Search Results - "Hoth, Lise R"
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Covalent Enzyme Inhibition through Fluorosulfate Modification of a Noncatalytic Serine Residue
Published in ACS chemical biology (18-08-2017)“…Irreversible enzyme inhibitors and covalent chemical biology probes often utilize the reaction of a protein cysteine residue with an appropriately positioned…”
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Probing the enzyme kinetics, allosteric modulation and activation of α1- and α2-subunit-containing AMP-activated protein kinase (AMPK) heterotrimeric complexes by pharmacological and physiological activators
Published in Biochemical journal (01-03-2016)“…AMP-activated protein kinase (AMPK) is a serine/threonine protein kinase that serves as a pleotropic regulator of whole body energy homoeostasis. AMPK exists…”
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3
Lysosomal integral membrane protein-2 as a phospholipid receptor revealed by biophysical and cellular studies
Published in Nature communications (04-12-2017)“…Lysosomal integral membrane protein-2 (LIMP-2/SCARB2) contributes to endosomal and lysosomal function. LIMP-2 deficiency is associated with neurological…”
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Crystal structure of human lysosomal acid lipase and its implications in cholesteryl ester storage disease[S]
Published in Journal of lipid research (01-08-2020)“…Lysosomal acid lipase (LAL) is a serine hydrolase that hydrolyzes cholesteryl ester (CE) and TGs delivered to the lysosomes into free cholesterol and fatty…”
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5
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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6
A potentiator of orthosteric ligand activity at GLP-1R acts via covalent modification
Published in Nature chemical biology (01-08-2014)“…BETP, a positive allosteric modulator of GLP-1R, a class B GPCR and an important therapeutic target for type II diabetes, covalently modifies two cysteine…”
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7
Activation of AMP-Activated Protein Kinase Revealed by Hydrogen/Deuterium Exchange Mass Spectrometry
Published in Structure (London) (05-11-2013)“…AMP-activated protein kinase (AMPK) monitors cellular energy, regulates genes involved in ATP synthesis and consumption, and is allosterically activated by…”
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Expression and functional characterization of human lysosomal acid lipase gene (LIPA) mutation responsible for cholesteryl ester storage disease (CESD) phenotype
Published in Protein expression and purification (01-06-2015)“…•Mutations in lysosomal acid lipase are associated with Wolman disease and CESD.•Patients homozygous for His295Tyr (H295Y) mutation have <5% of normal LAL…”
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Kinetic Analysis of Estrogen Receptor/Ligand Interactions
Published in Proceedings of the National Academy of Sciences - PNAS (25-06-2002)“…Surface plasmon resonance biosensor technology was used to directly measure the binding interactions of small molecules to the ligand-binding domain of human…”
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Introduction of a Crystalline, Shelf-Stable Reagent for the Synthesis of Sulfur(VI) Fluorides
Published in Organic letters (02-02-2018)“…The design, synthesis, and application of [4-(acetylamino)phenyl]imidodisulfuryl difluoride (AISF), a shelf-stable, crystalline reagent for the synthesis of…”
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Crystal structures of interleukin 17A and its complex with IL-17 receptor A
Published in Nature communications (2013)“…The constituent polypeptides of the interleukin-17 family form six different homodimeric cytokines (IL-17A–F) and the heterodimeric IL-17A/F. Their…”
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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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Binding site elucidation and structure guided design of macrocyclic IL-17A antagonists
Published in Scientific reports (16-08-2016)“…Interleukin-17A (IL-17A) is a principal driver of multiple inflammatory and immune disorders. Antibodies that neutralize IL-17A or its receptor (IL-17RA)…”
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14
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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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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Unexpected mucin-type O-glycosylation and host-specific N-glycosylation of human recombinant interleukin-17A expressed in a human kidney cell line
Published in Protein expression and purification (01-01-2013)“…► Human recombinant interleukin-17A expressed in HEK293 cells was variably glycosylated. ► Mass spectrometry was used to characterize its glycosylation. ► At…”
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Biophysical and Biochemical Approach to Locating an Inhibitor Binding Site on Cholesteryl Ester Transfer Protein
Published in Bioconjugate chemistry (01-08-2008)“…Cholesteryl ester transfer protein (CETP) transfers neutral lipids between different types of plasma lipoprotein. Inhibitors of CETP elevate the fraction of…”
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Binding to the Low-Density Lipoprotein Receptor Accelerates Futile Catalytic Cycling in PCSK9 and Raises the Equilibrium Level of Intramolecular Acylenzyme
Published in Biochemistry (Easton) (07-04-2009)“…Proprotein convertase subtilisin-kexin type 9 (PCSK9) binds to the low-density lipoprotein receptor (LDLR) on target cells and lowers the level of receptor by…”
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Cyclization of N-Terminal S-Carbamoylmethylcysteine Causing Loss of 17 Da from Peptides and Extra Peaks in Peptide Maps
Published in Journal of proteome research (01-03-2002)“…Enzymatic digests of proteins S-alkylated with iodoacetamide may contain peptides with N-terminal S-carbamoylmethylcysteine. These can be partly converted to a…”
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Synthesis and biological activity of selective pipecolic acid-based TNF-α converting enzyme (TACE) inhibitors
Published in Bioorganic & medicinal chemistry letters (20-05-2002)“…A series of novel, selective TNF-α converting enzyme inhibitors based on 4-hydroxy and 5-hydroxy pipecolate hydroxamic acid scaffolds is described. The potency…”
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