Literature DB >> 14515995

Bioactivatable, membrane-permeant analogs of cyclic nucleotides as biological tools for growth control of C6 glioma cells.

Martin Bartsch1, Michaela Zorn-Kruppa, Nicole Kühl, Hans-Gottfried Genieser, Frank Schwede, Bernd Jastorff.   

Abstract

In the present study, the cAMP analogs 8-bromo-cAMP (8-Br-cAMP), N6-2'O-dibutyryl-cAMP (DBcAMP) and 8-para-chlorophenylthio-cAMP (8-CPT-cAMP), as well as the corresponding cAMP-acetoxymethyl (AM)-ester-prodrugs were tested in a HPLC study for their membrane permeability, intracellular accumulation and biotransformation. Antiproliferative activities of these compounds were studied in the rat C6 glioma cell line. Chromatographic analysis revealed that the AM-ester analogs of the cyclic nucleotides penetrate quantitatively into rat C6 glioma cells and generate high amounts of their parent cyclic nucleotides intracellularly within 60 min; however, long-term growth inhibition tested in C6 cells is only slightly enhanced with the AM-ester prodrugs of 8-Br-cAMP or DBcAMP.

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Year:  2003        PMID： 14515995     DOI： 10.1515/BC.2003.148

Source DB:  PubMed          Journal:  Biol Chem        ISSN： 1431-6730            Impact factor:   3.915


  14 in total

1.  Biomolecular interaction analysis in functional proteomics.

Authors:  D Moll; A Prinz; F Gesellchen; S Drewianka; B Zimmermann; F W Herberg
Journal:  J Neural Transm (Vienna)       Date:  2006-07-13       Impact factor: 3.575

2.  FRET measurements of intracellular cAMP concentrations and cAMP analog permeability in intact cells.

Authors:  Sebastian Börner; Frank Schwede; Angela Schlipp; Filip Berisha; Davide Calebiro; Martin J Lohse; Viacheslav O Nikolaev
Journal:  Nat Protoc       Date:  2011-03-10       Impact factor: 13.491

3.  Quantification of cAMP and cGMP analogs in intact cells: pitfalls in enzyme immunoassays for cyclic nucleotides.

Authors:  Katharina Werner; Frank Schwede; Hans-Gottfried Genieser; Jörg Geiger; Elke Butt
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2011-06-29       Impact factor: 3.000

Review 4.  Recent advances in the discovery of small molecules targeting exchange proteins directly activated by cAMP (EPAC).

Authors:  Haijun Chen; Christopher Wild; Xiaobin Zhou; Na Ye; Xiaodong Cheng; Jia Zhou
Journal:  J Med Chem       Date:  2013-11-27       Impact factor: 7.446

5.  N4-monobutyryl-cCMP activates PKA RIα and PKA RIIα more potently and with higher efficacy than PKG Iα in vitro but not in vivo.

Authors:  Sabine Wolter; Stefan Dove; Marina Golombek; Frank Schwede; Roland Seifert
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2014-09-06       Impact factor: 3.000

6.  Enhanced Rap1 activation and insulin secretagogue properties of an acetoxymethyl ester of an Epac-selective cyclic AMP analog in rat INS-1 cells: studies with 8-pCPT-2'-O-Me-cAMP-AM.

Authors:  Oleg G Chepurny; Colin A Leech; Grant G Kelley; Igor Dzhura; Elvira Dzhura; Xiangquan Li; Michael J Rindler; Frank Schwede; Hans G Genieser; George G Holz
Journal:  J Biol Chem       Date:  2009-02-25       Impact factor: 5.157

Review 7.  cAMP-Dependent Signaling Pathways as Potential Targets for Inhibition of Plasmodium falciparum Blood Stages.

Authors:  Edwin Lasonder; Kunal More; Shailja Singh; Malak Haidar; Daniela Bertinetti; Eileen J Kennedy; Friedrich W Herberg; Anthony A Holder; Gordon Langsley; Chetan E Chitnis
Journal:  Front Microbiol       Date:  2021-05-24       Impact factor: 5.640

8.  Cyclic AMP induces IPC leukemia cell apoptosis via CRE-and CDK-dependent Bim transcription.

Authors:  S Huseby; G Gausdal; T J Keen; E Kjærland; C Krakstad; L Myhren; K Brønstad; C Kunick; F Schwede; H-G Genieser; R Kleppe; S O Døskeland
Journal:  Cell Death Dis       Date:  2011-12-08       Impact factor: 8.469

9.  The stable cyclic adenosine monophosphate analogue, dibutyryl cyclo-adenosine monophosphate (bucladesine), is active in a model of acute skin inflammation.

Authors:  Chris Rundfeldt; Hartwig Steckel; Torben Sörensen; Piotr Wlaź
Journal:  Arch Dermatol Res       Date:  2012-05       Impact factor: 3.017

10.  Introduction of aromatic ring-containing substituents in cyclic nucleotides is associated with inhibition of toxin uptake by the hepatocyte transporters OATP 1B1 and 1B3.

Authors:  Lars Herfindal; Camilla Krakstad; Lene Myhren; Hanne Hagland; Reidun Kopperud; Knut Teigen; Frank Schwede; Rune Kleppe; Stein Ove Døskeland
Journal:  PLoS One       Date:  2014-04-16       Impact factor: 3.240
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