polarization assay Open
Cyclic GMP-AMP synthase (cGAS) initiates the innate immune system in response to cytosolic dsDNA. After binding and activation from dsDNA, cGAS uses ATP and GTP to synthesize 2', 3' -cGAMP (cGAMP), a cyclic dinucleotide second messenger wi…
View article: Discovery of Fragment-Derived Small Molecules for in Vivo Inhibition of Ketohexokinase (KHK)
Discovery of Fragment-Derived Small Molecules for in Vivo Inhibition of Ketohexokinase (KHK) Open
Increased fructose consumption and its subsequent metabolism have been implicated in hepatic steatosis, dyslipidemia, obesity, and insulin resistance in humans. Since ketohexokinase (KHK) is the principal enzyme responsible for fructose me…
View article: Development of a high-throughput crystal structure-determination platform for JAK1 using a novel metal-chelator soaking system
Development of a high-throughput crystal structure-determination platform for JAK1 using a novel metal-chelator soaking system Open
Crystals of phosphorylated JAK1 kinase domain were initially generated in complex with nucleotide (ADP) and magnesium. The tightly bound Mg 2+ -ADP at the ATP-binding site proved recalcitrant to ligand displacement. Addition of a molar exc…
View article: Discovery of Selective Small Molecule Inhibitors of Monoacylglycerol Acyltransferase 3
Discovery of Selective Small Molecule Inhibitors of Monoacylglycerol Acyltransferase 3 Open
Inhibition of triacylglycerol (TAG) biosynthetic enzymes has been suggested as a promising strategy to treat insulin resistance, diabetes, dyslipidemia, and hepatic steatosis. Monoacylglycerol acyltransferase 3 (MGAT3) is an integral membr…