Recent Publications Prof. Dr. G. Bernhardt

M. Grundmann, M. Rothenhöfer, G. Bernhardt, A. Buschauer, F.-M. Matysik, Fast counter-electroosmotic capillary electrophoresis–time-of-flight mass spectrometry of hyaluronan oligosaccharides. Anal. Bioanal. Chem. , in press (2011)

S. Braun, A. Botzki, C. Textor, S. Salmen, G. Bernhardt, S. Dove, A. Buschauer, Design of benzimidazole- and benzoxazole-2-thione derivatives as inhibitors of bacterial hyaluronan lyase. Eur. J. Med. Chem. 46, in press (2011)

M. Keller, G. Bernhardt, A. Buschauer, [3H]UR-MK136 - a tritium labelled highly potent and selective neuropeptide Y Y1 receptor antagonist. ChemMedChem 6, in press (2011)

N. Pluym, A. Brennauer, M. Keller, R. Ziemek, N. Pop, G. Bernhardt, A. Buschauer, Application of the guanidine – acylguanidine bioisosteric approach to argininamide-type NPY Y2 receptor antagonists. ChemMedChem 6, in press (2011)

D. Posavec, A. Dorsch, U. Bogner, G. Bernhardt, S. Nagl, Polyvinyl butyral nanobeads: preparation, characterization, biocompatibility and cancer cell uptake. Microchimica Acta 173 (3-4), 391-399 (2011)

C. Ochoa Puentes, P. Höcherl, M. Kühnle, S. Bauer, K. Bürger, G. Bernhardt , A. Buschauer, B. König, Solid phase synthesis of tariquidar-related modulators of ABC transporters preferring breast cancer resistance protein (ABCG2). Bioorg. Med. Chem. Lett. 21 (12), 3654–3657 (2011)

N. Pop, P. Igel, N. Pluym, A. Brennauer, C. Cabrele, G. Bernhardt, R. Seifert, A. Buschauer, Functional reconstitution of human neuropeptide Y (NPY) Y2 and Y4 receptors in Sf9 insect cells. J. Recept. Signal Transduct. 31 (4), 271-285 (2011)

S. Weiss, G. Bernhardt, A. Buschauer, B. König, Synthesis and characterization of DMAP-Modified NPY Y1 receptor antagonists as acyl-transfer catalysts. Collect. Czechoslov. Chem. Commun. 76 (6), 763-780 (2011)

M. Keller, D. Erdmann, N. Pop, N. Pluym, S. Teng, G. Bernhardt, A. Buschauer, Red-fluorescent argininamide-type NPY Y1 receptor antagonists as pharmacological tools. Bioorg. Med. Chem. 19 (9), 2859–2878 (2011)

S. Weiss, M. Keller, G. Bernhardt, A. Buschauer, B. König, N(G)-Acyl-argininamides as NPY Y1 receptor antagonists: Influence of stucturally diverse acyl substituents on stability and affinity. Bioorg. Med. Chem. 18, 6292–6304 (2010)

P. Ghorai, A. Kraus, T. Birnkammer, R. Geyer, G. Bernhardt, S. Dove, R. Seifert, S. Elz, A. Buschauer, Chiral N(G)-acylated hetarylpropylguanidine-type histamine H2 receptor agonists do not show significant stereoselectivity. Bioorg. Med. Chem. Lett. 20 (10), 3173–3176 (2010)

M. Keller, S. Teng, G. Bernhardt, A. Buschauer, Bivalent Argininamide-Type Neuropeptide Y Y1 Antagonists Do Not Support the Hypothesis of Receptor Dimerisation. ChemMedChem 4 (10), 1746-1755 (2009)

Kühnle M, Egger M, Müller M, Mahringer A, Bernhardt G, Fricker G, König B, Buschauer A (2009) Potent and selective inhibitors of breast cancer resistance protein (ABCG2) derived from the p-glycoprotein (ABCB1) modulator tariquidar. J Med Chem 52: 1190–1197

Igel P, Schnell D, Bernhardt G, Seifert R, Buschauer A (2009) Tritium-labeled N1-[3-(1H-imidazol-4-yl)propyl]-N2-propionylguanidine ([3H]UR-PI294), a novel high affinity histamine H3 and H4 receptor radioligand. ChemMedChem 4: 225-231

Kraus A, Ghorai P, Birnkammer T, Schnell D, Elz S, Seifert R, Dove S, Bernhardt G, Buschauer A (2009) N(G)-Acylated aminothiazolylpropylguanidines as potent and selective histamine H2 receptor agonists, ChemMedChem 4: 232-240

Keller M, Pop N, Hutzler C, Beck-Sickinger AG, Bernhardt G, Buschauer A (2008) 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. J Med Chem 51: 8168-8172

Ghorai P, Kraus A, Keller M, Götte C, Igel P, Schneider E, Schnell D, Bernhardt G, Dove S, Zabel M, Elz S, Seifert S, Buschauer A (2008) Acylguanidines as bioisosteres of guanidines: N(G)-acylated imidazolyl­propylguanidines, a new class of histamine H2 receptor agonists. J Med Chem 51: 7193–7204

Weiss S, Keller M, Bernhardt G, Buschauer A, König B (2008) Modular synthesis of non-peptidic bivalent NPY Y1 receptor antagonists. Bioorg Med Chem 16: 9858–9866

Dai J, Jian J, Bosland M, Frenkel K, Bernhardt G, Huang X (2008) Roles of hormone replacement therapy and iron in proliferation of breast epithelial cells with different estrogen and progesterone receptor status. Breast 17: 172-179

Kutta RJ, Hofinger ESA, Preuss H, Bernhardt G, Dick B (2008) Blue light induced interaction of LOV domains from Chlamydomonas reinhardtii. Chembiochem 9: 1931-1938

Bernhardt G, Biersack B, Bollwein S, Schobert R, Zoldakova M (2008) Terpene conjugates of diaminodichloridoplatinum(II) complexes: antiproliferative effects in HL-60 leukemia, 518A2 melanoma and H T-29 colon cancer cells. Chem Biodivers 5: 1645-1659

Hubensack M, Müller C, Höcherl P, Fellner S, Spruss T, Bernhardt G, Buschauer A (2008) Effect of the ABCB1 modulators elacridar and tariquidar on the distribution of paclitaxel in nude mice. J Cancer Res Clin Oncol 134 (5): 597-607

Hofinger ESA, Hoechstetter J, Oettl M, Bernhardt G, Buschauer A (2008) Isoenzyme-specific differences in the degradation of hyaluronic acid by mammalian-type hyaluronidases. Glycoconj J 25 (2): 101-109

Schneider E, Keller M, Brennauer A, Hoefelschweiger B K, Gross D, Wolfbeis O S, Bernhardt G, Buschauer A (2007) Synthesis and Characterization of the First Fluorescent Nonpeptide NPY Y1 Receptor Antagonist.  ChemBioChem 8 (16): 1981-1988

Brennauer A, Keller M, Freund M, Bernhardt G, Buschauer A (2007) Decomposition of 1-(w-aminoalkanoyl)guanidines under alkaline conditions. Tetrahedron Lett. 48 (39): 6996-6999

Hofinger ESA, Bernhardt G, Buschauer A (2007) Kinetics of Hyal1 and PH-20 hyaluronidases: comparison of minimal substrates and analysis of the transglycosylation reaction. Glycobiology 17 (9), 963-971

Ziemek R, Schneider E, Kraus A, Cabrele C, Beck-Sickinger AG, Bernhardt G, Buschauer A (2007) Determination of affinity and activity of ligands at the human neuropeptide Y Y4 receptor by flow cytometry and aequorin luminescence. J Recept Signal Transduct Res 27 (4), 217-233

Egger M, Li X, Müller C, Bernhardt G, Buschauer A, König B (2007) Tariquidar analogues: synthesis by Cu(I)-catalysed N/O–aryl coupling and inhibitory activity against the ABCB1 transporter. Eur J Org Chem (16): 2643-2649

Hofinger E S A, Spickenreither M, Oschmann J, Bernhardt G, Rudolph R, Buschauer A (2007) Recombinant human hyaluronidase Hyal-1: insect cells versus E. coli as expression system and identification of low molecular weight inhibitors. Glycobiology 17: 444-453

Müller C, Gross D, Sarli V, Gartner M, Giannis A, Bernhardt G, Buschauer A (2007) Inhibitors of kinesin Eg5: antiproliferative activity of monastrol analogues against human glioblastoma cells. Cancer Chemother Pharmacol 59: 157-164

Schobert R, Bernhardt G, Biersack B, Bollwein S , Fallahi M, Grotemeier A, Hammond G L (2007) Steroid Conjugates of Dichloro(6-aminomethylnicotinate)platinum(II): Effects on DNA, Sex Hormone Binding Globulin, the Estrogen Receptor, and Various Breast Cancer Cell Lines. ChemMedChem 12: 333-342

Ziemek R, Brennauer A, Schneider E, Cabrele C, Beck-Sickinger A G, Bernhardt G, Buschauer A (2006) Fluorescence- and luminescence-based methods for the determination of affinity and activity of neuropeptide Y(2) receptor ligands. Eur J Pharmacol 551: 10-18

Rigden D J, Botzki A, Nukui M, Mewbourne R B, Lamani E, Braun S, von Angerer E, Bernhardt G, Dove S, Buschauer A, Jedrzejas M J (2006) Design of new benzoxazole-2-thione derived inhibitors of Streptococcus pneumoniae hyaluronan lyase: structure of a complex with a 2-phenylindole. Glycobiology 16: 757-765

Spickenreither M, Braun S, Bernhardt G, Dove S, Buschauer A (2006) Novel 6-O-acylated vitamin C derivatives as hyaluronidase inhibitors with selectivity for bacterial lyases. Bioorg Med Chem Lett 16: 5313-5316

Xie S-X , Petrache G, Schneider E, Ye Q-Z, Bernhardt G, Seifert R, Buschauer A (2006) Synthesis and pharmacological characterization of novel fluorescent histamine H2-receptor ligands derived from aminopotentidine. Bioorg Med Chem Lett 16: 3886-3890

Schneider E, Mayer M, Ziemek R, Li L, Hutzler C, Bernhardt G, Buschauer A (2006) A Simple and Powerful Flow Cytometric Method for the Simultaneous Determination of Multiple Parameters at G-Protein-coupled Receptor Subtypes. ChemBioChem 7: 1400-1409

Gross D, Bernhardt G, Buschauer A (2006) Platelet-derived growth factor receptor independent proliferation of human glioblastoma cells: selective tyrosine kinase inhibitors lack antiproliferative activity. J Cancer Res Clin Oncol 132: 589-599

Salmen S, Hoechstetter J, Käsbauer C, Paper D H, Bernhardt G, Buschauer A (2005) Sulphated oligosaccharides as inhibitors of hyaluronidases from bovine testis, bee venom and Streptococcus agalactiae. Planta Med 71: 727-732

Botzki A, Salmen S, Bernhardt G, Buschauer A, Dove S (2005) Structure-based design of bacterial hyaluronan lyase inhibitors. QSAR Comb Sci 24: 458-469

Lottner C, Knuechel R, Bernhardt G, Brunner H (2004) Distribution and subcellular localization of a water-soluble hematoporphyrin-platinum(II) complex in human bladder cancer cells. Cancer Lett 215: 167-177

Botzki A, Rigden D J, Braun S, Nukui M, Salmen S, Hoechstetter J, Bernhardt G, Dove S, Buschauer A, Jedrzejas M J (2004) L-ascorbic acid-6-hexadecanoate, a potent hyaluronidase inhibitor: X-ray structure and molecular modeling of enzyme-inhibitor complexes. J Biol Chem 279: 45990-45997

Bernhardt G, Brunner H, Gruber N, Lottner C, Pushpan S K, Tsuno T, Zabel M (2004) Carboplatin derivatives with superior antitumor activity compared to the parent compound. Inorganica Chimica Acta 357: 4452-4466

Gürtler U, Fuchs P, Stangelmayer A, Bernhardt G, Buschauer A, Spruss T (2004) Construction and Validation of a Microprocessor Controlled Extracorporal Circuit in Rats for the Optimization of Isolated Limb Perfusion. Arch Pharm Pharm Med Chem 337: 672-681

Lottner C, Knuechel R, Bernhardt G, Brunner H (2004) Combined chemotherapeutic and photodynamic treatment on human bladder cells by hematoporphyrin-platinum(II) conjugates. Cancer Lett 203: 171-80

Schertl S, Hartmann RW, Batzl-Hartmann C, Bernhardt G, Spruss T, Beckenlehner K, Koch M, Krauser R, Schlemmer R, Gust R, Schonenberger H (2004) [1, 2-Bis(2, 6-difluoro-3-hydroxyphenyl)ethylene-diamine]platinum(II) Complexes, Compounds for the Endocrine Therapy of Breast Cancer - Mode of Action I: Antitumor Activity Due to the Reduction of the Endogenous Estrogen Level. Arch Pharm Pharm Med Chem 337: 335-348

Schertl S, Hartmann RW, Batzl-Hartmann C, Bernhardt G, Spruss T, Beckenlehner K, Koch M, Krauser R, Schlemmer R, Gust R, Schonenberger H (2004) [1, 2-Bis(2, 6-difluoro-3-hydroxyphenyl)ethylene-diamine]platinum(II) Complexes, Compounds for the Endocrine Therapy of Breast Cancer - Mode of Action II: Contribution of Drug Inactivation, Cellular Drug Uptake and Sterical Factors in the Drug-Target Interaction to the Antitumor Activity. Arch Pharm Pharm Med Chem 337:349-59

Dittmar M, Kiourkenidis G, Horn M, Bollwein S, Bernhardt G (2004) Cerebral Ischemia, Matrix Metalloproteinases, and TNF-alpha: MMP Inhibitors May Act Not Exclusively by Reducing MMP Activity. Stroke 35:e338-339

L. Li, J. Kracht, S. Peng, G. Bernhardt, S. Elz, A. Buschauer, Synthesis and pharmacological activity of fluorescent histamine H2 receptor antagonists related to potentidine, Bioorg. Med. Chem. Lett. 13, 1717-1720 (2003).

M. Oettl, J. Hoechstetter, I. Asen, G. Bernhardt, A. Buschauer, Comparative characterization of bovine testicular hyaluronidase and a hyaluronate lyase from Streptococcus agalactiae in pharmaceutical preparations, Eur. J. Pharm. Sci. 18, 267 - 277 (2003).

L. Li, J. Kracht, S. Peng, G. Bernhardt , A. Buschauer, Synthesis and pharmacological activity of fluorescent histamine H1 receptor antagonists related to mepyramine, Bioorg. Med. Chem. Lett. 13, 1245 - 1248 (2003).

Klein M, Zabel M, Bernhardt G, König, B.(2003) Tetrahydroxy 10-membered Cyclic Enediynes. J Org Chem 68: 9379-9383

Li L, Mayer M, Schneider E, Schreiber E, Bernhardt G, Peng S, Buschauer A (2003) Preparation of fluorescent nonpeptidic neuropeptide Y receptor ligands: analogues of the quinazoline-type anti-obesity Y5 antagonist CGP 71683A. Arch Pharm Pharm Med Chem 336: 585-590

T. S. Weiss, G. Bernhardt, A. Buschauer, W. E. Thasler, D. Dolgner, H. Zirngibl, K.-W. Jauch, Polyamine levels of human colorectal adenocarcinomas are correlate with tumor stage and grade, Int. J. Colorectal Dis. 17, 381 - 387 (2002).

S. Fellner, B. Bauer, D. S. Miller, M. Schaffrik, M. Fankhänel, T. Spruß, G. Bernhardt, C. Graeff, L. Färber, H. Gschaidmeier, A. Buschauer and G. Fricker, Transport of paclitaxel (Taxol) across the blood-brain barrier in vitro and in vivo, J. Clin. Invest. 110, 1309 - 1318 (2002).

Weiss T, Bernhardt G, Buschauer A, Jauch KW, Zirngibl H (2002) Erratum to ''High-resolution reversed-phase high-performance liquid chromatography analysis of polyamines and their monoacetyl conjugates by fluorescence detection after derivatization with N-Hydroxysuccinimidyl 6-Quinolinyl carbamate'' [Anal. Biochem. 247 (1997) 294-304] Anal Biochem 311: 100

G. Bernhardt, K. Beckenlehner, T. Spruß, R. Schlemmer, H. Reile, H. Schönenberger, Establishment and characterization of new murine breast cancer cell lines, Arch. Pharm. Med. Chem. 335, 55-68 (2002).

W. Vogelhuber, T. Spruß, G. Bernhardt, A. Buschauer, A. Göpferich, Efficacy of BCNU and paclitaxel loaded subcutaneous implants in the interstitial chemotherapy of U-87 MG human glioblastoma xenografts, Intern. J. Pharmaceutics 238, 111 - 121 (2002).

C. Lottner, K.C. Bart, G. Bernhardt, H. Brunner. Hematoporphyrin-derived soluble porphyrin-platinum conjugates with combined cytotoxic and phototoxic antitumor activity. J. Med. Chem. 45: 2064-2078 (2002).

C. Lottner, K.C. Bart, G. Bernhardt, H. Brunner. Soluble tetraarylporphyrin-platinum conjugates as cytotoxic and phototoxic antitumor agents. J. Med. Chem. 45, 2079-2089 (2002).

R. Schlemmer, T. Spruß, G. Bernhardt, H. Schönenberger, Does [meso-1,2-bis(2,6-dichloro-4-hydroxyphenyl)ethylenediamine]dichloro-platinum(II) act as an immune response modifier? VI. Inhibition of the proliferation-increasing effect of progressively qrowing MXT-M-3,2 breast cancer on phagocytes by the title compound. Arch. Pharm. Med. Chem. 334, 309-317 (2001).

S. Schertl, R.W. Hartmann, C. Batzl-Hartmann, R. Schlemmer, T. Spruss, G. Bernhardt, R. Gust, H. Schönenberger, 1-(2,6-dichloro-4-hydroxyphenyl)-2-phenylethanes new biological response modifiers for the therapy of breast cancer. Synthesis and evaluation of estrogenic/antiestrogenic properties. Arch. Pharm. Med. Chem. 334, 125-37 (2001).

W. Vogelhuber, P. Rutunno, E. Magni, A. Gazzaniga, T. Spruss, G. Bernhardt, A. Buschauer, A. Goepferich, Programmable biodegradable implants, J Control Release, 73, 75-88, (2001)

A. Schuster, C. Götte, G. Bernhardt, A. Buschauer, Chiral separation of pheniramine-like 3-phenyl-3-heteroarylpropylamines by CE and HPLC methods, Chirality 13, 285-93 (2001)

Schlemmer R, Spruß Th, Bernhardt G., Schönenberger H (2000) Does [meso-1,2-bis(2,6-dichloro-4-hydroxyphenyl)ethylenediamine]dichloro-platinum(II) act on the hormone-sensitive, murine breast cancer as a biological response modifier? Part 1. The MXT-M-3,2 breast cancer stimulates the growth of an identical second graft: [meso-1,2-bis(2,6-dichloro-4-hydroxyphenyl)ethylenediamine]­dichloro­platinum(II) in­hibits this process. Arch Pharm Med Chem 333: 69-71

Moser C, Bernhardt G, Michel J, Schwarz H, Buschauer A (2000) Cloning and functional expression of the hNPY Y5 receptor in human endometrial cancer (HEC-1B) cells. Can J Physiol Pharm 78: 134-142

I. Aiglstorfer, I. Hendrich, C. Moser, G. Bernhardt, S. Dove, A. Buschauer, Structure-Activity Relationships of Neuropeptide Y Y₁ Receptor Antagonists Related to BIBP 3226, Bioorg. Med. Chem. Lett. 10, 1597-1600 (2000).

A. Buschauer, G. Bernhardt, S. Dove, NPY-Rezeptoren als Zielstrukturen für neue Arzneistoffe, Pharm. Ztg. 24, 11-18 (2000).

Schlemmer R, Spruß Th, Bernhardt G., Schönenberger H (2000) Does [meso-1,2-bis­(2,6-dichloro-4-hydroxyphenyl)ethylenediamine]dichloro-platinum(II) act on the hor­mone-sensitive, murine breast cancer as a biological response modifier? Part II. Studies on the influence of [meso-1,2-bis­(2,6-dichloro-4-hydroxyphenyl)-ethylene-diamine]dichloroplatinum(II) on the specific immune defense in MXT-M-3,2 breast cancer bearing mice. Arch Pharm Med Chem 333: 397-403

Schlemmer R, Spruß Th, Bernhardt G., Schönenberger H (2000) Does [meso-1,2-bis(2,6-dichloro-4-hydroxyphenyl)ethylenediamine]dichloroplatinum(II) act on the hormone-sensitive, murine breast cancer as a biological response modifier? Part III: Arch Pharm Med Chem 333: 404-414