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Items: 1 to 50 of 173

1.

Basal Histamine H4 Receptor Activation: Agonist Mimicry by the Diphenylalanine Motif.

Wifling D, Pfleger C, Kaindl J, Ibrahim P, Kling RC, Buschauer A, Gohlke H, Clark T.

Chemistry. 2019 Nov 18;25(64):14613-14624. doi: 10.1002/chem.201902801. Epub 2019 Oct 16.

PMID:
31498478
2.

[3H]UR-DEBa176: A 2,4-Diaminopyrimidine-Type Radioligand Enabling Binding Studies at the Human, Mouse, and Rat Histamine H4 Receptors.

Bartole E, Littmann T, Tanaka M, Ozawa T, Buschauer A, Bernhardt G.

J Med Chem. 2019 Sep 12;62(17):8338-8356. doi: 10.1021/acs.jmedchem.9b01342. Epub 2019 Aug 30.

PMID:
31469288
3.

Increasing the throughput of label-free cell assays to study the activation of G-protein-coupled receptors by using a serial agonist exposure protocol.

Stolwijk JA, Skiba M, Kade C, Bernhardt G, Buschauer A, Hübner H, Gmeiner P, Wegener J.

Integr Biol (Camb). 2019 May 13. pii: zyz010. doi: 10.1093/intbio/zyz010. [Epub ahead of print]

PMID:
31083709
4.

Structure-Activity Relationship of Hetarylpropylguanidines Aiming at the Development of Selective Histamine Receptor Ligands.

Pockes S, Wifling D, Buschauer A, Elz S.

ChemistryOpen. 2019 Mar 5;8(3):285-297. doi: 10.1002/open.201900011. eCollection 2019 Mar.

5.

Split luciferase-based assay for simultaneous analyses of the ligand concentration- and time-dependent recruitment of β-arrestin2.

Littmann T, Buschauer A, Bernhardt G.

Anal Biochem. 2019 May 15;573:8-16. doi: 10.1016/j.ab.2019.02.023. Epub 2019 Mar 8.

PMID:
30853375
6.

Alkyl derivatives of 1,3,5-triazine as histamine H4 receptor ligands.

Łażewska D, Mogilski S, Hagenow S, Kuder K, Głuch-Lutwin M, Siwek A, Więcek M, Kaleta M, Seibel U, Buschauer A, Filipek B, Stark H, Kieć-Kononowicz K.

Bioorg Med Chem. 2019 Apr 1;27(7):1254-1262. doi: 10.1016/j.bmc.2019.02.020. Epub 2019 Feb 12.

PMID:
30792106
7.

A split luciferase-based probe for quantitative proximal determination of Gαq signalling in live cells.

Littmann T, Ozawa T, Hoffmann C, Buschauer A, Bernhardt G.

Sci Rep. 2018 Nov 21;8(1):17179. doi: 10.1038/s41598-018-35615-w.

8.

Highly Potent, Stable, and Selective Dimeric Hetarylpropylguanidine-Type Histamine H2 Receptor Agonists.

Pockes S, Wifling D, Keller M, Buschauer A, Elz S.

ACS Omega. 2018 Mar 31;3(3):2865-2882. doi: 10.1021/acsomega.8b00128. Epub 2018 Mar 9.

9.

Tariquidar-Related Chalcones and Ketones as ABCG2 Modulators.

Peña-Solórzano D, Scholler M, Bernhardt G, Buschauer A, König B, Ochoa-Puentes C.

ACS Med Chem Lett. 2018 Jul 25;9(8):854-859. doi: 10.1021/acsmedchemlett.8b00289. eCollection 2018 Aug 9.

10.

In Search of NPY Y4R Antagonists: Incorporation of Carbamoylated Arginine, Aza-Amino Acids, or d-Amino Acids into Oligopeptides Derived from the C-Termini of the Endogenous Agonists.

Kuhn KK, Littmann T, Dukorn S, Tanaka M, Keller M, Ozawa T, Bernhardt G, Buschauer A.

ACS Omega. 2017 Jul 31;2(7):3616-3631. doi: 10.1021/acsomega.7b00451. Epub 2017 Jul 14.

11.

Structural basis of ligand binding modes at the neuropeptide Y Y1 receptor.

Yang Z, Han S, Keller M, Kaiser A, Bender BJ, Bosse M, Burkert K, Kögler LM, Wifling D, Bernhardt G, Plank N, Littmann T, Schmidt P, Yi C, Li B, Ye S, Zhang R, Xu B, Larhammar D, Stevens RC, Huster D, Meiler J, Zhao Q, Beck-Sickinger AG, Buschauer A, Wu B.

Nature. 2018 Apr;556(7702):520-524. doi: 10.1038/s41586-018-0046-x. Epub 2018 Apr 18.

12.

Structural basis of small-molecule inhibition of human multidrug transporter ABCG2.

Jackson SM, Manolaridis I, Kowal J, Zechner M, Taylor NMI, Bause M, Bauer S, Bartholomaeus R, Bernhardt G, Koenig B, Buschauer A, Stahlberg H, Altmann KH, Locher KP.

Nat Struct Mol Biol. 2018 Apr;25(4):333-340. doi: 10.1038/s41594-018-0049-1. Epub 2018 Apr 2.

PMID:
29610494
13.

Molecular Mechanisms of Biased and Probe-Dependent Signaling at CXC-Motif Chemokine Receptor CXCR3 Induced by Negative Allosteric Modulators.

Brox R, Milanos L, Saleh N, Baumeister P, Buschauer A, Hofmann D, Heinrich MR, Clark T, Tschammer N.

Mol Pharmacol. 2018 Apr;93(4):309-322. doi: 10.1124/mol.117.110296. Epub 2018 Jan 17.

PMID:
29343553
14.

Fluorescence- and Radiolabeling of [Lys4,Nle17,30]hPP Yields Molecular Tools for the NPY Y4 Receptor.

Dukorn S, Littmann T, Keller M, Kuhn K, Cabrele C, Baumeister P, Bernhardt G, Buschauer A.

Bioconjug Chem. 2017 Apr 19;28(4):1291-1304. doi: 10.1021/acs.bioconjchem.7b00103. Epub 2017 Apr 5.

PMID:
28345900
15.

Prototypic 18F-Labeled Argininamide-Type Neuropeptide Y Y1R Antagonists as Tracers for PET Imaging of Mammary Carcinoma.

Keller M, Maschauer S, Brennauer A, Tripal P, Koglin N, Dittrich R, Bernhardt G, Kuwert T, Wester HJ, Buschauer A, Prante O.

ACS Med Chem Lett. 2017 Feb 21;8(3):304-309. doi: 10.1021/acsmedchemlett.6b00467. eCollection 2017 Mar 9.

16.

Label-free versus conventional cellular assays: Functional investigations on the human histamine H1 receptor.

Lieb S, Littmann T, Plank N, Felixberger J, Tanaka M, Schäfer T, Krief S, Elz S, Friedland K, Bernhardt G, Wegener J, Ozawa T, Buschauer A.

Pharmacol Res. 2016 Dec;114:13-26. doi: 10.1016/j.phrs.2016.10.010. Epub 2016 Oct 15.

PMID:
27751876
17.

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.

Kuhn KK, Ertl T, Dukorn S, Keller M, Bernhardt G, Reiser O, Buschauer A.

J Med Chem. 2016 Jul 14;59(13):6045-58. doi: 10.1021/acs.jmedchem.6b00309. Epub 2016 Jun 22.

PMID:
27223253
18.

Label-free analysis of GPCR-stimulation: The critical impact of cell adhesion.

Lieb S, Michaelis S, Plank N, Bernhardt G, Buschauer A, Wegener J.

Pharmacol Res. 2016 Jun;108:65-74. doi: 10.1016/j.phrs.2016.04.026. Epub 2016 Apr 28.

PMID:
27133553
19.

Conformational Restriction and Enantioseparation Increase Potency and Selectivity of Cyanoguanidine-Type Histamine H4 Receptor Agonists.

Geyer R, Nordemann U, Strasser A, Wittmann HJ, Buschauer A.

J Med Chem. 2016 Apr 14;59(7):3452-70. doi: 10.1021/acs.jmedchem.6b00120. Epub 2016 Apr 5.

PMID:
27007611
20.

BK K+ channel blockade inhibits radiation-induced migration/brain infiltration of glioblastoma cells.

Edalat L, Stegen B, Klumpp L, Haehl E, Schilbach K, Lukowski R, Kühnle M, Bernhardt G, Buschauer A, Zips D, Ruth P, Huber SM.

Oncotarget. 2016 Mar 22;7(12):14259-78. doi: 10.18632/oncotarget.7423.

21.

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.

Keller M, Kuhn KK, Einsiedel J, Hübner H, Biselli S, Mollereau C, Wifling D, Svobodová J, Bernhardt G, Cabrele C, Vanderheyden PM, Gmeiner P, Buschauer A.

J Med Chem. 2016 Mar 10;59(5):1925-45. doi: 10.1021/acs.jmedchem.5b01495. Epub 2016 Feb 11.

PMID:
26824643
22.

Flavonoid derivatives as selective ABCC1 modulators: Synthesis and functional characterization.

Obreque-Balboa JE, Sun Q, Bernhardt G, König B, Buschauer A.

Eur J Med Chem. 2016 Feb 15;109:124-33. doi: 10.1016/j.ejmech.2015.12.010. Epub 2015 Dec 13.

PMID:
26774038
23.

N(ω)-Carbamoylation of the Argininamide Moiety: An Avenue to Insurmountable NPY Y1 Receptor Antagonists and a Radiolabeled Selective High-Affinity Molecular Tool ([(3)H]UR-MK299) with Extended Residence Time.

Keller M, Weiss S, Hutzler C, Kuhn KK, Mollereau C, Dukorn S, Schindler L, Bernhardt G, König B, Buschauer A.

J Med Chem. 2015 Nov 25;58(22):8834-49. doi: 10.1021/acs.jmedchem.5b00925. Epub 2015 Nov 4.

PMID:
26466164
24.

Histamine H(1)- and H(4)-receptor signaling cooperatively regulate MAPK activation.

Beermann S, Bernhardt G, Seifert R, Buschauer A, Neumann D.

Biochem Pharmacol. 2015 Dec 1;98(3):432-9. doi: 10.1016/j.bcp.2015.09.011. Epub 2015 Sep 15.

PMID:
26385311
25.

Autodisplay of Human Hyaluronidase Hyal-1 on Escherichia coli and Identification of Plant-Derived Enzyme Inhibitors.

Orlando Z, Lengers I, Melzig MF, Buschauer A, Hensel A, Jose J.

Molecules. 2015 Aug 26;20(9):15449-68. doi: 10.3390/molecules200915449.

26.

Esters of Bendamustine Are by Far More Potent Cytotoxic Agents than the Parent Compound against Human Sarcoma and Carcinoma Cells.

Huber S, Huettner JP, Hacker K, Bernhardt G, König J, Buschauer A.

PLoS One. 2015 Jul 21;10(7):e0133743. doi: 10.1371/journal.pone.0133743. eCollection 2015.

27.

Flow cytometric analysis with a fluorescently labeled formyl peptide receptor ligand as a new method to study the pharmacological profile of the histamine H2 receptor.

Werner K, Kälble S, Wolter S, Schneider EH, Buschauer A, Neumann D, Seifert R.

Naunyn Schmiedebergs Arch Pharmacol. 2015 Oct;388(10):1039-52. doi: 10.1007/s00210-015-1133-2. Epub 2015 May 30.

PMID:
26021872
28.

Topotecan-induced ABCG2 expression in MCF-7 cells is associated with decreased CD24 and EpCAM expression and a loss of tumorigenicity.

Huber S, Wege AK, Bernhardt G, Buschauer A, Brockhoff G.

Cytometry A. 2015 Aug;87(8):707-16. doi: 10.1002/cyto.a.22675. Epub 2015 Apr 17.

29.

Toward Labeled Argininamide-Type NPY Y1 Receptor Antagonists: Identification of a Favorable Propionylation Site in BIBO3304.

Keller M, Schindler L, Bernhardt G, Buschauer A.

Arch Pharm (Weinheim). 2015 Jun;348(6):390-8. doi: 10.1002/ardp.201400427. Epub 2015 Apr 17.

PMID:
25884646
30.

High performance anion exchange chromatography with pulsed amperometric detection (HPAEC-PAD) for the sensitive determination of hyaluronan oligosaccharides.

Rothenhöfer M, Grundmann M, Bernhardt G, Matysik FM, Buschauer A.

J Chromatogr B Analyt Technol Biomed Life Sci. 2015 Apr 15;988:106-15. doi: 10.1016/j.jchromb.2015.02.027. Epub 2015 Feb 25.

PMID:
25768984
31.

M2 Subtype preferring dibenzodiazepinone-type muscarinic receptor ligands: Effect of chemical homo-dimerization on orthosteric (and allosteric?) binding.

Keller M, Tränkle C, She X, Pegoli A, Bernhardt G, Buschauer A, Read RW.

Bioorg Med Chem. 2015 Jul 15;23(14):3970-90. doi: 10.1016/j.bmc.2015.01.015. Epub 2015 Jan 14.

PMID:
25650309
32.

Dimeric carbamoylguanidine-type histamine H2 receptor ligands: A new class of potent and selective agonists.

Kagermeier N, Werner K, Keller M, Baumeister P, Bernhardt G, Seifert R, Buschauer A.

Bioorg Med Chem. 2015 Jul 15;23(14):3957-69. doi: 10.1016/j.bmc.2015.01.012. Epub 2015 Jan 14.

PMID:
25639885
33.

The extracellular loop 2 (ECL2) of the human histamine H4 receptor substantially contributes to ligand binding and constitutive activity.

Wifling D, Bernhardt G, Dove S, Buschauer A.

PLoS One. 2015 Jan 28;10(1):e0117185. doi: 10.1371/journal.pone.0117185. eCollection 2015. Erratum in: PLoS One. 2015;10(3):e0122162.

34.

Stabilities of neutral and basic esters of bendamustine in plasma compared to the parent compound: kinetic investigations by HPLC.

Huber S, Antoni F, Schickaneder C, Schickaneder H, Bernhardt G, Buschauer A.

J Pharm Biomed Anal. 2015 Feb;104:137-43. doi: 10.1016/j.jpba.2014.11.038. Epub 2014 Nov 27.

PMID:
25499654
35.

[(3) H]UR-DE257: development of a tritium-labeled squaramide-type selective histamine H2 receptor antagonist.

Baumeister P, Erdmann D, Biselli S, Kagermeier N, Elz S, Bernhardt G, Buschauer A.

ChemMedChem. 2015 Jan;10(1):83-93. doi: 10.1002/cmdc.201402344. Epub 2014 Oct 15.

PMID:
25320025
36.

Loratadine and analogues: discovery and preliminary structure-activity relationship of inhibitors of the amino acid transporter B(0)AT2.

Cuboni S, Devigny C, Hoogeland B, Strasser A, Pomplun S, Hauger B, Höfner G, Wanner KT, Eder M, Buschauer A, Holsboer F, Hausch F.

J Med Chem. 2014 Nov 26;57(22):9473-9. doi: 10.1021/jm501086v. Epub 2014 Nov 7.

PMID:
25318072
37.

No evidence for histamine H4 receptor in human monocytes.

Werner K, Neumann D, Buschauer A, Seifert R.

J Pharmacol Exp Ther. 2014 Dec;351(3):519-26. doi: 10.1124/jpet.114.218107. Epub 2014 Oct 1.

PMID:
25273276
38.

Molecular determinants for the high constitutive activity of the human histamine H4 receptor: functional studies on orthologues and mutants.

Wifling D, Löffel K, Nordemann U, Strasser A, Bernhardt G, Dove S, Seifert R, Buschauer A.

Br J Pharmacol. 2015 Feb;172(3):785-98. doi: 10.1111/bph.12801. Epub 2014 Sep 5.

39.

Biodistribution of quantum dots in the kidney after intravenous injection.

Pollinger K, Hennig R, Bauer S, Breunig M, Tessmar J, Buschauer A, Witzgall R, Goepferich A.

J Nanosci Nanotechnol. 2014 May;14(5):3313-9.

PMID:
24734546
40.

Synthesis and functional characterization of imbutamine analogs as histamine H3 and H4 receptor ligands.

Geyer R, Kaske M, Baumeister P, Buschauer A.

Arch Pharm (Weinheim). 2014 Feb;347(2):77-88. doi: 10.1002/ardp.201300316. Epub 2013 Nov 12.

PMID:
24493592
41.

Synthesis and dual histamine H₁ and H₂ receptor antagonist activity of cyanoguanidine derivatives.

Sadek B, Alisch R, Buschauer A, Elz S.

Molecules. 2013 Nov 15;18(11):14186-202. doi: 10.3390/molecules181114186.

42.

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.

Berlicki L, Kaske M, Gutiérrez-Abad R, Bernhardt G, Illa O, Ortuño RM, Cabrele C, Buschauer A, Reiser O.

J Med Chem. 2013 Nov 14;56(21):8422-31. doi: 10.1021/jm4008505. Epub 2013 Oct 25.

PMID:
24090364
43.

Dimeric argininamide-type neuropeptide Y receptor antagonists: chiral discrimination between Y1 and Y4 receptors.

Keller M, Kaske M, Holzammer T, Bernhardt G, Buschauer A.

Bioorg Med Chem. 2013 Nov 1;21(21):6303-22. doi: 10.1016/j.bmc.2013.08.065. Epub 2013 Sep 8.

PMID:
24074877
44.

Quinoline carboxamide-type ABCG2 modulators: indole and quinoline moieties as anilide replacements.

Bauer S, Ochoa-Puentes C, Sun Q, Bause M, Bernhardt G, König B, Buschauer A.

ChemMedChem. 2013 Nov;8(11):1773-8. doi: 10.1002/cmdc.201300319. Epub 2013 Aug 28.

PMID:
24039190
45.

Luciferase reporter gene assay on human, murine and rat histamine H4 receptor orthologs: correlations and discrepancies between distal and proximal readouts.

Nordemann U, Wifling D, Schnell D, Bernhardt G, Stark H, Seifert R, Buschauer A.

PLoS One. 2013 Sep 2;8(9):e73961. doi: 10.1371/journal.pone.0073961. eCollection 2013.

46.

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.

Brunskole Hummel I, Reinartz MT, Kälble S, Burhenne H, Schwede F, Buschauer A, Seifert R.

PLoS One. 2013 May 31;8(5):e64556. doi: 10.1371/journal.pone.0064556. Print 2013.

47.

Synthesis and pharmacological characterization of new tetrahydrofuran based compounds as conformationally constrained histamine receptor ligands.

Bodensteiner J, Baumeister P, Geyer R, Buschauer A, Reiser O.

Org Biomol Chem. 2013 Jun 28;11(24):4040-55. doi: 10.1039/c3ob40441b.

PMID:
23670795
48.

Benzanilide-Biphenyl Replacement: A Bioisosteric Approach to Quinoline Carboxamide-Type ABCG2 Modulators.

Ochoa-Puentes C, Bauer S, Kühnle M, Bernhardt G, Buschauer A, König B.

ACS Med Chem Lett. 2013 Mar 4;4(4):393-6. doi: 10.1021/ml4000832. eCollection 2013 Apr 11.

49.

[(3)H]UR-PLN196: a selective nonpeptide radioligand and insurmountable antagonist for the neuropeptide Y Y(2) receptor.

Pluym N, Baumeister P, Keller M, Bernhardt G, Buschauer A.

ChemMedChem. 2013 Apr;8(4):587-93. doi: 10.1002/cmdc.201200566. Epub 2013 Jan 29.

PMID:
23361914
50.

Molecular and cellular analysis of human histamine receptor subtypes.

Seifert R, Strasser A, Schneider EH, Neumann D, Dove S, Buschauer A.

Trends Pharmacol Sci. 2013 Jan;34(1):33-58. doi: 10.1016/j.tips.2012.11.001. Epub 2012 Dec 17. Review.

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