Search Results - "McLean, Larry R."
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Selective Inhibition of Mutant Isocitrate Dehydrogenase 1 (IDH1) via Disruption of a Metal Binding Network by an Allosteric Small Molecule
Published in The Journal of biological chemistry (09-01-2015)“…Cancer-associated point mutations in isocitrate dehydrogenase 1 and 2 (IDH1 and IDH2) confer a neomorphic enzymatic activity: the reduction of α-ketoglutarate…”
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Spectroscopic Methods for Analysis of Protein Secondary Structure
Published in Analytical Biochemistry (15-01-2000)“…Several methods for determination of the secondary structure of proteins by spectroscopic measurements are reviewed. Circular dichroism (CD) spectroscopy…”
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Book Review Journal Article -
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Amelioration of PXR-mediated CYP3A4 induction by mGluR2 modulators
Published in Bioorganic & medicinal chemistry letters (15-10-2018)“…[Display omitted] •CYP3A4 induction data lead to PXR activation data for mGluR2 allosteric activators.•One of the compounds was also crystallized with PXR &…”
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X-ray crystallographic structure-based design of selective thienopyrazole inhibitors for interleukin-2-inducible tyrosine kinase
Published in Bioorganic & medicinal chemistry letters (01-05-2012)“…Beginning with a screening hit, unique thienopyrazole-indole inhibitors of Itk (interleukin-2-inducible tyrosine kinase) were designed, synthesized, and…”
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Protein disulfide isomerase appears necessary to maintain the catalytically active structure of the microsomal triglyceride transfer protein
Published in Biochemistry (Easton) (08-10-1991)“…Protein disulfide isomerase (PDI) is a component of the microsomal triglyceride transfer protein (MTP) complex. This study was initiated to help elucidate the…”
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Discovery of covalent inhibitors for MIF tautomerase via cocrystal structures with phantom hits from virtual screening
Published in Bioorganic & medicinal chemistry letters (01-12-2009)“…Virtual screen hits were shown to be covalent inhibitors by biochemical and X-ray crystallographic studies. Biochemical and X-ray crystallographic studies…”
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Fragment screening of inhibitors for MIF tautomerase reveals a cryptic surface binding site
Published in Bioorganic & medicinal chemistry letters (15-03-2010)“…Fragment screening by in silico docking followed by X-ray crystallography demonstrates the formation of a previously unreported surface binding site in MIF…”
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Influence of molecular packing and phospholipid type on rates of cholesterol exchange
Published in Biochemistry (Easton) (03-05-1988)“…The rates of [14C]cholesterol transfer from small unilamellar vesicles containing cholesterol dissolved in bilayers of different phospholipids have been…”
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Discovery of novel inhibitors for DHODH via virtual screening and X-ray crystallographic structures
Published in Bioorganic & medicinal chemistry letters (15-03-2010)“…Several amino-benzoic acid derivatives were found to be DHODH inhibitors through virtual screening, biochemical, and X-ray crystallographic studies…”
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Virtual Screening and X-ray Crystallography for Human Kallikrein 6 Inhibitors with an Amidinothiophene P1 Group
Published in ACS medicinal chemistry letters (09-02-2012)“…A series of compounds with an amidinothiophene P1 group and a pyrrolidinone-sulphonamide scaffold linker was identified as potent inhibitors of human…”
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Structural properties of the microsomal triglyceride-transfer protein complex
Published in Biochemistry (Easton) (07-05-1991)“…The microsomal triglyceride-transfer protein (MTP), which catalyzes the transport of triglyceride and cholesteryl ester between membranes, is a complex…”
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Effect of probucol on the physical properties of low-density lipoproteins oxidized by copper
Published in Biochemistry (Easton) (10-01-1989)“…Human plasma low-density lipoproteins (LDL) were incubated with 10 microM probucol for 1 h at 37 degrees C. Probucol incorporation into the LDL was complete as…”
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Kinetics of phosphatidylcholine and lysophosphatidylcholine exchange between unilamellar vesicles
Published in Biochemistry (Easton) (25-09-1984)“…The rates of exchange of phosphatidylcholine and lysophosphatidylcholine from unilamellar donor vesicles to acceptor vesicles of similar composition were…”
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Ascorbate and phenolic antioxidant interactions in prevention of liposomal oxidation
Published in Lipids (01-07-1992)“…Efficient prevention of membrane lipid peroxidation by vitamin E (α‐tocopherol) may involve its regeneration by vitamin C (ascorbate). Conceivably, the…”
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Minimal peptide length for interaction of amphipathic .alpha.-helical peptides with phosphatidylcholine liposomes
Published in Biochemistry (Easton) (01-01-1991)“…The interactions of a series of amphipathic alpha-helical peptides containing from 6 to 18 amino acid residues with dipalmitoylphosphatidylcholine (DPPC) and…”
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Identification of a Model Cardiac Glycoside Receptor: Comparisons with Na+,K+-ATPase
Published in Biochemistry (Easton) (12-05-1998)“…The availability of high-affinity anti-digoxin monoclonal antibodies (mAbs) offers the potential for their use as models for the characterization of the…”
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Examination of the role of the amphipathic .alpha.-helix in the interaction of neuropeptide Y and active cyclic analogs with cell membrane receptors and dimyristoylphosphatidylcholine
Published in Biochemistry (Easton) (27-02-1990)“…To test the potential importance of the putative C-terminal amphipathic alpha-helical region of neuropeptide Y (NPY) in receptor binding, the interactions of…”
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Micelle-bound conformations of a bombesin/gastrin releasing peptide receptor agonist and an antagonist by two-dimensional NMR and restrained molecular dynamics
Published in Biochemistry (Easton) (11-08-1992)“…Two nonapeptide analogs of the carboxyl termini of bombesin (Bn) and gastrin releasing peptide (GRP) have been synthesized. Despite the small difference in…”
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Heparin prevents the binding of phospholipase A2 to phospholipid micelles: importance of the amino-terminus
Published in Biochemistry (Easton) (01-09-1991)“…The activity of the major isoform of porcine pancreatic phospholipase A2 (PLA2), designated B-PLA2, against micellar substrates is inhibited by heparin…”
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