Search Results - "van Tilburg, Erica W."
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Boronic acid-based inhibitor of autotaxin reveals rapid turnover of LPA in the circulation
Published in Proceedings of the National Academy of Sciences - PNAS (20-04-2010)“…Autotaxin (ATX) is a secreted nucleotide pyrophosphatase/phosphodiesterase that functions as a lysophospholipase D to produce the lipid mediator…”
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Discovery and Optimization of Boronic Acid Based Inhibitors of Autotaxin
Published in Journal of medicinal chemistry (08-07-2010)“…Autotaxin (ATX) is an extracellular enzyme that hydrolyzes lysophosphatidylcholine (LPC) to produce the lipid mediator lysophosphatidic acid (LPA). The ATX−LPA…”
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Development of an Activity-Based Probe for Autotaxin
Published in Chembiochem : a European journal of chemical biology (02-11-2010)“…Autotaxin (ATX), or ecto‐nucleotide pyrophosphatase/phosphodiesterase 2 (ENPP2), is a secreted lysophospholipase D that hydrolyses lysophosphatidylcholine into…”
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Simplified parametric methods for [ 11C]PIB studies
Published in NeuroImage (Orlando, Fla.) (01-08-2008)“…The purpose of the present study was to evaluate the performance of various parametric reference tissue models for quantification of [ 11C]PIB studies. Several…”
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5‘-O-Alkyl Ethers of N,2-Substituted Adenosine Derivatives: Partial Agonists for the Adenosine A1 and A3 Receptors
Published in Journal of medicinal chemistry (30-08-2001)“…New N,5‘-di- and N,2,5‘-trisubstituted adenosine derivatives were synthesized in good overall yields. Appropriate 5-O-alkyl-substituted ribose moieties were…”
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Profiling Proteasome Activity in Tissue with Fluorescent Probes
Published in Molecular pharmaceutics (01-09-2007)“…With proteasome inhibitors in use in the clinic for the treatment of multiple myeloma and with clinical trials in progress investigating the treatment of a…”
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2,5‘-Disubstituted Adenosine Derivatives: Evaluation of Selectivity and Efficacy for the Adenosine A1, A2A, and A3 Receptor
Published in Journal of medicinal chemistry (17-01-2002)“…Novel 2,5‘-disubstituted adenosine derivatives were synthesized in good overall yields starting from commercially available guanosine. Binding affinities were…”
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2,8-Disubstituted adenosine derivatives as partial agonists for the adenosine A2A receptor
Published in Bioorganic & medicinal chemistry (15-05-2003)“…Novel 2,8-disubstituted adenosine derivatives were synthesized in good overall yields starting from 2-iodoadenosine. Binding affinities were determined for rat…”
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Extracellular adenosine-induced apoptosis in mouse neuroblastoma cells studies on involvement of adenosine receptors and adenosine uptake
Published in Biochemical pharmacology (15-02-2001)“…The induction of apoptosis by adenosine was studied in the mouse neuroblastoma cell line N1E-115. Apoptosis was characterized by fluorescence and electron…”
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One-pot synthesis of [11C]ureas via triphenylphosphinimines
Published in Journal of labelled compounds & radiopharmaceuticals (30-03-2006)“…A series of 11C‐labeled ureas was prepared using a rapid and efficient one‐pot procedure. First, the intermediate [11C]phenylisocyanate was formed with…”
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Functional role of adenosine receptor subtypes in the regulation of blood–brain barrier permeability: possible implications for the design of synthetic adenosine derivatives
Published in European journal of pharmaceutical sciences (01-05-2003)“…The objective of this investigation was to determine the functional role of adenosine receptor subtypes in the regulation of blood–brain barrier (BBB)…”
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Extracellular adenosine-induced apoptosis in mouse neuroblastoma cells studies on involvement of adenosine receptors and adenosine uptake11Abbreviations: NECA, 5′-(N-ethylcarboxamido)adenosine; AMDA, 5′-amino-5′-deoxyadenosine; CPA, N6-cyclopentyladenosine; NBI, nitrobenzylthioinosine; 2-Cl-IB-MECA, 2-chloro-N6-(3-iodobenzyl)adenosine-5′-N-methyluronamide; AMV–RT, Avian myeloblastosis virus–reverse transcriptase; PCR, polymerase chain reaction; DEVD-AMC, N-acetyl-Asp-Glu-Val-Asp-7-amino-4-methyl
Published in Biochemical pharmacology (01-02-2001)Get full text
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Cover Picture: Development of an Activity-Based Probe for Autotaxin (ChemBioChem 16/2010)
Published in Chembiochem : a European journal of chemical biology (02-11-2010)Get full text
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Why are A(2B) receptors low-affinity adenosine receptors? Mutation of Asn273 to Tyr increases affinity of human A(2B) receptor for 2-(1-Hexynyl)adenosine
Published in Molecular pharmacology (01-12-2000)“…Adenosine A(2B) receptors are known as low-affinity receptors due to their modest-to-negligible affinity for adenosine and prototypic agonists. Despite…”
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2,5'-Disubstituted adenosine derivatives: evaluation of selectivity and efficacy for the adenosine A(1), A(2A), and A(3) receptor
Published in Journal of medicinal chemistry (17-01-2002)“…Novel 2,5'-disubstituted adenosine derivatives were synthesized in good overall yields starting from commercially available guanosine. Binding affinities were…”
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2,5‘-Disubstituted Adenosine Derivatives: Evaluation of Selectivity and Efficacy for the Adenosine A 1 , A 2A , and A 3 Receptor
Published in Journal of medicinal chemistry (01-01-2002)Get full text
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2,8-Disubstituted adenosine derivatives as partial agonists for the adenosine A 2A receptor
Published in Bioorganic & medicinal chemistry (2003)“…Novel 2,8-disubstituted adenosine derivatives were synthesized in good overall yields starting from 2-iodoadenosine. Binding affinities were determined for rat…”
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18
5‘- O -Alkyl Ethers of N ,2-Substituted Adenosine Derivatives: Partial Agonists for the Adenosine A 1 and A 3 Receptors
Published in Journal of medicinal chemistry (01-08-2001)Get full text
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N 6 ,5‘-Disubstituted Adenosine Derivatives as Partial Agonists for the Human Adenosine A 3 Receptor
Published in Journal of medicinal chemistry (22-04-1999)Get full text
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N6,5‘-Disubstituted Adenosine Derivatives as Partial Agonists for the Human Adenosine A3 Receptor
Published in Journal of medicinal chemistry (22-04-1999)“…5'-(Alkylthio)-substituted analogues of N6-benzyl- and N6-(3-iodobenzyl)adenosine were synthesized in 37-61% overall yields. The affinities of these compounds…”
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