Petra Heffeter
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View article: ABCC1 promotes GSH-dependent iron transport and resistance to Fe(II) and Cu(II) chelators
ABCC1 promotes GSH-dependent iron transport and resistance to Fe(II) and Cu(II) chelators Open
Therapy resistance is a major challenge in cancer treatment, with multidrug resistance (MDR) being a well-characterized phenomenon wherein cancer cells develop resistance not only to the administered drug but also to structurally diverse c…
View article: The anticancer thiosemicarbazone triapine exerts immune-enhancing activities via immunogenic cell death induction and FAS upregulation
The anticancer thiosemicarbazone triapine exerts immune-enhancing activities via immunogenic cell death induction and FAS upregulation Open
The anticancer thiosemicarbazone Triapine is currently in a phase III clinical trial in combination with radiation therapy and cisplatin. Noteworthy, while radiotherapy induces an immune-activating cell death, so called immunogenic cell de…
View article: Hesperetin Protects from Palmitic-Acid-Induced Lipotoxicity through the Inhibition of Glutaminolysis, mTORC1 Signaling, and Limited Apoptosis
Hesperetin Protects from Palmitic-Acid-Induced Lipotoxicity through the Inhibition of Glutaminolysis, mTORC1 Signaling, and Limited Apoptosis Open
Palmitic acid-induced lipotoxicity contributes to the development of nonalcoholic fatty liver disease (NAFLD). Hesperetin has been reported to alleviate oxidative stress, inflammation, and cell death in NAFLD, while its potential to mitiga…
View article: Comparative Evaluation of Thiol- and Amine-Conjugating Moieties for Endogenous Albumin Binding after Intravenous Administration
Comparative Evaluation of Thiol- and Amine-Conjugating Moieties for Endogenous Albumin Binding after Intravenous Administration Open
Maleimides are widely used in anticancer drug development for linking small-molecule drugs to macromolecules like antibodies or proteins via thiol-Michael addition reactions. Despite their widespread use, even in clinically approved therap…
View article: DNA Methylation and Transcript Variant Analysis of CDKN2A Exon 2 Despite High Sequence Identity with CDKN2B Exon 2
DNA Methylation and Transcript Variant Analysis of CDKN2A Exon 2 Despite High Sequence Identity with CDKN2B Exon 2 Open
The tumor suppressor p16INK4a, encoded by CDKN2A, is frequently inactivated in cancer through genetic or epigenetic mechanisms. While promoter hypermethylation is the most common epigenetic cause, aberrant methylation of CDKN2A exon 2 has …
View article: Site-Selectively Functionalized Albumin with DFO*Maleimide for <sup>89</sup>Zr-Radiolabeling Yields a Metabolically Stable PET Probe that Enables Late Time-Point Tumor Imaging in Mice
Site-Selectively Functionalized Albumin with DFO*Maleimide for <sup>89</sup>Zr-Radiolabeling Yields a Metabolically Stable PET Probe that Enables Late Time-Point Tumor Imaging in Mice Open
Human serum albumin (HSA) is a clinically validated drug carrier that improves drug delivery to tumor tissues. However, clinical imaging strategies are lacking to stratify patients who will benefit from HSA-bound drugs. In this study, we s…
View article: Novel Maleimide Linkers Based on a Piperazine Motif for Strongly Increased Aqueous Solubility
Novel Maleimide Linkers Based on a Piperazine Motif for Strongly Increased Aqueous Solubility Open
Maleimides remain very popular conjugation moieties in the fields of bio(in)organic chemistry and biotechnology. They are particularly interesting for endogenous albumin binding in the bloodstream to exploit the enhanced permeability and r…
View article: Exploring the Structure–Activity Relationships of Albumin-Targeted Picoplatin-Based Platinum(IV) Prodrugs
Exploring the Structure–Activity Relationships of Albumin-Targeted Picoplatin-Based Platinum(IV) Prodrugs Open
Platinum(II) complexes prevail as first-line treatment for many cancers but are associated with serious side effects and resistance development. Picoplatin emerged as a promising alternative to circumvent GSH-induced tumor resistance by in…
View article: Structural variations in the <i>trans</i>-carboxylate/chlorido axis that impact the mode of action of Pt(<scp>ii</scp>) complexes
Structural variations in the <i>trans</i>-carboxylate/chlorido axis that impact the mode of action of Pt(<span>ii</span>) complexes Open
A new half-way type of non-conventional Pt complex with one acetate ( − OCOCH 3 ) and a chlorido, more active than its diacetate counterpart, has a different cellular uptake route and induces cancer cell death via non-DNA-associated mechan…
View article: Exploring the Anticancer Properties of 4‐Phenylthiazole‐Based Ru(II) and Os(II) Metallacycles Featuring 1‐Methylimidazole as <i>N</i>‐Donor Functionality
Exploring the Anticancer Properties of 4‐Phenylthiazole‐Based Ru(II) and Os(II) Metallacycles Featuring 1‐Methylimidazole as <i>N</i>‐Donor Functionality Open
Ten organometallic complexes of the general formula [M( p ‐cymene)thi CΛN MeIm]NO 3 (M = Ru, Os; MeIm = 1‐methylimidazole, thi = 4‐phenylthiazole) differing in their substituents on the 4‐phenylthiazole scaffold were prepared and character…
View article: A new fluorescent oxaliplatin(<scp>iv</scp>) complex with EGFR-inhibiting properties for the treatment of drug-resistant cancer cells
A new fluorescent oxaliplatin(<span>iv</span>) complex with EGFR-inhibiting properties for the treatment of drug-resistant cancer cells Open
KP2749 is a new anticancer agent that releases two independent cytotoxic agents upon reduction: oxaliplatin and the fluorescent EGFR inhibitor KP2187.
View article: Selectivity for TP53 signalling drives the mode of action of a highly potent <i>N</i> , <i>O</i> , <i>O</i> -tridentate naphthoquinone-based organo-ruthenium anticancer drug candidate
Selectivity for TP53 signalling drives the mode of action of a highly potent <i>N</i> , <i>O</i> , <i>O</i> -tridentate naphthoquinone-based organo-ruthenium anticancer drug candidate Open
The mode of action of an N , O , O -tridentate organoruthenium complex based on a naphthoquinone backbone is found to selectively impact on the TP53-DDX3X-p21 signalling axis, which also explains its tumour inhibition in vivo .
View article: Albumin-targeted oxaliplatin(<scp>iv</scp>) prodrugs bearing STING agonists
Albumin-targeted oxaliplatin(<span>iv</span>) prodrugs bearing STING agonists Open
An oxaliplatin( iv )-maleimide prodrug containing the STING agonist MSA-2 was synthesized with improved pharmacological properties and diminished hematotoxicity. The complex exerted anticancer effects but did not outperform free oxaliplati…
View article: Opposing effects of mycotoxins alternariol and deoxynivalenol on the immunomodulatory effects of oxaliplatin and triapine
Opposing effects of mycotoxins alternariol and deoxynivalenol on the immunomodulatory effects of oxaliplatin and triapine Open
Mycotoxin occurrence in food worldwide is estimated to increase due to climate change. Moreover, studies on how these food contaminants interfere with medications and especially anticancer therapies are rare. With the rise of anticancer im…
View article: When Metal Complexes Evolve, and a Minor Species is the Most Active: the Case of Bis(Phenanthroline)Copper in the Catalysis of Glutathione Oxidation and Hydroxyl Radical Generation
When Metal Complexes Evolve, and a Minor Species is the Most Active: the Case of Bis(Phenanthroline)Copper in the Catalysis of Glutathione Oxidation and Hydroxyl Radical Generation Open
Several copper‐ligands, including 1,10‐phenanthroline (Phen), have been investigated for anticancer purposes based on their capacity to bind excess copper (Cu) in cancer tissues and form redox active complexes able to catalyse the formatio…
View article: When metal complexes evolve, and a minor species is the most active: the case of bis(phenanthroline)copper in the catalysis of glutathione oxidation and hydroxyl radical generation
When metal complexes evolve, and a minor species is the most active: the case of bis(phenanthroline)copper in the catalysis of glutathione oxidation and hydroxyl radical generation Open
Several copper-ligands, including 1,10-phenanthroline (Phen), have been investigated for anticancer purposes based on their capacity to bind excess Cu in cancer tissues and form redox active complexes able to catalyse the formation of reac…
View article: Competition with glutathione explains the impact of lysosomal pH on the pro-oxidant and anticancer activity of the copper-phenanthroline complex
Competition with glutathione explains the impact of lysosomal pH on the pro-oxidant and anticancer activity of the copper-phenanthroline complex Open
Several Cu-ligands, including 1,10-phenanthroline (Phen), have been investigated for anticancer purposes based on their capacity to bind excess Cu in cancer tissues and form redox active complexes able to catalyse the formation of reactive…
View article: Elevated PINK1/Parkin-Dependent Mitophagy and Boosted Mitochondrial Function Mediate Protection of HepG2 Cells from Excess Palmitic Acid by Hesperetin
Elevated PINK1/Parkin-Dependent Mitophagy and Boosted Mitochondrial Function Mediate Protection of HepG2 Cells from Excess Palmitic Acid by Hesperetin Open
Deregulation of mitochondrial functions in hepatocytes contributes to many liver diseases, such as nonalcoholic fatty liver disease (NAFLD). Lately, it was referred to as MAFLD (metabolism-associated fatty liver disease). Hesperetin (Hst),…
View article: Targeting PHGDH reverses the immunosuppressive phenotype of tumor-associated macrophages through α-ketoglutarate and mTORC1 signaling
Targeting PHGDH reverses the immunosuppressive phenotype of tumor-associated macrophages through α-ketoglutarate and mTORC1 signaling Open
View article: Paraptotic Cell Death as an Unprecedented Mode of Action Observed for New Bipyridine-Silver(I) Compounds Bearing Phosphane Coligands
Paraptotic Cell Death as an Unprecedented Mode of Action Observed for New Bipyridine-Silver(I) Compounds Bearing Phosphane Coligands Open
In this work, we investigated the anticancer activity of several novel silver(I) 2,2'-bipyridine complexes containing either triphenylphosphane (PPh3) or 1,2-bis(diphenylphosphino)ethane (dppe) ligands. All compounds were charac…
View article: Synthesis and preclinical evaluation of BOLD-100 radiolabeled with ruthenium-97 and ruthenium-103
Synthesis and preclinical evaluation of BOLD-100 radiolabeled with ruthenium-97 and ruthenium-103 Open
Radiolabeling of the chemotherapeutic agent BOLD-100 with ruthenium-103 enables animal experiments with lower amounts of injected drug. This leads to a relatively higher tumor uptake and promising tumor-to-background ratio for future imagi…
View article: Stepwise optimization of tumor-targeted dual-action platinum(<scp>iv</scp>)-gemcitabine prodrugs
Stepwise optimization of tumor-targeted dual-action platinum(<span>iv</span>)-gemcitabine prodrugs Open
An albumin-binding cisplatin( iv )-gemcitabine complex was step-by-step improved based on stability, reduction, albumin-binding and in vivo data yielding a carboplatin( iv ) complex with distinctly improved overall survival and anticancer …
View article: Synthesis and Preclinical Evaluation of Radiolabeled [103Ru]BOLD-100
Synthesis and Preclinical Evaluation of Radiolabeled [103Ru]BOLD-100 Open
The first-in-class ruthenium-based chemotherapeutic agent BOLD-100 (formerly IT-139, NKP-1339, KP1339) is currently the subject of clinical evaluation for the treatment of gastric, pancreatic, colorectal and bile duct cancer. A radiolabele…
View article: Detection of oxaliplatin- and cisplatin-DNA lesions requires different global genome repair mechanisms that affect their clinical efficacy
Detection of oxaliplatin- and cisplatin-DNA lesions requires different global genome repair mechanisms that affect their clinical efficacy Open
The therapeutic efficacy of cisplatin and oxaliplatin depends on the balance between the DNA damage induction and the DNA damage response of tumor cells. Based on clinical evidence, oxaliplatin is administered to cisplatin-unresponsive can…
View article: The Lipid Metabolism as Target and Modulator of BOLD‐100 Anticancer Activity: Crosstalk with Histone Acetylation
The Lipid Metabolism as Target and Modulator of BOLD‐100 Anticancer Activity: Crosstalk with Histone Acetylation Open
The leading first‐in‐class ruthenium‐complex BOLD‐100 currently undergoes clinical phase‐II anticancer evaluation. Recently, BOLD‐100 is identified as anti‐Warburg compound. The present study shows that also deregulated lipid metabolism pa…
View article: Targeting YB-1 via entinostat enhances cisplatin sensitivity of pleural mesothelioma in vitro and in vivo
Targeting YB-1 via entinostat enhances cisplatin sensitivity of pleural mesothelioma in vitro and in vivo Open
Pleural mesothelioma (PM) is characterized by poor prognosis and limited therapeutic options. Y-box-binding protein 1 (YB-1) was shown to drive growth and migration of PM cells. Here, we evaluated the effect of genetic and pharmacological …
View article: Carboplatin-induced upregulation of pan β-tubulin and class III β-tubulin is implicated in acquired resistance and cross-resistance of ovarian cancer
Carboplatin-induced upregulation of pan β-tubulin and class III β-tubulin is implicated in acquired resistance and cross-resistance of ovarian cancer Open
View article: Insertion of (Bioactive) Equatorial Ligands into Platinum(IV) Complexes
Insertion of (Bioactive) Equatorial Ligands into Platinum(IV) Complexes Open
Platinum(IV) prodrugs are highly interesting alternatives to platinum(II) anticancer therapeutics due to their increased tumor selectivity and reduced side effects. In contrast to the established theory, we recently observed that the equat…
View article: Einbau von (Bioaktiven) Äquatorialen Liganden in Platin(IV)‐Komplexe
Einbau von (Bioaktiven) Äquatorialen Liganden in Platin(IV)‐Komplexe Open
Platin(IV)‐Prodrugs sind aufgrund ihrer erhöhten Tumorselektivität und geringeren Nebenwirkungen äußerst interessante Alternativen zu Platin(II)‐Antitumortherapeutika. Im Gegensatz zur gängigen Theorie haben wir kürzlich beobachtet, dass ä…
View article: Human serum albumin as a copper source for anticancer thiosemicarbazones
Human serum albumin as a copper source for anticancer thiosemicarbazones Open
Thiosemicarbazones (TSCs) are a class of biologically active compounds with promising anticancer activity. Their typical mechanism, especially of the clinically far developed representative Triapine, is chelation of iron (Fe), with the Fe-…