Armin Buschauer

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Armin Buschauer (2010)

Armin Buschauer (born March 31, 1955 in Herchweiler ; † July 18, 2017 in Lappersdorf ) was a German pharmaceutical and medical chemist and pharmacist. From 1993 to 2017 he was professor and holder of the chair for Pharmaceutical and Medicinal Chemistry II as well as temporarily managing director of the Institute for Pharmacy, Vice Dean and Dean of the Faculty of Chemistry and Pharmacy and a member of the Senate at the University of Regensburg .

His work was oriented towards modern medical-chemical drug research. In his teaching, the focus was on interdisciplinary scientific training for pharmacists, with which they can survive not only in the pharmacy, but also in university and industrial research.

Life

Armin Buschauer studied pharmacy at the Johannes Gutenberg University in Mainz from 1975 to 1979 and received his license to practice medicine in 1980 . In 1984 he received his doctorate in Mainz under the guidance of Professor Walter Schunack Dr. rer. nat. via histamine H 2 receptor-selective imidazole compounds with a target-oriented medical-chemical approach. In 1990 he qualified as a professor at the Free University of Berlin in the field of pharmaceutical chemistry with a thesis on positively inotropically effective histamine receptor agonists. In 1993 he was appointed full professor at the University of Regensburg, where he held the Chair of Pharmaceutical and Medicinal Chemistry II until his death.

Scientific research and work areas

The focus of his scientific work in medicinal chemistry was on the development of new ligands for G-protein-coupled receptors . By combining chemical syntheses and rational drug design , he and his colleagues developed numerous new substances that were comprehensively characterized by analytical, pharmacological, molecular and cell biological investigations as well as structure-activity relationships. High-affinity receptor ligands for the various histamine and neuropeptide Y receptor subtypes were created. These ligands also served as pharmacological tools to elucidate binding and action mechanisms. In this regard, the development of fluorescent and radioligands for aminergic and peptidergic GPCRs was of particular importance. Another medical-chemical research area was hyaluronic acids, bacterial and human hyaluronidases, their characterization and the structure-based development of hyaluronidase inhibitors.

Preclinical tumor pharmacology was Armin Buschauer's second research focus. The focus was on pharmacokinetic approaches for the improved therapy of brain tumors such as the use of ABC transporter modulators to overcome the blood-brain barrier with cytostatic drugs and interstitial chemotherapy, in which biodegradable polymers are loaded with cytostatic drugs and implanted directly in the tumor area. Further tumor pharmacological studies concerned the use of PDGFR antagonists and kinesin inhibitors in glioblastomas and the co-administration of hyaluronidases in breast cancer in order to improve the penetration of cytostatic drugs into the tumor and thus to achieve tumor-effective drug levels.

These focal points also included the development and application of biochemical and (molecular) pharmacological test methods (assays). In addition to binding studies using radio and fluorescent ligands, studies on isolated organs, functional cellular assays and the cloning and expression of GPCR mutants, luminescence- based methods for the analysis of ligand-GPCR interactions and the effects of the co-administration of cytostatics and ABC transporters used in the chemotherapy of malignant brain tumors (fluorescence or bioluminescence imaging).

Armin Buschauer has published more than 250 articles in scientific journals, supervised over 80 doctorates and was spokesman for two DFG graduate colleges on ligands of G-protein coupled receptors from 2002-2011 and 2013-2017 .

Prizes and awards

Publications (selection)

  • Armin Buschauer: Synthesis and in vitro pharmacology of arpromidine and related Phenylpyridylalkylguanidines, a potential new class of positive inotropic drugs. In: Journal of Medicinal Chemistry 32, 1989, pp. 1963-1970.
  • Martial Ruat, Elisabeth Traiffort, ML Bouthenet, Jean-Charles Schwartz, Jürgen Hirschfeld, Armin Buschauer, Walter Schunack: Reversible and irreversible labeling and autoradiographic localization of the cerebral histamine H_2-receptor. In: Proceedings of the National Academy of Sciences of the USA 87, 1990, pp. 1658-1662.
  • Iris Aiglstorfer, Ingo Hendrich, Christiane Moser, Günther Bernhardt, Stefan Dove, Armin Buschauer: Structure-Activity Relationships of Neuropeptide Y Y_1 Receptor Antagonists Related to BIBP 3226. In: Bioorganic & Medicinal Chemistry Letters 10, 2000, pp. 1597–1600.
  • Melissa T. Kelley, Tilmann Bürckstümmer, Katharina Wenzel-Seifert, Stefan Dove, Armin Buschauer, Roland Seifert: Distinct interaction of human and guinea pig histamine H_2-Receptor with guanidine-type agonists. In: Molecular Pharmacology 60, 2001, pp. 1210-1225.
  • Stephan Fellner, Björn Bauer, David S. Miller, Martina Schaffrick, Martina Fankhänel, Thilo Spruß, Günther Bernhardt, Claudia Graeff, Lothar Färber, Harald Gschaidmeier, Armin Buschauer, Gert Fricker: Transport of paclitaxel (Taxol) across the blood-brain barrier in vitro and in vivo. In: The Journal of Clinical Investigation 110, 2002, pp. 1309-1318.
  • Alexander Botzki, Daniel J. Rigden, Stephan Braun, Masatoshi Nukui, Sunnhild Salmen, Julia Hoechstetter, Günther Bernhardt, Stefan Dove, Armin Buschauer, Mark J. Jedrzejas: L-ascorbic acid-6-hexadecanoate, a potent hyaluronidase inhibitor: X- ray structure and molecular modeling of enzyme-inhibitor complexes. In: The Journal of Biological Chemistry 279, 2004, pp. 45990-45997.
  • Dietmar Gross, Günther Bernhardt, Armin Buschauer: Platelet-derived growth factor receptor independent proliferation of human glioblastoma cells: selective tyrosine kinase inhibitors lack antiproliferative activity. In: Journal of Cancer Research and Clinical Oncology 132, 2006, pp. 589-599.
  • Erich Schneider, Matthias Mayer, Ralf Ziemek, Liantao Li, Christoph Hutzler, Günther Bernhardt, Armin Buschauer: A Simple and Powerful Flow Cytometric Method for the Simultaneous Determination of Multiple Parameters at G-Protein-Coupled Receptor Subtypes. In: ChemBioChem 7, 2006, pp. 1400-1409.
  • Ralf Ziemek, Albert Brennauer, Erich Schneider, Chiara Cabrele, Annette G. Beck-Sickinger, Günther Bernhardt, Armin Buschauer: Fluorescence- and luminescence-based methods for the determination of affinity and activity of neuropeptide Y (2) receptor ligands. In: European Journal of Pharmacology 551, 2006, pp. 10-8.
  • Edith SA Hofinger, Martin Spickenreither, Jan Oschmann, Günther Bernhardt, Rainer Rudolph, Armin Buschauer: Recombinant human hyaluronidase Hyal-1: insect cells versus E. coli as expression system and identification of low molecular weight inhibitors. In: Glycobiology 17, 2007, pp. 444-453.
  • Erich Schneider, Max Keller, Albert Brennauer, Bianca K. Hoefelschweiger, Dietmar Gross, Otto S. Wolfbeis, Günther Bernhardt, Armin Buschauer: Synthesis and Characterization of the First Fluorescent Nonpeptide NPY Y1 Receptor Antagonist. In: ChemBioChem 8, 2007, pp. 1981–1988.
  • Max Keller, Nathalie Pop, Christoph Hutzler, Annette G. Beck-Sickinger, Günther Bernhardt, Armin Buschauer: 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. In: Journal of Medicinal Chemistry 51, 2008, pp. 8168-8172 .
  • Patrick Igel, Erich Schneider, David Schnell, Sigurd Elz, Roland Seifert, Armin Buschauer: N (G) -Acylated imidazolylpropylguanidines as potent histamine H4 receptor agonists: selectivity by variation of the N (G) -substituent. In: Journal of Medicinal Chemistry 52, 2009, pp. 2623-2627.
  • Patrick Igel, David Schnell, Günther Bernhardt, Roland Seifert, Armin Buschauer: Tritium-labeled N1- [3- (1H-imidazol-4-yl) propyl] -N2-propionylguanidine ([3H] UR-PI294), a high affinity histamine H3 and H4 receptor radioligand. In: ChemMedChem 4, 2009, pp. 225-231.
  • Matthias Kühnle, Michael Egger, Christine Müller, Anne Mahringer, Günther Bernhardt, Gert Fricker, Burkhard König, Armin Buschauer: Potent and selective inhibitors of breast cancer resistance protein (ABCG2) derived from the p-glycoprotein (ABCB1) modulator tariquidar. In: Journal of Medicinal Chemistry 52, 2009, pp. 1190-1197.
  • Max Keller, Daniela Erdmann, Shangjun Teng, Nathalie Pop, Nikola Pluym, Günther Bernhardt, Armin Buschauer: Red-fluorescent argininamide-type NPY Y (1) receptor antagonists as pharmacological tools. In: Bioorganic & Medicinal Chemistry 19, 2011, pp. 2859-2878.
  • Tobias Birnkammer, Anja Spickenreither, Irena Brunskole, Miroslaw Lopuch, Nicole Kagermeier, Günther Bernhardt, Stefan Dove, Roland Seifert, Sigurd Elz, Armin Buschauer: The bivalent ligand approach leads to highly potent and selective acylguanidine-type histamine H2 receptor agonists. In: Journal of Medicinal Chemistry 55, 2012, pp. 1147-1160.
  • Uwe Nordemann, David Wifling, David Schnell, Günther Bernhardt, Holger Stark, Roland Seifert, Armin Buschauer: Luciferase reporter gene assay on human, murine and rat histamine H4 receptor orthologs: correlations and discrepancies between distal and proximal readouts. In: PLoS One 8, 2013, p. E73961.
  • Roland Seifert, Andrea Strasser, Erich H. Schneider, Detlef Neumann, Stefan Dove, Armin Buschauer: Molecular and cellular analysis of human histamine receptor subtypes. In: Trends in Pharmacological Sciences 34, 2013, pp. 33-58.
  • Paul Baumeister, Daniela Erdmann, Sabrina Biselli, Nicole Kagermeier, Sigurd Elz, Günther Bernhardt, Armin Buschauer: 3HUR-DE257: Development of a tritium-labeled squaramide-type selective histamine H2 receptor antagonist. In: ChemMedChem 10, 2015, pp. 83-93.
  • Stefan Huber, Johannes Philip Huettner, Hacker Kristina, Günther Bernhardt, Jörg König, Armin Buschauer: Esters of bendamustine are by far more potent cytotoxic agents than the parent compound against human sarcoma and carcinoma cells. In: PLoS One 10, 2015, p. E0133743.
  • David Wifling, Karolinaken, Uwe Nordemann, Andrea Strasser, Günther Bernhardt, Stefan Dove, Roland Seifert, Armin Buschauer: Molecular determinants for the high constitutive activity of the human histamine H4 receptor: Functional studies on orthologs and mutants. In: British Journal of Pharmacology 172, 2015, pp. 785-798.
  • Max Keller, Kilian K. Kuhn, Jürgen Einsiedel, Harald Hübner, Sabrina Biselli, Catherine Mollereau, David Wifling, Jaroslava Svobodova, Günther Bernhardt, Chiara Cabrele, Patrick Vanderheyden, Peter Gmeiner, Armin Buschauer: Mimicking of arginine by functionalized Nω-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. In: Journal of Medicinal Chemistry 59, 2016, pp. 1925-1945.
  • Kilian K. Kuhn, Thomas Ertl, Stefanie Dukorn, Max Keller, Günther Bernhardt, Oliver Reiser, Armin Buschauer: 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. In: Journal of Medicinal Chemistry 59, 2016, pp. 6045-6058.
  • Sebastian Lieb, Timo Littmann, Nicole Plank, Johannes Felixberger, Miho Tanaka, Thorsten Schäfer, Stéphane Krief, Sigurd Elz, Kristina Friedland, Günther Bernhardt, Joachim Wegener, Takeaki Ozawa, Armin Buschauer: Label-free versus conventional cellular assays: functional investigations on the human histamine H1 receptor. In: Pharmacological Research 114, 2016, pp. 13-26.

Web links

Individual evidence

  1. ↑ Katrin Gross: In memory of Prof. Dr. Armin Buschauer - University of Regensburg. Retrieved April 22, 2018 .
  2. ↑ Prof. Dr. Armin Buschauer: Obituary notice . ( Mittelbayerische-trauer.de [accessed on April 22, 2018]).
  3. ^ Obituary: In memoriam Armin Buschauer, Regensburg . In: DAZ.online . August 10, 2017 ( deutsche-apotheker-zeitung.de [accessed April 25, 2018]).
  4. ↑ Buschauer Secretariat: Prof. Dr. Armin Buschauer - University of Regensburg. Retrieved April 22, 2018 .
  5. ↑ Carl Mannich research grant for PD Dr. Armin Buschauer . In: Pharmacy in Our Time . tape 20 , no. 3 , 1991, ISSN  0048-3664 , pp. 116-116 , doi : 10.1002 / pauz.19910200311 .
  6. ↑ Pharmaceutical Science Award : Phoenix honors top pharmaceutical research . In: DAZ.online . October 26, 2003 ( deutsche-apotheker-zeitung.de [accessed April 25, 2018]).
personal data
SURNAME Buschauer, Armin
BRIEF DESCRIPTION German pharmaceutical and medical chemist and pharmacist
DATE OF BIRTH March 31, 1955
PLACE OF BIRTH Herchweiler
DATE OF DEATH 18th July 2017
Place of death Lappersdorf