- UHRA Home
- Browsing by Author
Browsing by Author "Berkhout, Theo"
Now showing items 1-20 of 33
-
Analysis of histones from the yeast Saccharomyces carlsbergensis
Pastink, A.; Berkhout, Theo; Mager, W.H.; Planta, R.J. (1979-02)Basic chromosomal proteins were isolated from the chromatin of the yeast Saccharomyces carlsbergensis by extraction with H2SO4 and were purified by ion-exchange chromatography. Electrophoresis of the purified fraction on ... -
CCR2: Characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach
Berkhout, Theo; Blaney, F.E.; Bridges, A.M.; Cooper, D.G.; Forbes, I.T.; Gribble, A.D.; Groot, P.H.E.; Hardy, A.; Ife, R.J.; Kaur, R.; Moores, K.E.; Shillito, H.; Willetts, J.; Witherington, J. (2003-09-11)We describe here a classical molecular modeling exercise that was carried out to provide a basis for the design of novel antagonist ligands of the CCR2 receptor. Using a theoretical model of the CCR2 receptor, docking ... -
CCR2B receptor antagonists : Conversion of a weak HTS hit to a potent lead compound
Forbes, Ian T.; Cooper, David G.; Dodds, Emma K.; Hickey, Deirdre M. B.; Ife, Robert J.; Meeson, Malcolm; Stockley, Martin; Berkhout, Theo; Gohil, Jayneeta; Groot, Pieter H. E.; Moores, Kitty E. (2000-08-21)A weak HTS hit at the CCR2B receptor has been converted into a potent antagonist by array SAR studies. Selectivity over the closely related CCR5 receptor is also achieved. (C) 2000 Elsevier Science Ltd. All rights reserved. -
Cloning, in vitro expression, and functional characterization of a novel human CC chemokine of the monocyte chemotactic protein (MCP) family (MCP-4) that binds and signals through the CC chemokine receptor 2B
Berkhout, Theo; Sarau, Henry M.; Moores, Kitty E.; White, John R.; Elshourbagy, Nabil; Appelbaum, Edward; Reape, Theresa J.; Brawner, Mary; Makwana, Jayneeta; Foley, James J.; Schmidt, Dulcie B.; Imburgia, Christine; McNulty, Dean; Matthews, Jane; O'Donnell, Kevin; O'Shannessy, Daniel; Scott, Miller; Groot, Pieter H E; Macphee, Colin H. (1997-06-27)Here we describe the characterization of a novel human CC chemokine, tentatively named monocyte chemotactic protein (MCP-4). This chemokine was detected by random sequencing of expressed sequence tags in cDNA libraries. ... -
Conformationally restricted indolopiperidine derivatives as potent CCR2B receptor antagonists
Witherington, Jason; Bordas, Vincent; Cooper, Dave G.; Forbes, Ian T.; Gribble, Andrew D.; Ife, Robert J.; Berkhout, Theo; Gohil, Jayneeta; Groot, Pieter H. E. (2001-08-20)The preparation and biological evaluation of a series of indolopiperidine CCR2B receptor antagonists possessing a conformationally restricted C-5 linker chain in combination with a restricted piperidine ring are described. ... -
Coupling of photoactivatable glycolipid probes to apolipoproteins A-I and A-II in human high density lipoproteins 2 and 3
Berkhout, Theo; Groot, P. H.; van Belzen, R.; Wirtz, K. W. (1985-08)High density lipoprotein (HDL) from human serum was subfractionated into HDL2 and HDL3 by rate-zonal density gradient ultracentrifugation. The orientation of apoproteins (apo) A-I and A-II in these subfractions was ... -
The disintegrin-like metalloproteinase ADAM 10 is involved in coinstitutive cleavage of CX3CL1 (fractalkine) and regulates CX3CL1-mediated cell-cell adhesion
Hundhausen, C.; Misztela, D.; Berkhout, Theo; Broadway, N.; Saftig, P.; Reiss, K.; Hartmann, D.; Fahrenholz, F.; Postina, R.; Matthews, J.; Kallen, K.J.; Rose-John, S.; Ludwig, A. (2003-08-15)The CX3C chemokine fractalkine (CX3CL1) exists as a membrane-expressed protein promoting cell-cell adhesion and as a soluble molecule inducing chemotaxis. Transmembrane CX3CL1 is converted into its soluble form by defined ... -
The effect of (-)-hydroxycitrate and mevinolin on the activity of the low-density lipoprotein receptor and 3-hydroxy-3-methylglutaryl-coenzyme A reductase in the human hepatoma Hep G2
Berkhout, Theo; Groot, P.H.E.; Havekes, Louis M.; Pearce, N. J. (W. Zuckwerdt Verlag, 1992) -
The effect of (-)-hydroxycitrate on the activity of the low-density-lipoprotein receptor and 3-hydroxy-3-methylglutaryl-CoA reductase levels in the human hepatoma cell line Hep G2
Berkhout, Theo; Havekes, Louis M.; Pearce, N. J.; Groot, P.H.E. (1990)(-)-Hydroxycitrate, a potent inhibitor of ATP citrate-lyase, was tested in Hep G2 cells for effects on cholesterol homoeostasis. After 2.5 h and 18 h incubations with (-)-hydroxycitrate at concentrations of 0.5 mM or higher, ... -
Effects of a novel lanosterol 14α-demethylase inhibitor on the regulation of 3-hydroxy-3-methylglutaryl-coenzyme A reductase in Hep G2 cells
Mayer, R. J.; Adams, J. L.; Bossard, M. J.; Berkhout, Theo (1991-12-10)A 32-carboxylic acid derivative of lanosterol (SKF 104976) was found to be a potent inhibitor of lanosterol 14α-demethylase (14αDM). 14αDM activity in a Hep G2 cell extract was inhibited 50% by 2 nM SKF 104976. Exposure ... -
Fractalkine cleavage from neuronal membranes represents an acute event in the inflammatory response to excitotoxic brain damage
Chapman, G. A.; Moores, K. E.; Harrison, D.; Campbell, C. A.; Stewart, B. R.; Strijbos, P. J.; Berkhout, Theo (2000-08-01)Fractalkine is a recently identified chemokine that exhibits cell adhesion and chemoattractive properties. It represents a unique member of the chemokine superfamily because it is located predominantly in the brain in which ... -
Fractalkine is expressed by smooth muscle cells in response to IFN-gamma and TNF-alpha and is modulated by metalloproteinase activity
Ludwig, A.; Berkhout, Theo; Moores, K.; Groot, P.; Chapman, G. (2002-01-15)Fractalkine/CX3C-chemokine ligand 1 is expressed as a membrane-spanning adhesion molecule that can be cleaved from the cell surface to produce a soluble chemoattractant. Within the vasculature, fractalkine is known to be ... -
HBMBU-14 is a receptor for the chemokine PF4
School of Life and Medical Sciences; Department of Pharmacy; Health & Human Sciences Research Institute; Medicinal and Analytical Chemistry; Berkhout, Theo; Moores, Kitty E.; MacPhee, Colin H. (1999)The ligand PF-4 has been identified as a ligand for the 7TM receptor HBMBU14, also known as TYMSTR, STRL-33 and BONZO. -
Identification of a truncated form of the CC chemokine CKβ-8 demonstrating greatly enhanced biological activity
MacPhee, Colin H.; Appelbaum, Edward R.; Johanson, Kyung; Moores, Kitty E.; Imburgia, Christina S.; Fornwald, Jim; Berkhout, Theo; Brawner, Mary; Groot, Pieter H. E.; O'Donnell, Kevin; O'Shannessy, Daniel; Scott, Gil; White, John R. (1998-12-01)A new CC chemokine, designated CKβ-8 or myeloid progenitor inhibitor factor-1, was recently identified in a large scale sequencing effort and was cloned from a human aortic endothelial library. CKβ-8 cDNA encodes a signal ... -
Identification of membrane proteins of human blood platelets with a hydrophobic photolabel
Berkhout, Theo; Schiphorst, M. E.; Wirtz, K. W.; Sixma, J. J. (1984-12-05)A photoactivable glycolipid probe, 12-(4-azido-2-nitrophenoxy)stearoyl[1-14C]glucosamine, was used to label proteins and lipids of platelet membranes. The proteins were analyzed by two-dimensional high-resolution ... -
Identification of the lipid-binding site of phosphatidylcholine-transfer protein with phosphatidylcholine analogs containing photoactivable carbene precursors
Westerman, J.; Wirtz, K.W.A.; Berkhout, Theo; Vandeenen, L.L.M.; Radhakrishnan, R.; Khorana, H.G. (1983)The lipid binding site of the phosphatidylcholine transfer protein from bovine liver has been investigated by use of phosphatidylcholine analogs which carry a diazirinophenoxy group linked to the ω-carbon of either the ... -
Induction of cytochrome P4503A by the antiglucocorticoid mifepristone and a novel hypocholesterolaemic drug
Williams, J. Andrew; Chenery, Richard J.; Berkhout, Theo; Hawksworth, Gabrielle M. (1997-06-01)Rat liver microsomal testosterone (250μM) hydroxylation and immunoreactive CYP3A protein were compared after administration of the antiglucocorticoid RU 486 (50 mg-kg-1 · day-1 for 4 days) and the hypocholesterolaemic drug ... -
Labeling of phospholipids in vesicles and human-erythrocytes by photoactivable fatty-acid derivatives
Berkhout, Theo; Vanamerongen, A.; Wirtz, K.W.A. (1984-07)The photoactivable glycolipid probes, 2-(4-azido-2-nitrophenoxy)palmitoyl[1-I4C]glucosamine (compound A) and 12-(4-azido-2-nitrophenoxy)stearoyl[1-14C]glucosamine (compound B) were synthesized essentially as described ... -
The lipid binding site of the phosphatidylcholine transfer protein from bovine liver
van Loon, D.; Berkhout, Theo; Demel, R. A.; Wirtz, K. W. A. (1985-08-30)The phosphatidylcholine transfer protein (PC-TP) from bovine liver has a binding site for phosphatidylcholine (PC). Structural and molecular characteristics of this site were investigated by binding PC-analogues carrying ...