Armin Buschauer

Publications

• Basal Histamine H Receptor Activation: Agonist Mimicry by the Diphenylalanine Motif
  Chemistry (Weinheim an Der Bergstrasse, Germany). Nov, 2019  |   Pubmed ID: 31498478
• [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
• 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
• Alkyl Derivatives of 1,3,5-triazine As Histamine H Receptor Ligands
  Bioorganic & Medicinal Chemistry. 04, 2019  |   Pubmed ID: 30792106
• A Split Luciferase-based Probe for Quantitative Proximal Determination of Gα Signalling in Live Cells
  Scientific Reports. 11, 2018  |   Pubmed ID: 30464299
• Highly Potent, Stable, and Selective Dimeric Hetarylpropylguanidine-Type Histamine H Receptor Agonists
  ACS Omega. Mar, 2018  |   Pubmed ID: 30221224
• Tariquidar-Related Chalcones and Ketones As ABCG2 Modulators
  ACS Medicinal Chemistry Letters. Aug, 2018  |   Pubmed ID: 30128080
• Structural Basis of Ligand Binding Modes at the Neuropeptide Y Y Receptor
  Nature. 04, 2018  |   Pubmed ID: 29670288
• Structural Basis of Small-molecule Inhibition of Human Multidrug Transporter ABCG2
  Nature Structural & Molecular Biology. Apr, 2018  |   Pubmed ID: 29610494
• 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
• 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
• Fluorescence- and Radiolabeling of [Lys,Nle]hPP Yields Molecular Tools for the NPY Y Receptor
  Bioconjugate Chemistry. 04, 2017  |   Pubmed ID: 28345900
• 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
• 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
• Conformational Restriction and Enantioseparation Increase Potency and Selectivity of Cyanoguanidine-Type Histamine H4 Receptor Agonists
  Journal of Medicinal Chemistry. Apr, 2016  |   Pubmed ID: 27007611
• BK K+ Channel Blockade Inhibits Radiation-induced Migration/brain Infiltration of Glioblastoma Cells
  Oncotarget. Mar, 2016  |   Pubmed ID: 26893360
• 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
• Flavonoid Derivatives As Selective ABCC1 Modulators: Synthesis and Functional Characterization
  European Journal of Medicinal Chemistry. Feb, 2016  |   Pubmed ID: 26774038
• Histamine H(1)- and H(4)-receptor Signaling Cooperatively Regulate MAPK Activation
  Biochemical Pharmacology. Dec, 2015  |   Pubmed ID: 26385311
• 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
• 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
• Toward Labeled Argininamide-Type NPY Y1 Receptor Antagonists: Identification of a Favorable Propionylation Site in BIBO3304
  Archiv Der Pharmazie. Jun, 2015  |   Pubmed ID: 25884646
• 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
• 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
• Dimeric Carbamoylguanidine-type Histamine H2 Receptor Ligands: A New Class of Potent and Selective Agonists
  Bioorganic & Medicinal Chemistry. Jul, 2015  |   Pubmed ID: 25639885
• 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
• No Evidence for Histamine H4 Receptor in Human Monocytes
  The Journal of Pharmacology and Experimental Therapeutics. Dec, 2014  |   Pubmed ID: 25273276
• 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
• Synthesis and Dual Histamine H₁ and H₂ Receptor Antagonist Activity of Cyanoguanidine Derivatives
  Molecules (Basel, Switzerland). Nov, 2013  |   Pubmed ID: 24248146
• 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
• Dimeric Argininamide-type Neuropeptide Y Receptor Antagonists: Chiral Discrimination Between Y1 and Y4 Receptors
  Bioorganic & Medicinal Chemistry. Nov, 2013  |   Pubmed ID: 24074877
• 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
• 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
• Molecular and Cellular Analysis of Human Histamine Receptor Subtypes
  Trends in Pharmacological Sciences. Jan, 2013  |   Pubmed ID: 23254267
• 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
• 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
• Fast Counter-electroosmotic Capillary Electrophoresis-time-of-flight Mass Spectrometry of Hyaluronan Oligosaccharides
  Analytical and Bioanalytical Chemistry. Mar, 2012  |   Pubmed ID: 21800126
• 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
• Design of Benzimidazole- and Benzoxazole-2-thione Derivatives As Inhibitors of Bacterial Hyaluronan Lyase
  European Journal of Medicinal Chemistry. Sep, 2011  |   Pubmed ID: 21803461
• 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
• 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
• 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
• Histamine H4 Receptor Agonists
  Bioorganic & Medicinal Chemistry Letters. Dec, 2010  |   Pubmed ID: 21044842
• 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
• Chiral NG-acylated Hetarylpropylguanidine-type Histamine H2 Receptor Agonists Do Not Show Significant Stereoselectivity
  Bioorganic & Medicinal Chemistry Letters. May, 2010  |   Pubmed ID: 20409707
• Synthesis and Structure-activity Relationships of Cyanoguanidine-type and Structurally Related Histamine H4 Receptor Agonists
  Journal of Medicinal Chemistry. Oct, 2009  |   Pubmed ID: 19791743
• 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
• 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
• 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
• 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
• Frontiers in Medicinal Chemistry in Regensburg
  ChemMedChem. Aug, 2008  |   Pubmed ID: 18655207
• 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
• Isoenzyme-specific Differences in the Degradation of Hyaluronic Acid by Mammalian-type Hyaluronidases
  Glycoconjugate Journal. Feb, 2008  |   Pubmed ID: 17620008
• 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
• 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
• Inhibitors of Kinesin Eg5: Antiproliferative Activity of Monastrol Analogues Against Human Glioblastoma Cells
  Cancer Chemotherapy and Pharmacology. Feb, 2007  |   Pubmed ID: 16703323
• 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
• Novel 6-O-acylated Vitamin C Derivatives As Hyaluronidase Inhibitors with Selectivity for Bacterial Lyases
  Bioorganic & Medicinal Chemistry Letters. Oct, 2006  |   Pubmed ID: 16908142
• 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
• 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
• 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
• Sulphated Oligosaccharides As Inhibitors of Hyaluronidases from Bovine Testis, Bee Venom and Streptococcus Agalactiae
  Planta Medica. Aug, 2005  |   Pubmed ID: 16142636
• 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
• Structure-activity Relationships of Histamine H2 Receptor Ligands
  Mini Reviews in Medicinal Chemistry. Nov, 2004  |   Pubmed ID: 15544555
• 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
• 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
• Transport of Paclitaxel (Taxol) Across the Blood-brain Barrier in Vitro and in Vivo
  The Journal of Clinical Investigation. Nov, 2002  |   Pubmed ID: 12417570
• Polyamine Levels of Human Colorectal Adenocarcinomas Are Correlated with Tumor Stage and Grade
  International Journal of Colorectal Disease. Nov, 2002  |   Pubmed ID: 12355213