TY  - JOUR
A1  - Leurs, Ulrike
A1  - Mezo, Gabor
A1  - Öhlschläger, Peter
A1  - Orban, Erika
A1  - Marquard, Andrea
A1  - Manea, Marilena
T1  - Design, synthesis, in vitro stability and cytostatic effect of multifunctional anticancer drug-bioconjugates containing GnRH-III as a targeting moiety
JF  - Peptide Science
N2  - 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.
Y1  - 2012
U6  - http://dx.doi.org/10.1002/bip.21640
SN  - 1097-0282
VL  - 98
IS  - 1
SP  - 1
EP  - 10
PB  - Wiley
CY  - New York, NY
ER  - 
TY  - JOUR
A1  - Lempiäinen, Harri
A1  - Couttet, Philippe
A1  - Bolognani, Federico
A1  - Müller, Arne
A1  - Dubost, Valérie
A1  - Luisier, Raphaëlle
A1  - Rio-Espinola, Alberto del
A1  - Vitry, Veronique
A1  - Unterberger, Elif B.
A1  - Thomson, John P.
A1  - Treindl, Fridolin
A1  - Metzger, Ute
A1  - Wrzodek, Clemens
A1  - Hahne, Florian
A1  - Zollinger, Tulipan
A1  - Brasa, Sarah
A1  - Kalteis, Magdalena
A1  - Marcellin, Magali
A1  - Giudicelli, Fanny
A1  - Braeuning, Albert
A1  - Morawiec, Laurent
A1  - Zamurovic, Natasa
A1  - Längle, Ulrich
A1  - Scheer, Nico
A1  - Schübeler, Dirk
A1  - Goodman, Jay
A1  - Chibout, Salah-Dine
A1  - Marlowe, Jennifer
A1  - Theil, Dietlinde
A1  - Heard, David J.
A1  - Grenet, Olivier
A1  - Zell, Andreas
A1  - Templin, Markus F.
A1  - Meehan, Richard R.
A1  - Wolf, Roland C.
A1  - Elcombe, Clifford R.
A1  - Schwarz, Michael
A1  - Moulin, Pierre
A1  - Terranova, Rémi
A1  - Moggs, Jonathan G.
T1  - Identification of Dlk1-Dio3 imprinted gene cluster non-coding RNAs as novel candidate biomarkers for liver tumor promotion
JF  - Toxicological Sciences
N2  - The molecular events during nongenotoxic carcinogenesis and their temporal order are poorly understood but thought to include long-lasting perturbations of gene expression. Here, we have investigated the temporal sequence of molecular and pathological perturbations at early stages of phenobarbital (PB) mediated liver tumor promotion in vivo. Molecular profiling (mRNA, microRNA [miRNA], DNA methylation, and proteins) of mouse liver during 13 weeks of PB treatment revealed progressive increases in hepatic expression of long noncoding RNAs and miRNAs originating from the Dlk1-Dio3 imprinted gene cluster, a locus that has recently been associated with stem cell pluripotency in mice and various neoplasms in humans. PB induction of the Dlk1-Dio3 cluster noncoding RNA (ncRNA) Meg3 was localized to glutamine synthetase-positive hypertrophic perivenous hepatocytes, sug- gesting a role for β-catenin signaling in the dysregulation of Dlk1-Dio3 ncRNAs. The carcinogenic relevance of Dlk1-Dio3 locus ncRNA induction was further supported by in vivo genetic dependence on constitutive androstane receptor and β-catenin pathways. Our data identify Dlk1-Dio3 ncRNAs as novel candidate early biomarkers for mouse liver tumor promotion and provide new opportunities for assessing the carcinogenic potential of novel compounds.
Y1  - 2012
U6  - http://dx.doi.org/10.1093/toxsci/kfs303
SN  - 1094-2025
VL  - 131
IS  - 2
SP  - 375
EP  - 386
PB  - Oxford University Press
CY  - Oxford
ER  - 
TY  - JOUR
A1  - Lawson, Nathan D.
A1  - Scheer, Nico
A1  - Pham, Van N.
A1  - Kim, Ceol-Hee
A1  - Chitnis, Ajay B.
A1  - Campos-Ortega, José A.
A1  - Weinstein, Brant M.
T1  - Notch signaling is required for arterial-venous differentiation during embryonic vascular development
JF  - Development
Y1  - 2001
SN  - 1477-9129
VL  - 128
IS  - 19
SP  - 3675
EP  - 3683
ER  - 
TY  - PAT
A1  - Lauth, Jakob
A1  - Wolf, Gerhard
A1  - Burkhart, Bernd
T1  - Preparation of alkoxylation products in the presence of mixed hydroxides modified with additives : United States Patent ; patent number 5,741,947 ; date of patent: Apr. 21, 1998 / assignee: BASF Aktiengesellschaft. Inventors: Gerhard Wolf ; Bernd Burkhart ; Guenter Lauth ...
Y1  - 1998
N1  - Barcode: US005741947A ; Volltext über Datenbank: http://www.google.com/patents
PB  - [United States Trademark and Patent Office]
CY  - [Alexandria, VA]
ER  - 
TY  - PAT
A1  - Lauth, Jakob
A1  - Trübenbach, Peter
A1  - Hagemeyer, Alfred
T1  - Monomodal and polymodal catalyst supports and catalysts having narrow pore size distributions and their production : United States Patent ; patent number 5,935,898 ; date of patent: Aug. 10, 1999 / assignee: BASF Aktiengesellschaft. Inventors: Peter Trubenbach ; Alfred Hagemeyer ; Gunter Lauth ...
Y1  - 1999
N1  - Barcode: US005935898A ; Volltext über Datenbank: http://www.google.com/patents ; Falsche Namensansetzung in Datenbank: Gunter ...
PB  - [United States Patent and Trademark Office]
CY  - [Alexandria, VA]
ER  - 
TY  - JOUR
A1  - Lauth, Jakob
A1  - Solomun, T.
A1  - Hirschwald, W.
A1  - Christmann, K.
T1  - The interaction of carbon monoxide with a ruthenium(1010) surface
JF  - Surface Science. 210 (1989), H. 1-2
Y1  - 1989
SN  - 0039-6028
SP  - 201
EP  - 224
ER  - 
TY  - JOUR
A1  - Lauth, Jakob
A1  - Solomun, T.
A1  - Hirschwald, W.
A1  - Christmann, K.
T1  - The interaction of carbon monoxide with a ruthenium(1010) surface
JF  - Surface Science Letters. 210 (1989), H. 1-2
Y1  - 1989
SN  - 0167-2584
SP  - A74
EP  - A75
ER  - 
TY  - PAT
A1  - Lauth, Jakob
A1  - Müller, Ulrich
A1  - Hoelderich, Wolfgang
T1  - Colored crystalline aluminophosphates and/or silicoaluminophosphates of the AEL or VFI type : United States Patent ; patent number 5,360,474 ; date of patent: Nov. 1, 1994 / assignee: BASF Aktiengesellschaft
Y1  - 1994
N1  - Barcode: US005360474A ; Volltext über Datenbank: http://www.google.com/patents
PB  - [United States Trademark and Patent Office]
CY  - [Alexandria, VA]
ER  - 
TY  - PAT
A1  - Lauth, Jakob
A1  - Müller, Ulrich
A1  - Hoelderich, Wolfgang
T1  - Preparation of aluminophosphates and silicoaluminophosphates having the AEL structure using 1,2-bis-( 4-pyridyl)-ethane : United States Patent ; patent number 5,324,493 ; date of patent: Jun. 28, 1994 / assignee: BASF Aktiengesellschaft. Inventors: Ulrich Mueller ; Wolfgang Hoelderich ; Guenter Lauth
Y1  - 1994
N1  - Barcode: US005324493A ; Volltext über Datenbank: http://www.google.com/patents
PB  - [United States Trademark and Patent Office]
CY  - [Alexandria, VA]
ER  - 
TY  - BOOK
A1  - Lauth, Jakob
A1  - Hoelderich, Wolfgang
A1  - Wagenblast, Gerhard
T1  - Molecular sieves containing azo dyes ; Internationale [Pantent]anmeldung WO93/17965 ; Veröffentlichungsdatum: 16.09.1993  / Anmelder: BASF AG
Y1  - 1993
N1  - Volltext über Datenbank http://depatisnet.dpma.de/
PB  - Weltorganisation für geistiges Eigentum, Internat. Büro
CY  - [Genf]
ER  - 
TY  - PAT
A1  - Lauth, Jakob
A1  - Hoelderich, Wolfgang
A1  - Wagenblast, Gerhard
T1  - Molecular sieves containing azo dyes : United States Patent ; patent number 5,573,585 ; date of patent: Nov. 12, 1996 / assignee: Wolfgang Hoelderich. Inventors: Guenter Lauth ; Wolfgang Hoelderich ; Gerhard Wagenblast ...
Y1  - 1996
N1  - Barcode: US005573585A ; Volltext über Datenbank: http://www.google.com/patents
PB  - [United States Trademark and Patent Office]
CY  - [Alexandria, VA]
ER  - 
TY  - PAT
A1  - Lauth, Jakob
A1  - Hoelderich, Wolfgang
A1  - Harth, Klaus
A1  - Hibst, Hartmuth
T1  - Coated catalysts : United States Patent ; patent number 5,559,065 ; date of patent: Sep. 24, 1996 / assignee: BASF Aktiengesellschaft
Y1  - 1996
N1  - Barcode: US005559065A ; Volltext über Datenbank: http://www.google.com/patents
PB  - [United States Trademark and Patent Office]
CY  - [Alexandria, VA]
ER  - 
TY  - JOUR
A1  - Lauth, Jakob
A1  - Hoelderich, W.
A1  - Wagenblast, G.
T1  - Molecular sieves containing azo dyes
JF  - Zeolites. 15 (1995), H. 2
Y1  - 1995
SN  - 0144-2449
SP  - 184
ER  - 
TY  - JOUR
A1  - Lauth, Jakob
A1  - Hoelderich, W.
A1  - Wagenblast, G.
T1  - Crystalline zeolites containing indigo dyes
JF  - Zeolites. 15 (1995), H. 1
Y1  - 1995
SN  - 0144-2449
SP  - 86
ER  - 
TY  - BOOK
A1  - Lauth, Jakob
A1  - Harreus, Albrecht
A1  - Götz, Norbert
A1  - Rang, Harald [u.a.]
T1  - Preparation O-(2-Hydroxyalkyl)Oximes = of Verfahren zur Herstellung von O-(2-Hydroxy)Oximen : Europäische Patentschrift EP0775107B1 ; Veröffentlichungstag im Patentblatt: 18.11.1999 / Anmelder: BASF AG, 67063 Ludwigshafen. Erfinder: Albrecht Harreus ; Norbert Götz ; Harald Rang ... Günter Lauth
Y1  - 1999
N1  - Volltext über Datenbank: http://publikationen.dpma.de/ ; Text in engl. ; Deutsche Übersetzung unter DE69512786T2 ; Internationale Veröffentlichungsnummer: WO 96/04238
PB  - Europäisches Patentamt
CY  - [München u.a.]
ER  - 
TY  - PAT
A1  - Lauth, Jakob
A1  - Harreus, Albrecht
A1  - Goetz, Norbert
A1  - Rang, Harald
T1  - Preparation of O-(2-hydroxyalkyl) oximes : [South African Patent ] publication number: ZA9506402 ; publication date: 1997-02-03 / applicant: BASF AG.  Inventor: Harreus, Albrecht ; Goetz, Norbert ; Rang, Harald .... Lauth, Guenter ...
Y1  - 1997
N1  - Also published as WO9604238
PB  - [South African Companies and Intellectual Property Registration Office]
CY  - [Pretoria]
ER  - 
TY  - PAT
A1  - Lauth, Jakob
A1  - Hagemeyer, Alfred
A1  - Lautensack, Thomas
A1  - Deimling, Axel
T1  - Catalyst and catalytic oxidative dehydrogenation of alkylaromatics and paraffins : United States Patent ; patent number 5,902,918 ; date of patent: May 11, 1999 / Assignee: BASF Aktiengesellschaft. Inventors: Alfred Hagemeyer ; Gunter Lauth ; Thomas Lautensack ; Axel Deimling
Y1  - 1999
N1  - Barcode: US005902918A ; Volltext über Datenbank: http://www.google.com/patents ; Falsche Namensansetzung: Gunter ...
PB  - United States Trademark and Patent Office
CY  - [Alexandria, VA]
ER  - 
TY  - PAT
A1  - Lauth, Jakob
A1  - Dingerdissen, Uwe
A1  - Trübenbach, Peter
A1  - Steuerle, Ulrich
T1  - Preparation of aziridines : United States Patent ; patent number 5,693,825 ; date of patent: Dec. 2, 1997 / assignee: BASF Aktiengesellschaft. Inventors: Uwe Dingerdissen ; Gunter Lauth ; Peter Trubenbach ; Ulrich Steuerle
Y1  - 1997
N1  - Barcode: US005324493A ; Volltext über Datenbank: http://www.google.com/patents ; Falsche Namensansetzung in Datenbank: Gunter ...
PB  - United States Patent and Trademark Office
CY  - [Alexandria, VA]
ER  - 
TY  - BOOK
A1  - Lauth, Jakob
A1  - Dingerdissen, Uwe
A1  - Steuerle, Ulrich
T1  - Cup catalyst and process for producing aziridines : [Internationale Pantentanmeldung WO9633018] ; Veröffentlichungsdatum: 1996-10-24 / Anmelder: BASF AG ; Dingerdissen, Uwe ; Lauth, Guenther ; Steuerle, Ulrich. Erfinder: Dingerdissen, Uwe ; Lauth, Guenther ; Steuerle, Ulrich
Y1  - 1996
PB  - [Weltorganisation für geistiges Eigentum]
CY  - [Genf]
ER  - 
TY  - PAT
A1  - Lauth, Jakob
A1  - Dingerdissen, Uwe
A1  - Henne, Andreas
T1  - Preparation of amines  : United States Patent ; patent number 5,817,871 ; date of patent: Oct. 6, 1998 / Assignee: BASF Aktiengesellschaft. Inventors: Uwe Dingerdissen ; Gunter Lauth ; Andreas Henne ....
Y1  - 1998
N1  - Barcode: US005817871A ; Volltext über Datenbank: http://www.google.com/patents ; Falsche Namensansetzung: Gunter ...
PB  - [United States Trademark and Patent Office]
CY  - [Alexandria, VA]
ER  -