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Angela Casini

Cette personne n’est plus à l’EPFL

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Publications associées (43)

Organometallic antitumour agents with alternative modes of action

Paul Joseph Dyson, Christian Hartinger, Alexey Nazarov, Angela Casini

The therapeutic index of drugs that target DNA, a ubiquitous target present in nearly all cells, is low. Nevertheless, DNA has remained the primary target for medicinal chemists developing metal-based anticancer drugs, although DNA has been essentially aba ...

2010

Molecular Mechanisms and Proposed Targets for Selected Anticancer Gold Compounds

Angela Casini

Nowadays, gold compounds constitute a family of very promising experimental agents for cancer treatment. Indeed, several gold(I) and gold(III) compounds were shown to manifest outstanding antiproliferative properties in vitro against selected human tumor c ...

2010

Reactivity of anticancer metallodrugs with serum proteins: New insights from size exclusion chromatography-ICP-MS and ESI-MS

Paul Joseph Dyson, Angela Casini, Michael Groessl

A method based on the coupling of high resolution size-exclusion liquid chromatography using a polymer stationary phase with inductively coupled plasma mass spectrometry was developed to study the interactions of two metallodrugs - cisplatin and RAPTA-T - ...

Royal Society of Chemistry2010

1) Trace copper(II) or zinc(II) ions drastically modify the aggregation behaviour of Aβ1–42: an AFM study

Angela Casini, Andrea Innocenti Malini

Formation of amyloid-beta (A beta)(1-42) amyloid fibrils, a characteristic feature of Alzheimer's disease (AD), was monitored in situ through atomic force microscopy (AFM). Well-structured amyloid fibrils slowly formed in solution within 24 hours for which ...

2010

Rationalization of the inhibition activity of structurally related organometallic compounds against the drug target cathepsin B by DFT

Paul Joseph Dyson, Angela Casini, Fabio Edafe

A series of organometallic compds. of general formula [(arene)M(PTA)nXm]Y (arene = η6-C10H14, η-C5Me5); (M = Ru(II), Os(II), Rh(III) and Ir(III); X = Cl, mPTA; Y = OTf, PF6) have been screened for their cytotoxicity and ability to inhibit cathepsin B in vi ...

Royal Society of Chemistry2010

Antiproliferative Activity of Gold(I) Alkyne Complexes Containing Water-Soluble Phosphane Ligands

Paul Joseph Dyson, Angela Casini, Olivier Pierre Zava, elena vergara

A series of mono-, di-, and trinuclear organometallic alkynyl phosphane gold(I) complexes contg. the stable and water-sol. PTA and DAPTA ligands have been synthesized and characterized. The solid-state structure of one of these compds. was also established ...

American Chemical Society2010

Next-Generation Anticancer Metallodrugs

Angela Casini

More than 99% of currently approved clinical drugs are organic compounds. In contrast, the percentage of metal-containing drugs (metallodrugs) is very low. In cancer chemotherapy, however, platinum coordination compounds represented by cisplatin and deriva ...

2010

The X-ray Structure of the Adduct between NAMI-A and Carbonic Anhydrase Provides Insights into the Reactivity of this Metallodrug with Proteins

Angela Casini

2010

Cytotoxic profile and peculiar reactivity with biomolecules of a novel “rule-breaker” iodo-platinum(II) complex

Angela Casini

Novel and surprising biological properties were disclosed for the platinum(II) complex cis-diiodidodiisopropylamineplatinum(II). Remarkably this new platinum(II) complex manifests pronounced antiproliferative properties in vitro, in some cases superior to ...

2010

[Au2(phen2Me)2(μ-O)2](PF6)2, a novel dinuclear gold(III) complex showing excellent antiproliferative properties

Angela Casini

A novel dioxo-bridged dinuclear gold(III) complex with two 2,9-dimethylphenanthroline ligands was synthesized and thoroughly characterized. Its crystal structure was solved, and its solution behavior assessed. Remarkably, this compound revealed excellent a ...

2010

Proteins as Possible Targets for Cytotoxic trans-Platinum(II) Complexes with Aliphatic Amine Ligands: Further Exceptions to the DNA Paradigm

Paul Joseph Dyson, Angela Casini, Michael Groessl

The reactivity of three cytotoxic trans-PtII complexes bearing aliph. amine ligands, with transferrin and single-stranded oligonucleotides as DNA models, was investigated by ESI-MS and the results obtained are discussed in comparison with cisplatin. Tandem ...

Wiley-Blackwell2010

Trans-cis-cis-[RuCl2(DMSO)(2)(2-amino-5-methyl-thiazole)(2)], (PMRu52), a novel ruthenium(II) compound acting as a strong inhibitor of cathepsin B

Angela Casini

A novel ruthenium(II) compound, trans-cis-cis-[Ru(II)Cl-2(DMSO)(2)(2-amino-5-methyl-thiazole)(2)], (I), PMRu52 hereafter, that may be obtained from the previously described (cis and trans)[Ru(II)Cl-2(DMSO)(4)] complexes, was designed, synthesized and chara ...

2010

Reactivity of an antimetastatic organometallic ruthenium compound with metallothionein-2: relevance to the mechanism of action

Paul Joseph Dyson, Angela Casini

The reaction of metallothionein-2 (MT-2) with the organometallic antitumour compound [Ru(eta(6)-p-cymene)Cl-2(pta)], RAPTA-C, was investigated using ESI MS and ICP AES. The studies were performed in comparison to cisplatin and significant differences in th ...

2009

Thioredoxin reductase: A target for gold compounds acting as potential anticancer drugs

Angela Casini

The thioredoxin system plays a key role in regulating the overall intracellular redox balance. It basically comprises the small redox protein thioredoxin (Trx), nicotinamide adenine dinucleotide phosphate, in its reduced form (NADPH), and thioredoxin reduc ...

2009

Excellent correlation between cathepsin B inhibition and cytotoxicity for a series of palladacycles

Paul Joseph Dyson, Angela Casini, Olivier Pierre Zava

The reaction of the five- or six-membered C,N or C,S-palladacycles [(L)PdCl]2 with PTA (1,3,5-triaza-7-phosphaadamantane) led to the monomeric complexes [(L)Pd(PTA)Cl] 6a, 6b and 7 where LH= N,N-dimethyl-1-phenylmethanamine, benzyl(methyl)sulfane or 1-meth ...

Royal Society of Chemistry2009

Exploring metallodrug-protein interactions by mass spectrometry: comparisons between platinum coordination complexes and an organometallic ruthenium compound

Paul Joseph Dyson, Angela Casini

Electrospray ionisation mass spectrometry was used to analyze the reactions of metal compds. with mixts. of selected proteins. Three representative medicinally relevant compds., cisplatin, transplatin and the organometallic ruthenium compd. RAPTA-C, were r ...

Springer-Verlag2009

Solution Behaviour and Biomolecular Interactions of Two Cytotoxic trans-Platinum(II) Complexes Bearing Aliphatic Amine Ligands

Angela Casini

A novel trans-platinum(II) complex bearing one dimethylamine (dma) and one methylamine (ma) ligand, namely trans-[PtCl2(dma)(ma)], recently synthesised and characterised in our laboratory, displayed relevant antiproliferative properties in vitro, being mor ...

2009

Chemistry, antiproliferative properties, tumor selectivity, and molecular mechanisms of novel gold(III) compounds for cancer treatment: a systematic study

Angela Casini

The antiproliferative properties of a group of 13 structurally diverse gold(III) compounds, including six mononuclear gold(III) complexes, five dinuclear oxo-bridged gold(III) complexes, and two organogold(III) compounds, toward several human tumor cell li ...

Springer-Verlag2009

Emerging Protein Targets for Anticancer Metallodrugs: Inhibition of Thioredoxin Reductase and Cathepsin B by Antitumor Ruthenium(II)-Arene Compounds

Paul Joseph Dyson, Christian Hartinger, Angela Casini

A series of ruthenium(II)-arene (RAPTA) compds. were evaluated for their ability to inhibit thioredoxin reductase (either cytosolic or mitochondrial) and cathepsin B, two possible targets for anticancer metallodrugs. In general, inhibition of the thioredox ...

2008

Gold(III) compounds as anticancer agents: Relevance of gold-protein interactions for their mechanism of action

Paul Joseph Dyson, Christian Hartinger, Angela Casini

Gold(III) compds. constitute an emerging class of biol. active substances, of special interest as potential anticancer agents. During the past decade a no. of structurally diverse gold(III) complexes were reported to be acceptably stable under physiol.-lik ...

2008

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