Giovanni Natile
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View article: Interactions with DNA Models of the Oxaliplatin Analog (cis-1,3-DACH)PtCl2
Interactions with DNA Models of the Oxaliplatin Analog (cis-1,3-DACH)PtCl2 Open
It is generally accepted that adjacent guanine residues in DNA are the primary target for platinum antitumor drugs and that differences in the conformations of the Pt-DNA adducts can play a role in their antitumor activity. In this study, …
View article: Hydrophobic Nanocrystals Coated with an Amphiphilic Polymer Shell: A General Route to Water Soluble Nanocrystals
Hydrophobic Nanocrystals Coated with an Amphiphilic Polymer Shell: A General Route to Water Soluble Nanocrystals Open
A general strategy is described which allows for transferring hydrophobically capped nanocrystals from organic to aqueous solution by\nwrapping an amphiphilic polymer around the particles. In particular, high quality CoPt3, Au, CdSe/ZnS, a…
View article: Cisplatin and zoledronic acid: two drugs combined in a Pt(<scp>ii</scp>) complex with potential antitumor activity towards bone tumors and metastases
Cisplatin and zoledronic acid: two drugs combined in a Pt(<span>ii</span>) complex with potential antitumor activity towards bone tumors and metastases Open
Two drugs already approved by the U.S. Food and Drug Administration and the European Medicinal Agency combined in a dinuclear Pt( ii ) complex.
View article: Crystal Structure of the Human Copper Chaperone ATOX1 Bound to Zinc Ion
Crystal Structure of the Human Copper Chaperone ATOX1 Bound to Zinc Ion Open
The bioavailability of copper (Cu) in human cells may depend on a complex interplay with zinc (Zn) ions. We investigated the ability of the Zn ion to target the human Cu-chaperone Atox1, a small cytosolic protein capable of anchoring Cu(I)…
View article: Improvement of Kiteplatin Efficacy by a Benzoato Pt(IV) Prodrug Suitable for Oral Administration
Improvement of Kiteplatin Efficacy by a Benzoato Pt(IV) Prodrug Suitable for Oral Administration Open
Kiteplatin, [PtCl2(cis-1,4-DACH)] (DACH = diaminocyclohexane), contains an isomeric form of the oxaliplatin diamine ligand trans-1R,2R-DACH and has been proposed as a valuable drug candidate against cisplatin- and oxaliplatin-resistant tum…
View article: Multinuclear Metal-Binding Ability of the N-Terminal Region of Human Copper Transporter Ctr1: Dependence Upon pH and Metal Oxidation State
Multinuclear Metal-Binding Ability of the N-Terminal Region of Human Copper Transporter Ctr1: Dependence Upon pH and Metal Oxidation State Open
The 14mer peptide corresponding to the N-terminal region of human copper transporter Ctr1 was used to investigate the intricate mechanism of metal binding to this plasma membrane permease responsible for copper import in eukaryotic cells. …
View article: <sup>19</sup>F NMR Allows the Investigation of the Fate of Platinum(IV) Prodrugs in Physiological Conditions
<sup>19</sup>F NMR Allows the Investigation of the Fate of Platinum(IV) Prodrugs in Physiological Conditions Open
Pt IV prodrugs can overcome resistance and side effects of conventional Pt II anticancer therapies. By 19 F‐labeling of a Pt IV prodrug (Pt‐FBA, FBA=p‐fluorobenzoate), the activation under physiological conditions could be investigated. Un…
View article: New Oxaliplatin-Pyrophosphato Analogs with Improved In Vitro Cytotoxicity
New Oxaliplatin-Pyrophosphato Analogs with Improved In Vitro Cytotoxicity Open
Two new Pt(II)-pyrophosphato complexes containing the carrier ligands cis-1,3-diaminocyclohexane (cis-1,3-DACH) and trans-1,2-diamine-4-cyclohexene (1,2-DACHEX), variants of the 1R,2R-diaminocyclohexane ligand present in the clinically use…
View article: Platinum(IV) Complexes of trans-1,2-diamino-4-cyclohexene: Prodrugs Affording an Oxaliplatin Analogue that Overcomes Cancer Resistance
Platinum(IV) Complexes of trans-1,2-diamino-4-cyclohexene: Prodrugs Affording an Oxaliplatin Analogue that Overcomes Cancer Resistance Open
Six platinum(IV) compounds derived from an oxaliplatin analogue containing the unsaturated cyclic diamine trans-1,2-diamino-4-cyclohexene (DACHEX), in place of the 1,2-diaminocyclohexane, and a range of axial ligands, were synthesized and …
View article: CCDC 1960672: Experimental Crystal Structure Determination
CCDC 1960672: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
CCDC 933014: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
CCDC 933015: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Oxidation of Human Copper Chaperone Atox1 and Disulfide Bond Cleavage by Cisplatin and Glutathione
Oxidation of Human Copper Chaperone Atox1 and Disulfide Bond Cleavage by Cisplatin and Glutathione Open
Cancer cells cope with high oxidative stress levels, characterized by a shift toward the oxidized form (GSSG) of glutathione (GSH) in the redox couple GSSG/2GSH. Under these conditions, the cytosolic copper chaperone Atox1, which delivers …
View article: Mechanistic and Structural Basis for Inhibition of Copper Trafficking by Platinum Anticancer Drugs
Mechanistic and Structural Basis for Inhibition of Copper Trafficking by Platinum Anticancer Drugs Open
Copper (Cu) is required for maturation of cuproenzymes, cell proliferation, and angiogenesis, and its transport entails highly specific protein-protein interactions. In humans, the Cu chaperone Atox1 mediates Cu(I) delivery to P-type ATPas…
View article: A minimal structural variation can overcome tumour resistance of oxaliplatin: the case of 4,5-dehydrogenation of the cyclohexane ring
A minimal structural variation can overcome tumour resistance of oxaliplatin: the case of 4,5-dehydrogenation of the cyclohexane ring Open
A new family of anticancer compounds has been derived from oxaliplatin by inserting a double-bond between carbons 4 and 5 of the 1,2-diaminocyclohexane ring.
View article: Cytotoxic phenanthroline derivatives alter metallostasis and redox homeostasis in neuroblastoma cells
Cytotoxic phenanthroline derivatives alter metallostasis and redox homeostasis in neuroblastoma cells Open
Copper homeostasis is generally investigated focusing on a single component of the metallostasis network. Here we address several of the factors controlling the metallostasis for neuroblastoma cells (SH-SY5Y) upon treatment with 2,9-dimeth…
View article: Effect of<i>in vivo</i>post-translational modifications of the HMGB1 protein upon binding to platinated DNA: a molecular simulation study
Effect of<i>in vivo</i>post-translational modifications of the HMGB1 protein upon binding to platinated DNA: a molecular simulation study Open
Cisplatin is one of the most widely used anticancer drugs. Its efficiency is unfortunately severely hampered by resistance. The High Mobility Group Box (HMGB) proteins may sensitize tumor cells to cisplatin by specifically binding to plati…
Multi-Acting Mitochondria-Targeted Platinum(IV) Prodrugs of Kiteplatin with α-Lipoic Acid in the Axial Positions Open
Platinum(II) drugs are activated intracellularly by aquation of the leaving groups and then bind to DNA, forming DNA adducts capable to activate various signal-transduction pathways. Mostly explored in recent years are Pt(IV) complexes whi…
Translocator Protein (TSPO) Open
The high number of papers submitted and ultimately accepted for publication in this special issue attests the great amount of research being conducted on TSPO and its role in living cells. Thus, TSPO has become an extremely attractive subc…
Dual-acting antitumor Pt(<span>iv</span>) prodrugs of kiteplatin with dichloroacetate axial ligands Open
DNA and mitochondria of tumor cells are the targets of Pt(iv) complexes of kiteplatin with biologically active dichloroacetate as axial ligands.
An Updated View of Translocator Protein (TSPO) Open
Decades of study on the role of mitochondria in living cells have evidenced the importance of the 18 kDa mitochondrial translocator protein (TSPO), first discovered in the 1977 as an alternative binding site for the benzodiazepine diazepam…
Novel Antitumor Platinum(II) Conjugates Containing the Nonsteroidal Anti-inflammatory Agent Diclofenac: Synthesis and Dual Mechanisms of Antiproliferative Effects Open
One concept how to improve anticancer effects of conventional metallodrugs consists in conjugation of these compounds with other biologically (antitumor) active agents, acting by a different mechanism. Here, we present synthesis, biologica…
Anticancer kiteplatin pyrophosphate derivatives show unexpected target selectivity for DNA Open
This study demonstrates that unexpectedly DNA appears to be an important target of the biological activity of new anticancer derivatives of kiteplatin with a pyrophosphate carrier ligand.
CCDC 1507593: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
Synthesis, Characterization, and Cytotoxicity of the First Oxaliplatin Pt(IV) Derivative Having a TSPO Ligand in the Axial Position Open
The first Pt(IV) derivative of oxaliplatin carrying a ligand for TSPO (the 18-kDa mitochondrial translocator protein) has been developed. The expression of the translocator protein in the brain and liver of healthy humans is usually low, o…
Hydroxyapatite nanocrystals as a smart, pH sensitive, delivery system for kiteplatin Open
Synthetic hydroxyapatite nanocrystals are proposed as a pH-sensitive carrier capable to release an antitumor platinum-drug selectively at the tumor site.