Search Results - "Subashi, Timothy A."
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Structural Basis for AMPK Activation: Natural and Synthetic Ligands Regulate Kinase Activity from Opposite Poles by Different Molecular Mechanisms
Published in Structure (London) (05-08-2014)“…AMP-activated protein kinase (AMPK) is a principal metabolic regulator affecting growth and response to cellular stress. Comprised of catalytic and regulatory…”
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Cryo-EM structures of the human glutamine transporter SLC1A5 (ASCT2) in the outward-facing conformation
Published in eLife (03-10-2019)“…Alanine-serine-cysteine transporter 2 (ASCT2, SLC1A5) is the primary transporter of glutamine in cancer cells and regulates the mTORC1 signaling pathway. The…”
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Structural and biophysical studies of PCSK9 and its mutants linked to familial hypercholesterolemia
Published in Nature structural & molecular biology (01-05-2007)“…Proprotein convertase subtilisin kexin type 9 (PCSK9) lowers the abundance of surface low-density lipoprotein (LDL) receptor through an undefined mechanism…”
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Glycomimetic Ligands for the Human Asialoglycoprotein Receptor
Published in Journal of the American Chemical Society (01-02-2012)“…The asialoglycoprotein receptor (ASGPR) is a high-capacity galactose-binding receptor expressed on hepatocytes that binds its native substrates with low…”
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Pharmacologic inhibition of site 1 protease activity inhibits sterol regulatory element-binding protein processing and reduces lipogenic enzyme gene expression and lipid synthesis in cultured cells and experimental animals
Published in The Journal of pharmacology and experimental therapeutics (01-09-2008)“…Sterol regulatory element-binding proteins (SREBPs) are major transcriptional regulators of cholesterol, fatty acid, and glucose metabolism. Genetic disruption…”
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Assessment of cholesteryl ester transfer protein inhibitors for interaction with proteins involved in the immune response to infection[S]
Published in Journal of lipid research (01-05-2010)“…The CETP inhibitor, torcetrapib, was prematurely terminated from phase 3 clinical trials due to an increase in cardiovascular and noncardiovascular mortality…”
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Crystal structure of cholesteryl ester transfer protein reveals a long tunnel and four bound lipid molecules
Published in Nature structural & molecular biology (01-02-2007)“…Cholesteryl ester transfer protein (CETP) shuttles various lipids between lipoproteins, resulting in the net transfer of cholesteryl esters from…”
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Discovery of Selective Small Molecule Inhibitors of Monoacylglycerol Acyltransferase 3
Published in Journal of medicinal chemistry (24-09-2015)“…Inhibition of triacylglycerol (TAG) biosynthetic enzymes has been suggested as a promising strategy to treat insulin resistance, diabetes, dyslipidemia, and…”
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Novel 3-O-carbamoyl erythromycin A derivatives (carbamolides) with activity against resistant staphylococcal and streptococcal isolates
Published in Bioorganic & medicinal chemistry letters (15-03-2013)“…A novel series of 3-O-carbamoyl erythromycin A derived analogs, labeled carbamolides, with activity versus resistant bacterial isolates of staphylococci…”
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Development of a high-throughput crystal structure-determination platform for JAK1 using a novel metal-chelator soaking system
Published in Acta crystallographica. Section F, Structural biology communications (01-11-2016)“…Crystals of phosphorylated JAK1 kinase domain were initially generated in complex with nucleotide (ADP) and magnesium. The tightly bound Mg2+‐ADP at the…”
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A systematic study of 50S ribosomal subunit purification enabling robust crystallization
Published in Acta crystallographica. Section D, Biological crystallography. (01-12-2009)“…A systematic analysis was undertaken to seek correlations between the integrity, purity and activity of 50S ribosomal subunit preparations from Deinococcus…”
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Purification of the large ribosomal subunit via its association with the small subunit
Published in Analytical biochemistry (01-12-2009)“…We have developed an affinity purification of the large ribosomal subunit from Deinococcus radiodurans that exploits its association with FLAG-tagged 30S…”
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CP-225,917 and CP-263,114, novel Ras farnesylation inhibitors from an unidentified fungus. I. Taxonomy, fermentation, isolation, and biochemical properties
Published in Journal of antibiotics (1997)“…During the course of our screening for squalene synthase inhibitors and Ras farnesylation inhibitors, a novel fungal culture was discovered to produce two…”
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Discovery of Fragment-Derived Small Molecules for in Vivo Inhibition of Ketohexokinase (KHK)
Published in Journal of medicinal chemistry (28-09-2017)“…Increased fructose consumption and its subsequent metabolism have been implicated in hepatic steatosis, dyslipidemia, obesity, and insulin resistance in…”
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