Institute of Pharmacy
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Polyamine levels of human colorectal adenocarcinomas are correlated with tumor stage and grade.
International journal of colorectal disease Nov, 2002 | Pubmed ID: 12355213
Transport of paclitaxel (Taxol) across the blood-brain barrier in vitro and in vivo.
The Journal of clinical investigation Nov, 2002 | Pubmed ID: 12417570
Functional expression of the interleukin-11 receptor alpha-chain and evidence of antiapoptotic effects in human colonic epithelial cells.
The Journal of biological chemistry Mar, 2004 | Pubmed ID: 14701802
L-Ascorbic acid 6-hexadecanoate, a potent hyaluronidase inhibitor. X-ray structure and molecular modeling of enzyme-inhibitor complexes.
The Journal of biological chemistry Oct, 2004 | Pubmed ID: 15322107
Structure-activity relationships of histamine H2 receptor ligands.
Mini reviews in medicinal chemistry Nov, 2004 | Pubmed ID: 15544555
Construction and validation of a microprocessor controlled extracorporal circuit in rats for the optimization of isolated limb perfusion.
Archiv der Pharmazie Dec, 2004 | Pubmed ID: 15597400
Sulphated oligosaccharides as inhibitors of hyaluronidases from bovine testis, bee venom and Streptococcus agalactiae.
Planta medica Aug, 2005 | Pubmed ID: 16142636
Design of new benzoxazole-2-thione-derived inhibitors of Streptococcus pneumoniae hyaluronan lyase: structure of a complex with a 2-phenylindole.
Glycobiology Aug, 2006 | Pubmed ID: 16638841
Inhibitors of kinesin Eg5: antiproliferative activity of monastrol analogues against human glioblastoma cells.
Cancer chemotherapy and pharmacology Feb, 2007 | Pubmed ID: 16703323
Platelet-derived growth factor receptor independent proliferation of human glioblastoma cells: selective tyrosine kinase inhibitors lack antiproliferative activity.
Journal of cancer research and clinical oncology Sep, 2006 | Pubmed ID: 16736141
A simple and powerful flow cytometric method for the simultaneous determination of multiple parameters at G protein-coupled receptor subtypes.
Chembiochem : a European journal of chemical biology Sep, 2006 | Pubmed ID: 16888730
Novel 6-O-acylated vitamin C derivatives as hyaluronidase inhibitors with selectivity for bacterial lyases.
Bioorganic & medicinal chemistry letters Oct, 2006 | Pubmed ID: 16908142
Fluorescence- and luminescence-based methods for the determination of affinity and activity of neuropeptide Y2 receptor ligands.
European journal of pharmacology Dec, 2006 | Pubmed ID: 17027743
Constitutive activity and ligand selectivity of human, guinea pig, rat, and canine histamine H2 receptors.
The Journal of pharmacology and experimental therapeutics Jun, 2007 | Pubmed ID: 17332265
Mutations of Cys-17 and Ala-271 in the human histamine H2 receptor determine the species selectivity of guanidine-type agonists and increase constitutive activity.
The Journal of pharmacology and experimental therapeutics Jun, 2007 | Pubmed ID: 17347323
Isoenzyme-specific differences in the degradation of hyaluronic acid by mammalian-type hyaluronidases.
Glycoconjugate journal Feb, 2008 | Pubmed ID: 17620008
Effect of the ABCB1 modulators elacridar and tariquidar on the distribution of paclitaxel in nude mice.
Journal of cancer research and clinical oncology May, 2008 | Pubmed ID: 17932689
Frontiers in medicinal chemistry in Regensburg.
ChemMedChem Aug, 2008 | Pubmed ID: 18655207
Acylguanidines as bioisosteres of guanidines: NG-acylated imidazolylpropylguanidines, a new class of histamine H2 receptor agonists.
Journal of medicinal chemistry Nov, 2008 | Pubmed ID: 18950149
Guanidine-acylguanidine bioisosteric approach in the design of radioligands: synthesis of a tritium-labeled N(G)-propionylargininamide ([3H]-UR-MK114) as a highly potent and selective neuropeptide Y Y1 receptor antagonist.
Journal of medicinal chemistry Dec, 2008 | Pubmed ID: 19053784
Potent and selective inhibitors of breast cancer resistance protein (ABCG2) derived from the p-glycoprotein (ABCB1) modulator tariquidar.
Journal of medicinal chemistry Feb, 2009 | Pubmed ID: 19170519
N(G)-acylated imidazolylpropylguanidines as potent histamine H4 receptor agonists: selectivity by variation of the N(G)-substituent.
Journal of medicinal chemistry Apr, 2009 | Pubmed ID: 19317445
Synthesis and structure-activity relationships of cyanoguanidine-type and structurally related histamine H4 receptor agonists.
Journal of medicinal chemistry Oct, 2009 | Pubmed ID: 19791743
Chiral NG-acylated hetarylpropylguanidine-type histamine H2 receptor agonists do not show significant stereoselectivity.
Bioorganic & medicinal chemistry letters May, 2010 | Pubmed ID: 20409707
G protein-coupled receptors function as logic gates for nanoparticle binding and cell uptake.
Proceedings of the National Academy of Sciences of the United States of America Jun, 2010 | Pubmed ID: 20498042
Histamine H4 receptor agonists.
Bioorganic & medicinal chemistry letters Dec, 2010 | Pubmed ID: 21044842
Expression and functional properties of canine, rat, and murine histamine H₄ receptors in Sf9 insect cells.
Naunyn-Schmiedeberg's archives of pharmacology May, 2011 | Pubmed ID: 21359967
Functional reconstitution of human neuropeptide Y (NPY) Y(2) and Y(4) receptors in Sf9 insect cells.
Journal of receptor and signal transduction research Aug, 2011 | Pubmed ID: 21745157
Role of the second and third extracellular loops of the histamine H(4) receptor in receptor activation.
Naunyn-Schmiedeberg's archives of pharmacology Sep, 2011 | Pubmed ID: 21800093
Fast counter-electroosmotic capillary electrophoresis-time-of-flight mass spectrometry of hyaluronan oligosaccharides.
Analytical and bioanalytical chemistry Mar, 2012 | Pubmed ID: 21800126
Design of benzimidazole- and benzoxazole-2-thione derivatives as inhibitors of bacterial hyaluronan lyase.
European journal of medicinal chemistry Sep, 2011 | Pubmed ID: 21803461
Synthesis and histamine H(3) and H(4) receptor activity of conformationally restricted cyanoguanidines related to UR-PI376.
Archiv der Pharmazie Dec, 2011 | Pubmed ID: 21987304
The bivalent ligand approach leads to highly potent and selective acylguanidine-type histamine H₂ receptor agonists.
Journal of medicinal chemistry Feb, 2012 | Pubmed ID: 22216892
Species-dependent activities of G-protein-coupled receptor ligands: lessons from histamine receptor orthologs.
Trends in pharmacological sciences Jan, 2013 | Pubmed ID: 23228711
The neuropeptide y y(1) receptor: a diagnostic marker? Expression in mcf-7 breast cancer cells is down-regulated by antiestrogens in vitro and in xenografts.
PloS one , 2012 | Pubmed ID: 23236424
Molecular and cellular analysis of human histamine receptor subtypes.
Trends in pharmacological sciences Jan, 2013 | Pubmed ID: 23254267
Dissociations in the effects of β2-adrenergic receptor agonists on cAMP formation and superoxide production in human neutrophils: support for the concept of functional selectivity.
PloS one , 2013 | Pubmed ID: 23741338
Luciferase reporter gene assay on human, murine and rat histamine H4 receptor orthologs: correlations and discrepancies between distal and proximal readouts.
PloS one , 2013 | Pubmed ID: 24023919
Dimeric argininamide-type neuropeptide Y receptor antagonists: chiral discrimination between Y1 and Y4 receptors.
Bioorganic & medicinal chemistry Nov, 2013 | Pubmed ID: 24074877
Replacement of Thr32 and Gln34 in the C-terminal neuropeptide Y fragment 25-36 by cis-cyclobutane and cis-cyclopentane β-amino acids shifts selectivity toward the Y(4) receptor.
Journal of medicinal chemistry Nov, 2013 | Pubmed ID: 24090364
Synthesis and dual histamine H₁ and H₂ receptor antagonist activity of cyanoguanidine derivatives.
Molecules (Basel, Switzerland) Nov, 2013 | Pubmed ID: 24248146
Synthesis and functional characterization of imbutamine analogs as histamine H3 and H4 receptor ligands.
Archiv der Pharmazie Feb, 2014 | Pubmed ID: 24493592
Benzanilide-Biphenyl Replacement: A Bioisosteric Approach to Quinoline Carboxamide-Type ABCG2 Modulators.
ACS medicinal chemistry letters Apr, 2013 | Pubmed ID: 24900683
No evidence for histamine H4 receptor in human monocytes.
The Journal of pharmacology and experimental therapeutics Dec, 2014 | Pubmed ID: 25273276
The extracellular loop 2 (ECL2) of the human histamine H4 receptor substantially contributes to ligand binding and constitutive activity.
PloS one , 2015 | Pubmed ID: 25629160
Dimeric carbamoylguanidine-type histamine H2 receptor ligands: A new class of potent and selective agonists.
Bioorganic & medicinal chemistry Jul, 2015 | Pubmed ID: 25639885
M2 Subtype preferring dibenzodiazepinone-type muscarinic receptor ligands: Effect of chemical homo-dimerization on orthosteric (and allosteric?) binding.
Bioorganic & medicinal chemistry Jul, 2015 | Pubmed ID: 25650309
High performance anion exchange chromatography with pulsed amperometric detection (HPAEC-PAD) for the sensitive determination of hyaluronan oligosaccharides.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences Apr, 2015 | Pubmed ID: 25768984
Toward Labeled Argininamide-Type NPY Y1 Receptor Antagonists: Identification of a Favorable Propionylation Site in BIBO3304.
Archiv der Pharmazie Jun, 2015 | Pubmed ID: 25884646
Topotecan-induced ABCG2 expression in MCF-7 cells is associated with decreased CD24 and EpCAM expression and a loss of tumorigenicity.
Cytometry. Part A : the journal of the International Society for Analytical Cytology Aug, 2015 | Pubmed ID: 25892097
Esters of Bendamustine Are by Far More Potent Cytotoxic Agents than the Parent Compound against Human Sarcoma and Carcinoma Cells.
PloS one , 2015 | Pubmed ID: 26196503
Histamine H(1)- and H(4)-receptor signaling cooperatively regulate MAPK activation.
Biochemical pharmacology Dec, 2015 | Pubmed ID: 26385311
Flavonoid derivatives as selective ABCC1 modulators: Synthesis and functional characterization.
European journal of medicinal chemistry Feb, 2016 | Pubmed ID: 26774038
Mimicking of Arginine by Functionalized N(ω)-Carbamoylated Arginine As a New Broadly Applicable Approach to Labeled Bioactive Peptides: High Affinity Angiotensin, Neuropeptide Y, Neuropeptide FF, and Neurotensin Receptor Ligands As Examples.
Journal of medicinal chemistry Mar, 2016 | Pubmed ID: 26824643
BK K+ channel blockade inhibits radiation-induced migration/brain infiltration of glioblastoma cells.
Oncotarget Mar, 2016 | Pubmed ID: 26893360
Conformational Restriction and Enantioseparation Increase Potency and Selectivity of Cyanoguanidine-Type Histamine H4 Receptor Agonists.
Journal of medicinal chemistry Apr, 2016 | Pubmed ID: 27007611
High Affinity Agonists of the Neuropeptide Y (NPY) Y4 Receptor Derived from the C-Terminal Pentapeptide of Human Pancreatic Polypeptide (hPP): Synthesis, Stereochemical Discrimination, and Radiolabeling.
Journal of medicinal chemistry 07, 2016 | Pubmed ID: 27223253
Prototypic F-Labeled Argininamide-Type Neuropeptide Y YR Antagonists as Tracers for PET Imaging of Mammary Carcinoma.
ACS medicinal chemistry letters Mar, 2017 | Pubmed ID: 28337321
Fluorescence- and Radiolabeling of [Lys,Nle]hPP Yields Molecular Tools for the NPY Y Receptor.
Bioconjugate chemistry 04, 2017 | Pubmed ID: 28345900
Molecular Mechanisms of Biased and Probe-Dependent Signaling at CXC-Motif Chemokine Receptor CXCR3 Induced by Negative Allosteric Modulators.
Molecular pharmacology 04, 2018 | Pubmed ID: 29343553
Structural basis of small-molecule inhibition of human multidrug transporter ABCG2.
Nature structural & molecular biology Apr, 2018 | Pubmed ID: 29610494
Structural basis of ligand binding modes at the neuropeptide Y Y receptor.
Nature 04, 2018 | Pubmed ID: 29670288
In Search of NPY YR Antagonists: Incorporation of Carbamoylated Arginine, Aza-Amino Acids, or d-Amino Acids into Oligopeptides Derived from the C-Termini of the Endogenous Agonists.
ACS omega Jul, 2017 | Pubmed ID: 30023699
Tariquidar-Related Chalcones and Ketones as ABCG2 Modulators.
ACS medicinal chemistry letters Aug, 2018 | Pubmed ID: 30128080
Highly Potent, Stable, and Selective Dimeric Hetarylpropylguanidine-Type Histamine H Receptor Agonists.
ACS omega Mar, 2018 | Pubmed ID: 30221224
A split luciferase-based probe for quantitative proximal determination of Gα signalling in live cells.
Scientific reports 11, 2018 | Pubmed ID: 30464299
Alkyl derivatives of 1,3,5-triazine as histamine H receptor ligands.
Bioorganic & medicinal chemistry 04, 2019 | Pubmed ID: 30792106
Split luciferase-based assay for simultaneous analyses of the ligand concentration- and time-dependent recruitment of β-arrestin2.
Analytical biochemistry 05, 2019 | Pubmed ID: 30853375
[H]UR-DEBa176: A 2,4-Diaminopyrimidine-Type Radioligand Enabling Binding Studies at the Human, Mouse, and Rat Histamine H Receptors.
Journal of medicinal chemistry Sep, 2019 | Pubmed ID: 31469288
Basal Histamine H Receptor Activation: Agonist Mimicry by the Diphenylalanine Motif.
Chemistry (Weinheim an der Bergstrasse, Germany) Nov, 2019 | Pubmed ID: 31498478
Judith A. Stolwijk1,
Anne-Kathrin Mildner1,
Christian Kade1,
Michael Skiba1,
Guenther Bernhardt2,
Armin Buschauer2,
Harald Huebner3,
Peter Gmeiner3,
Joachim Wegener1,4
1Institute of Analytical Chemistry, Chemo- and Biosensors, University of Regensburg,
2Institute of Pharmacy, University of Regensburg,
3Department of Chemistry and Pharmacy, Friedrich-Alexander University Erlangen-Nuernberg,
4, Fraunhofer Research Institution for Microsystems and Solid State Technologies EMFT
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