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  1. AU="Galanski, Mathea S"
  2. AU="Abdelmalek, Fady"
  3. AU="Junkiert, Ukasz"
  4. AU="Nuss, Rachelle"
  5. AU="Hogenkamp, David G"
  6. AU="Song, Weixiao"
  7. AU="Sharma, Siddhanth"
  8. AU="Maheen, Sara"
  9. AU=Weinhard Laetitia
  10. AU="Sun, Mi"
  11. AU="Pospísil, V"
  12. AU=Driscoll David R AU=Driscoll David R
  13. AU="Wojtalewicz, Nathalie"
  14. AU="Waingrow, Marshall"
  15. AU="Daymé Gonzalez Rodriguez"
  16. AU="Lou, Shuyi"
  17. AU="Figueiredo, Rodrigo S"
  18. AU=Fleet James C
  19. AU="Brohawn, David G"
  20. AU="Cho, Chun-Chieh"
  21. AU="van Raalte, Daniël H"
  22. AU="Zargarian, Loussiné"
  23. AU=Hascalovici Jacob
  24. AU="Spagnolo, Jennifer B"
  25. AU="Anderloni, Giulia"
  26. AU="Ahmad, Shoaib"
  27. AU="Du, Roujia"
  28. AU="Colmenero-Repiso, Ana"
  29. AU="Alvarez-Carbonell, David"
  30. AU="Phelippeau, Michael"
  31. AU="Lunghi, Laura"
  32. AU=Giersiepen Klaus
  33. AU="Drobyshev, Sergey"
  34. AU="Timme, Kathleen H"
  35. AU=Sfriso Paolo
  36. AU="Kim, John S"
  37. AU=Farkash Evan A AU=Farkash Evan A
  38. AU="Xia, Xueqian"

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  1. Artikel: Combination of Drug Delivery Properties of PAMAM Dendrimers and Cytotoxicity of Platinum(IV) Complexes-A More Selective Anticancer Treatment?

    Lerchbammer-Kreith, Yvonne / Hejl, Michaela / Vician, Petra / Jakupec, Michael A / Berger, Walter / Galanski, Mathea S / Keppler, Bernhard K

    Pharmaceutics

    2023  Band 15, Heft 5

    Abstract: Based on their drug delivery properties and activity against tumors, we combined PAMAM dendrimers with various platinum(IV) complexes in order to provide an improved approach of anticancer treatment. Platinum(IV) complexes were linked to terminal ... ...

    Abstract Based on their drug delivery properties and activity against tumors, we combined PAMAM dendrimers with various platinum(IV) complexes in order to provide an improved approach of anticancer treatment. Platinum(IV) complexes were linked to terminal NH
    Sprache Englisch
    Erscheinungsdatum 2023-05-17
    Erscheinungsland Switzerland
    Dokumenttyp Journal Article
    ZDB-ID 2527217-2
    ISSN 1999-4923
    ISSN 1999-4923
    DOI 10.3390/pharmaceutics15051515
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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  2. Artikel ; Online: Not the usual suspect - an unexpected organometallic product during the synthesis of cytotoxic platinum(II) complexes.

    Maier, Thomas / Wutschitz, Judith / Gajic, Natalie / Hejl, Michaela / Cseh, Klaudia / Mai, Sebastian / Jakupec, Michael A / Galanski, Mathea S / Keppler, Bernhard K

    Dalton transactions (Cambridge, England : 2003)

    2023  Band 52, Heft 44, Seite(n) 16326–16335

    Abstract: The reaction of ( ... ...

    Abstract The reaction of (1
    Mesh-Begriff(e) Humans ; Platinum/chemistry ; Organoplatinum Compounds/chemistry ; Cell Line, Tumor ; Antineoplastic Agents/chemistry ; DNA ; Drug Screening Assays, Antitumor
    Chemische Substanzen Platinum (49DFR088MY) ; Organoplatinum Compounds ; Antineoplastic Agents ; DNA (9007-49-2)
    Sprache Englisch
    Erscheinungsdatum 2023-11-14
    Erscheinungsland England
    Dokumenttyp Journal Article
    ZDB-ID 1472887-4
    ISSN 1477-9234 ; 1364-5447 ; 0300-9246 ; 1477-9226
    ISSN (online) 1477-9234 ; 1364-5447
    ISSN 0300-9246 ; 1477-9226
    DOI 10.1039/d3dt01736b
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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  3. Artikel: Platinum(IV)-Loaded Degraded Glycol Chitosan as Efficient Platinum(IV) Drug Delivery Platform.

    Lerchbammer-Kreith, Yvonne / Sommerfeld, Nadine S / Cseh, Klaudia / Weng-Jiang, Xian / Odunze, Uchechukwu / Schätzlein, Andreas G / Uchegbu, Ijeoma F / Galanski, Mathea S / Jakupec, Michael A / Keppler, Bernhard K

    Pharmaceutics

    2023  Band 15, Heft 4

    Abstract: A new class of anticancer prodrugs was designed by combining the cytotoxicity of platinum(IV) complexes and the drug carrier properties of glycol chitosan polymers: Unsymmetrically carboxylated platinum(IV) analogues of cisplatin, carboplatin and ... ...

    Abstract A new class of anticancer prodrugs was designed by combining the cytotoxicity of platinum(IV) complexes and the drug carrier properties of glycol chitosan polymers: Unsymmetrically carboxylated platinum(IV) analogues of cisplatin, carboplatin and oxaliplatin, namely (OC-6-44)-acetatodiammine(3-carboxypropanoato)dichloridoplatinum(IV), (OC-6-44)-acetaodiammine(3-carboxypropanoato)(cyclobutane-1,1-dicarboxylato)platinum(IV) and (OC-6-44)-acetato(3-carboxypropanoato)(1R,2R-cyclohexane-1,2-diamine)oxalatoplatinum(IV) were synthesised and conjugated via amide bonding to degraded glycol chitosan (dGC) polymers with different chain lengths (5, 10, 18 kDa). The 15 conjugates were investigated with
    Sprache Englisch
    Erscheinungsdatum 2023-03-24
    Erscheinungsland Switzerland
    Dokumenttyp Journal Article
    ZDB-ID 2527217-2
    ISSN 1999-4923
    ISSN 1999-4923
    DOI 10.3390/pharmaceutics15041050
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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  4. Artikel: Quaternary Ammonium Palmitoyl Glycol Chitosan (GCPQ) Loaded with Platinum-Based Anticancer Agents-A Novel Polymer Formulation for Anticancer Therapy.

    Lerchbammer-Kreith, Yvonne / Hejl, Michaela / Sommerfeld, Nadine S / Weng-Jiang, Xian / Odunze, Uchechukwu / Mellor, Ryan D / Workman, David G / Jakupec, Michael A / Schätzlein, Andreas G / Uchegbu, Ijeoma F / Galanski, Mathea S / Keppler, Bernhard K

    Pharmaceuticals (Basel, Switzerland)

    2023  Band 16, Heft 7

    Abstract: Quaternary ammonium palmitoyl glycol chitosan (GCPQ) has already shown beneficial drug delivery properties and has been studied as a carrier for anticancer agents. Consequently, we synthesised cytotoxic platinum(IV) conjugates of cisplatin, carboplatin ... ...

    Abstract Quaternary ammonium palmitoyl glycol chitosan (GCPQ) has already shown beneficial drug delivery properties and has been studied as a carrier for anticancer agents. Consequently, we synthesised cytotoxic platinum(IV) conjugates of cisplatin, carboplatin and oxaliplatin by coupling via amide bonds to five GCPQ polymers differing in their degree of palmitoylation and quaternisation. The conjugates were characterised by
    Sprache Englisch
    Erscheinungsdatum 2023-07-19
    Erscheinungsland Switzerland
    Dokumenttyp Journal Article
    ZDB-ID 2193542-7
    ISSN 1424-8247
    ISSN 1424-8247
    DOI 10.3390/ph16071027
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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  5. Artikel ; Online: Multifunctional Pt(iv) prodrug candidates featuring the carboplatin core and deferoxamine.

    Harringer, Sophia / Hejl, Michaela / Enyedy, Éva A / Jakupec, Michael A / Galanski, Mathea S / Keppler, Bernhard K / Dyson, Paul J / Varbanov, Hristo P

    Dalton transactions (Cambridge, England : 2003)

    2021  Band 50, Heft 23, Seite(n) 8167–8178

    Abstract: The synergistic combination of the anticancer drug carboplatin and the iron chelator deferoxamine (DFO) served as a foundation for the development of novel multifunctional prodrugs. Hence, five platinum(iv) complexes, featuring the equatorial ... ...

    Abstract The synergistic combination of the anticancer drug carboplatin and the iron chelator deferoxamine (DFO) served as a foundation for the development of novel multifunctional prodrugs. Hence, five platinum(iv) complexes, featuring the equatorial coordination sphere of carboplatin, and one or two DFO units incorporated at axial positions, were synthesized and characterized using ESI-HRMS, multinuclear (
    Mesh-Begriff(e) Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacology ; Carboplatin/chemistry ; Carboplatin/pharmacology ; Cell Proliferation/drug effects ; Cell Survival/drug effects ; Deferoxamine/chemistry ; Deferoxamine/pharmacology ; Drug Screening Assays, Antitumor ; Humans ; Molecular Structure ; Organoplatinum Compounds/chemical synthesis ; Organoplatinum Compounds/chemistry ; Organoplatinum Compounds/pharmacology ; Prodrugs/chemical synthesis ; Prodrugs/chemistry ; Prodrugs/pharmacology ; Tumor Cells, Cultured
    Chemische Substanzen Antineoplastic Agents ; Organoplatinum Compounds ; Prodrugs ; Carboplatin (BG3F62OND5) ; Deferoxamine (J06Y7MXW4D)
    Sprache Englisch
    Erscheinungsdatum 2021-05-25
    Erscheinungsland England
    Dokumenttyp Journal Article
    ZDB-ID 1472887-4
    ISSN 1477-9234 ; 1364-5447 ; 0300-9246 ; 1477-9226
    ISSN (online) 1477-9234 ; 1364-5447
    ISSN 0300-9246 ; 1477-9226
    DOI 10.1039/d1dt00214g
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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  6. Artikel ; Online: The role of the equatorial ligands for the redox behavior, mode of cellular accumulation and cytotoxicity of platinum(IV) prodrugs.

    Göschl, Simone / Varbanov, Hristo P / Theiner, Sarah / Jakupec, Michael A / Galanski, Mathea S / Keppler, Bernhard K

    Journal of inorganic biochemistry

    2016  Band 160, Seite(n) 264–274

    Abstract: The current study aims to elucidate the possible reasons for the significantly different pharmacological behavior of platinum(IV) complexes with cisplatin-, carboplatin- or nedaplatin-like cores and how this difference can be related to their main ... ...

    Abstract The current study aims to elucidate the possible reasons for the significantly different pharmacological behavior of platinum(IV) complexes with cisplatin-, carboplatin- or nedaplatin-like cores and how this difference can be related to their main physicochemical properties. Chlorido-containing complexes are reduced fast (within hours) by ascorbate and are able to unwind plasmid DNA in the presence of ascorbate, while their tri- and tetracarboxylato analogs are generally inert under the same conditions. Comparison of the lipophilicity, cellular accumulation and cytotoxicity of the investigated platinum compounds revealed the necessity to define new structure-property/activity relationships (SPRs and SARs). The higher activity and improved accumulation of platinum(IV) complexes bearing Cl(-) in equatorial position cannot only be attributed to passive diffusion facilitated by their lipophilicity. Therefore, further platinum accumulation experiments under conditions where active/facilitated transport mechanisms are suppressed were performed. Under hypothermic conditions (4°C), accumulation of dichloridoplatinum(IV) complexes is reduced down to 10% of the amount determined at 37°C. These findings suggest the involvement of active and/or facilitated transport in cellular uptake of platinum(IV) complexes with a cisplatin-like core. Studies with ATP depletion mediated by oligomycin and low glucose partially confirmed these observations, but their feasibility was severely limited in the adherent cell culture setting.
    Mesh-Begriff(e) Adenosine Triphosphate/antagonists & inhibitors ; Adenosine Triphosphate/metabolism ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/pharmacology ; Biological Transport ; Carboplatin/chemistry ; Cell Line, Tumor ; Cell Survival/drug effects ; Cisplatin/chemistry ; Cold Temperature ; Coordination Complexes/chemical synthesis ; Coordination Complexes/pharmacology ; Glucose/deficiency ; Glucose/pharmacology ; Hep G2 Cells ; Humans ; Hydrophobic and Hydrophilic Interactions ; Ligands ; Oligomycins/pharmacology ; Organoplatinum Compounds/chemical synthesis ; Organoplatinum Compounds/chemistry ; Organoplatinum Compounds/pharmacology ; Oxidation-Reduction ; Platinum/chemistry ; Prodrugs/chemistry ; Prodrugs/pharmacology ; Structure-Activity Relationship
    Chemische Substanzen Antineoplastic Agents ; Coordination Complexes ; Ligands ; Oligomycins ; Organoplatinum Compounds ; Prodrugs ; Platinum (49DFR088MY) ; Adenosine Triphosphate (8L70Q75FXE) ; nedaplatin (8UQ3W6JXAN) ; Carboplatin (BG3F62OND5) ; Glucose (IY9XDZ35W2) ; Cisplatin (Q20Q21Q62J)
    Sprache Englisch
    Erscheinungsdatum 2016-03-17
    Erscheinungsland United States
    Dokumenttyp Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 162843-4
    ISSN 1873-3344 ; 0162-0134
    ISSN (online) 1873-3344
    ISSN 0162-0134
    DOI 10.1016/j.jinorgbio.2016.03.005
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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  7. Artikel ; Online: The impact of whole human blood on the kinetic inertness of platinum(iv) prodrugs - an HPLC-ICP-MS study.

    Theiner, Sarah / Grabarics, Márkó / Galvez, Luis / Varbanov, Hristo P / Sommerfeld, Nadine S / Galanski, Mathea S / Keppler, Bernhard K / Koellensperger, Gunda

    Dalton transactions (Cambridge, England : 2003)

    2018  Band 47, Heft 15, Seite(n) 5252–5258

    Abstract: The potential advantage of platinum(iv) complexes as alternatives to classical platinum(ii)-based drugs relies on their kinetic stability in the body before reaching the tumor site and on their activation by reduction inside cancer cells. In this study, ... ...

    Abstract The potential advantage of platinum(iv) complexes as alternatives to classical platinum(ii)-based drugs relies on their kinetic stability in the body before reaching the tumor site and on their activation by reduction inside cancer cells. In this study, an analytical workflow has been developed to investigate the reductive biotransformation and kinetic inertness of platinum(iv) prodrugs comprising different ligand coordination spheres (respectively, lipophilicity and redox behavior) in whole human blood. The distribution of platinum(iv) complexes in blood pellets and plasma was determined by inductively coupled plasma-mass spectrometry (ICP-MS) after microwave digestion. An analytical approach based on reversed-phase (RP)-ICP-MS was used to monitor the parent compound and the formation of metabolites using two different extraction procedures. The ligand coordination sphere of the platinum(iv) complexes had a significant impact on their accumulation in red blood cells and on their degree of kinetic inertness in whole human blood. The most lipophilic platinum(iv) compound featuring equatorial chlorido ligands showed a pronounced penetration into blood cells and a rapid reductive biotransformation. In contrast, the more hydrophilic platinum(iv) complexes with a carboplatin- and oxaliplatin-core exerted kinetic inertness on a pharmacologically relevant time scale with notable amounts of the compound accumulated in the plasma fraction.
    Mesh-Begriff(e) Carboplatin/blood ; Carboplatin/pharmacokinetics ; Chromatography, High Pressure Liquid ; Coordination Complexes/blood ; Coordination Complexes/pharmacokinetics ; Humans ; Hydrophobic and Hydrophilic Interactions ; Kinetics ; Ligands ; Nanospheres/chemistry ; Organoplatinum Compounds/blood ; Organoplatinum Compounds/pharmacokinetics ; Oxaliplatin ; Oxidation-Reduction ; Prodrugs/pharmacokinetics
    Chemische Substanzen Coordination Complexes ; Ligands ; Organoplatinum Compounds ; Prodrugs ; Oxaliplatin (04ZR38536J) ; Carboplatin (BG3F62OND5)
    Sprache Englisch
    Erscheinungsdatum 2018-04-11
    Erscheinungsland England
    Dokumenttyp Journal Article
    ZDB-ID 1472887-4
    ISSN 1477-9234 ; 1364-5447 ; 0300-9246 ; 1477-9226
    ISSN (online) 1477-9234 ; 1364-5447
    ISSN 0300-9246 ; 1477-9226
    DOI 10.1039/c7dt04537a
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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  8. Artikel ; Online: Nano-scale imaging of dual stable isotope labeled oxaliplatin in human colon cancer cells reveals the nucleolus as a putative node for therapeutic effect.

    Legin, Anton A / Schintlmeister, Arno / Sommerfeld, Nadine S / Eckhard, Margret / Theiner, Sarah / Reipert, Siegfried / Strohhofer, Daniel / Jakupec, Michael A / Galanski, Mathea S / Wagner, Michael / Keppler, Bernhard K

    Nanoscale advances

    2020  Band 3, Heft 1, Seite(n) 249–262

    Abstract: Oxaliplatin shows a superior clinical activity in colorectal cancer compared to cisplatin. Nevertheless, the knowledge about its cellular distribution and the mechanisms responsible for the different range of oxaliplatin-responsive tumors is far from ... ...

    Abstract Oxaliplatin shows a superior clinical activity in colorectal cancer compared to cisplatin. Nevertheless, the knowledge about its cellular distribution and the mechanisms responsible for the different range of oxaliplatin-responsive tumors is far from complete. In this study, we combined highly sensitive element specific and isotope selective imaging by nanometer-scale secondary ion mass spectrometry (NanoSIMS) with transmission electron microscopy to investigate the subcellular accumulation of oxaliplatin in three human colon cancer cell lines (SW480, HCT116 wt, HCT116 OxR). Oxaliplatin bearing dual stable isotope labeled moieties,
    Sprache Englisch
    Erscheinungsdatum 2020-11-26
    Erscheinungsland England
    Dokumenttyp Journal Article
    ISSN 2516-0230
    ISSN (online) 2516-0230
    DOI 10.1039/d0na00685h
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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  9. Artikel ; Online: Oxaliplatin reacts with DMSO only in the presence of water.

    Varbanov, Hristo P / Ortiz, Daniel / Höfer, Doris / Menin, Laure / Galanski, Mathea S / Keppler, Bernhard K / Dyson, Paul J

    Dalton transactions (Cambridge, England : 2003)

    2017  Band 46, Heft 28, Seite(n) 8929–8932

    Abstract: Herein we show that oxaliplatin reacts rapidly with DMSO in aqueous solutions, despite being stable in pure DMSO and pure water. Furthermore, the reactivity of the clinically applied Pt(ii) drugs in water/DMSO and PBS/DMSO mixtures, and the nature of the ...

    Abstract Herein we show that oxaliplatin reacts rapidly with DMSO in aqueous solutions, despite being stable in pure DMSO and pure water. Furthermore, the reactivity of the clinically applied Pt(ii) drugs in water/DMSO and PBS/DMSO mixtures, and the nature of the species formed were investigated by MS, NMR and RP-HPLC techniques.
    Sprache Englisch
    Erscheinungsdatum 2017-04-21
    Erscheinungsland England
    Dokumenttyp Journal Article
    ZDB-ID 1472887-4
    ISSN 1477-9234 ; 1364-5447 ; 0300-9246 ; 1477-9226
    ISSN (online) 1477-9234 ; 1364-5447
    ISSN 0300-9246 ; 1477-9226
    DOI 10.1039/c7dt01628j
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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  10. Artikel ; Online: Impact of the equatorial coordination sphere on the rate of reduction, lipophilicity and cytotoxic activity of platinum(IV) complexes.

    Höfer, Doris / Varbanov, Hristo P / Hejl, Michaela / Jakupec, Michael A / Roller, Alexander / Galanski, Mathea S / Keppler, Bernhard K

    Journal of inorganic biochemistry

    2017  Band 174, Seite(n) 119–129

    Abstract: The impact of the equatorial coordination sphere on the reduction behavior (i.e. rate of reduction) of platinum(IV) complexes with axial carboxylato ligands was studied. Moreover, the influence of equatorial ligands on the stability, lipophilicity and ... ...

    Abstract The impact of the equatorial coordination sphere on the reduction behavior (i.e. rate of reduction) of platinum(IV) complexes with axial carboxylato ligands was studied. Moreover, the influence of equatorial ligands on the stability, lipophilicity and cytotoxicity of platinum(IV) compounds was evaluated. For this purpose, a series of platinum(IV) complexes featuring axial carboxylato ligands (succinic acid monoesters) was synthesized; anionic carboxylato (OAc
    Mesh-Begriff(e) Cell Line, Tumor ; Cytotoxins/chemical synthesis ; Cytotoxins/chemistry ; Cytotoxins/pharmacokinetics ; Female ; Humans ; Neoplasms/drug therapy ; Neoplasms/metabolism ; Organoplatinum Compounds/chemical synthesis ; Organoplatinum Compounds/chemistry ; Organoplatinum Compounds/pharmacology ; Secretoglobins
    Chemische Substanzen Cytotoxins ; Organoplatinum Compounds ; SCGB1D1 protein, human ; Secretoglobins
    Sprache Englisch
    Erscheinungsdatum 2017-06-16
    Erscheinungsland United States
    Dokumenttyp Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 162843-4
    ISSN 1873-3344 ; 0162-0134
    ISSN (online) 1873-3344
    ISSN 0162-0134
    DOI 10.1016/j.jinorgbio.2017.06.005
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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