@article{LeursMezoOehlschlaegeretal.2012, author = {Leurs, Ulrike and Mezo, Gabor and {\"O}hlschl{\"a}ger, Peter and Orban, Erika and Marquard, Andrea and Manea, Marilena}, title = {Design, synthesis, in vitro stability and cytostatic effect of multifunctional anticancer drug-bioconjugates containing GnRH-III as a targeting moiety}, series = {Peptide Science}, volume = {98}, journal = {Peptide Science}, number = {1}, publisher = {Wiley}, address = {New York, NY}, issn = {1097-0282}, doi = {10.1002/bip.21640}, pages = {1 -- 10}, year = {2012}, abstract = {Bioconjugates containing the GnRH-III hormone decapeptide as a targeting moiety are able to deliver chemotherapeutic agents specifically to cancer cells expressing GnRH receptors, thereby increasing their local efficacy while limiting the peripheral toxicity. However, the number of GnRH receptors on cancer cells is limited and they desensitize under continuous hormone treatment. A possible approach to increase the receptor mediated tumor targeting and consequently the cytostatic effect of the bioconjugates would be the attachment of more than one chemotherapeutic agent to one GnRH-III molecule. Here we report on the design, synthesis and biochemical characterization of multifunctional bioconjugates containing GnRH-III as a targeting moiety and daunorubicin as a chemotherapeutic agent. Two different drug design approaches were pursued. The first one was based on the bifunctional [4Lys]-GnRH-III (Glp-His-Trp-Lys-His-Asp-Trp-Lys-Pro-Gly-NH2) containing two lysine residues in positions 4 and 8, whose ϵ-amino groups were used for the coupling of daunorubicin. In the second drug design, the native GnRH-III (Glp-His-Trp-Ser-His-Asp-Trp-Lys-Pro-Gly-NH2) was used as a scaffold; an additional lysine residue was coupled to the ϵ-amino group of 8Lys in order to generate two free amino groups available for conjugation of daunorubicin. The in vitro stability/degradation of all synthesized compounds was investigated in human serum, as well as in the presence of rat liver lysosomal homogenate. Their cellular uptake was determined on human breast cancer cells and the cytostatic effect was evaluated on human breast, colon and prostate cancer cell lines. Compared with a monofunctional compound, both drug design approaches resulted in multifunctional bioconjugates with increased cytostatic effect.}, language = {en} } @article{ManeaLeursOrbanetal.2011, author = {Manea, Marilena and Leurs, Ulrike and Orban, Erika and Baranyai, Zsuzsa and {\"O}hlschl{\"a}ger, Peter and Marquardt, Andreas and Schulcz, Akos and Tejeda, Miguel}, title = {Enhanced Enzymatic Stability and Antitumor Activity of Daunorubicin-GnRH-III Bioconjugates Modified in Position 4}, series = {Bioconjugate Chemistry}, volume = {22}, journal = {Bioconjugate Chemistry}, number = {7}, publisher = {ACS}, address = {Washington, DC}, isbn = {1520-4812}, pages = {1320 -- 1329}, year = {2011}, language = {en} } @article{SpiessWilfriedAlvarezetal.2011, author = {Spiess, Elmar and Wilfried, Reichardt and Alvarez, Gerardo and Gottrup, Marcus and {\"O}hlschl{\"a}ger, Peter}, title = {An Artificial PAP Gene Breaks Self-tolerance and Promotes Tumor Regression in the TRAMP Model for Prostate Carcinoma}, series = {Molecular Therapy}, volume = {20}, journal = {Molecular Therapy}, number = {3}, publisher = {Elsevier}, address = {Amsterdam}, isbn = {1525-0016}, pages = {555 -- 564}, year = {2011}, language = {en} } @article{SchiffelsPinkenburgScheldenetal.2013, author = {Schiffels, Johannes and Pinkenburg, Olaf and Schelden, Maximilian and Aboulnaga, El-Hussiny A. A. and Baumann, Marcus and Selmer, Thorsten}, title = {An innovative cloning platform enables large-scale production and maturation of an oxygen-tolerant [NiFe]-hydrogenase from cupriavidus necator in Escherichia coli}, series = {PLOS one. 2013}, journal = {PLOS one. 2013}, publisher = {Public Library of Science}, address = {San Francisco, California}, issn = {1932-6203}, doi = {10.1371/journal.pone.0068812}, year = {2013}, language = {en} } @article{KotterLoveraRiekert1976, author = {Kotter, Michael and Lovera, P. and Riekert, L.}, title = {Charakterisierung eines Tr{\"a}gerkatalysators durch effektive Diffusionskoeffizienten, Labyrinthfaktor und mittlere Porenradien}, series = {Berichte der Bunsen-Gesellschaft f{\"u}r Physikalische Chemie}, volume = {80}, journal = {Berichte der Bunsen-Gesellschaft f{\"u}r Physikalische Chemie}, number = {1}, publisher = {Wiley-VCH}, address = {Weinheim}, isbn = {0005-9021}, doi = {10.1002/bbpc.19760800112}, pages = {61 -- 66}, year = {1976}, abstract = {Der effektive Diffusionskoeffizient Deff von Gasen in einem por{\"o}sen Medium h{\"a}ngt im Knudsen- bzw. {\"U}bergangsgebiet vom effektiven Porenradius 〈r〉 der Struktur ab. 〈r〉 kann aus Deff ermittelt werden, sofern der Labyrinthfaktor χ der Struktur aus der Kinetik des Stoffaustausches in den mit einer fl{\"u}ssigen Phase gef{\"u}llten Poren separat bestimmt wird. An einem Tr{\"a}gerkatalysator (CuO auf γ-Al₂O₃) ergab sich auf diese Weise ein f{\"u}r die Diffusion maßgebender effektiver Porenradius, der in den Bereich der Makroporen f{\"a}llt. Ein Vergleich mit dem aus reaktionskinetischen Daten ermittelten effektiven Diffusionskoeffizienten l{\"a}ßt auf eine ungleichm{\"a}ßige Verteilung der aktiven Komponente im Kontaktkorn schließen.}, language = {de} } @article{KotterHammon1986, author = {Kotter, Michael and Hammon, U.}, title = {Preparation of pellets with well-defined pore structure / U. Hammon ; A. Kotter}, series = {International chemical engineering. 26 (1986), H. 4}, journal = {International chemical engineering. 26 (1986), H. 4}, isbn = {0020-6318}, pages = {563 -- 573}, year = {1986}, language = {en} } @article{Elbers1993, author = {Elbers, Gereon}, title = {Messung von Ruß in der Außenluft - Praktische Erfahrungen und Meßergebnisse aus NRW}, series = {Aktuelle Aufgaben der Messtechnik in der Luftreinhaltung : Kolloquium Heidelberg, 2. bis 4. Juni 1993 / Kommission Reinhaltung der Luft im VDI und DIN}, journal = {Aktuelle Aufgaben der Messtechnik in der Luftreinhaltung : Kolloquium Heidelberg, 2. bis 4. Juni 1993 / Kommission Reinhaltung der Luft im VDI und DIN}, publisher = {VDI-Verl.}, address = {D{\"u}sseldorf}, isbn = {3-18-091059-3}, pages = {337}, year = {1993}, language = {de} } @article{ElbersPfefferFrieseletal.1993, author = {Elbers, Gereon and Pfeffer, H.-U. and Friesel, J. and Beier, R.}, title = {Pilotuntersuchungen gem{\"a}ß dem Verordnungsentwurf nach \S 40, Abs. 2 des Bundesimmissionsschutzgesetzes / H.-U. Pfeffer, J. Friesel, G. Elbers, R. Beier, K. Ellermann}, series = {Drei Jahrzehnte Luftqualit{\"a}ts{\"u}berwachung : Vortr{\"a}ge und Berichte zum Kolloquium "Drei Jahrzehnte Luftqualit{\"a}ts{\"u}berwachung - Bilanz und Perspektiven" am 11. November 1993 in Essen / [Hrsg.: Landesanstalt f{\"u}r Immissionsschutz Nordrhein-Westfalen. Red. Bearb.: Robert Niesenhaus]}, journal = {Drei Jahrzehnte Luftqualit{\"a}ts{\"u}berwachung : Vortr{\"a}ge und Berichte zum Kolloquium "Drei Jahrzehnte Luftqualit{\"a}ts{\"u}berwachung - Bilanz und Perspektiven" am 11. November 1993 in Essen / [Hrsg.: Landesanstalt f{\"u}r Immissionsschutz Nordrhein-Westfalen. Red. Bearb.: Robert Niesenhaus]}, address = {Essen}, pages = {117}, year = {1993}, language = {de} } @article{ElbersRichter1994, author = {Elbers, Gereon and Richter, J.}, title = {Messung kraftfahrzeugbedingter Rußimmissionen}, series = {Staub, Reinhaltung der Luft : air quality control. 54 (1994)}, journal = {Staub, Reinhaltung der Luft : air quality control. 54 (1994)}, isbn = {0039-0771}, pages = {19}, year = {1994}, language = {de} } @article{ElbersBauerBucketal.1994, author = {Elbers, Gereon and Bauer, H. D. and Buck, Manfred and Dahmann, D.}, title = {Rußmessungen am Arbeitsplatz und in der Außenluft - Vergleich zweier Meßmethoden / H.D. Bauer, M. Buck, D. Dahmann, G. Elbers, H.-H. Fricke}, series = {Staub, Reinhaltung der Luft : air quality control. 54 (1994)}, journal = {Staub, Reinhaltung der Luft : air quality control. 54 (1994)}, isbn = {0039-0771}, pages = {55}, year = {1994}, language = {de} }