Publications de Wee Han Ang | EPFL Graph Search

A structure-based mechanism of cisplatin resistance mediated by glutathione transferase P1-1

Paul Joseph Dyson, Laure Menin, Wee Han Ang

Cisplatin [cis-diamminedichloroplatinum(II) (cis-DDP)] is one of the most successful anticancer agents effective against a wide range of solid tumors. However, its use is restricted by side effects and/or by intrinsic or acquired drug resistance. Here, we ...

National Academy of Sciences2019

Development of an Efficient Dual-Action GST-Inhibiting Anticancer Platinum(IV) Prodrug

Paul Joseph Dyson, Patrycja Nowak-Sliwinska, Wee Han Ang

The cytotoxicity of cisplatin (cDDP) is enhanced when co-administered with ethacrynic acid (EA), a glutathione S-transferase (GST) inhibito r. A Pt-lV EA conjugate containing a cDDP core and two axial ethacrynate ligands (compound 1) was shown to be an ex ...

2018

Ligand substitutions between ruthenium-cymene compounds can control protein versus DNA targeting and anticancer activity

Paul Joseph Dyson, Ursula Röthlisberger, Wee Han Ang, Alexey Nazarov, Pablo Campomanes Ramos, Catherine Marie Amélie Clavel, Michael Groessl

Ruthenium compounds have become promising alternatives to platinum drugs by displaying specific activities against different cancers and favourable toxicity and clearance properties. Nonetheless, their molecular targeting and mechanism of action are poorly ...

Nature Research2014

Phosphorylation of Diaminopyridines: Synthesis of a Compound Containing Both a Diphosphinoamine ( P-N-P) and an Iminobiphosphine ( N=P-P) Fragment

Paul Joseph Dyson, Rosario Scopelliti, Zhaofu Fei, Wee Han Ang, Emilia Paunescu

The phosphorylation of a series of diaminopyridines (2,3-, 3,4-, 2,5- and 2,6-diaminopyridine), with various molecular equivalents of chlorodiphenylphosphine in the presence of TEA has been studied. Notably, phosphorylation of 2,3- and 3,4-diaminopyridine ...

Wiley-V C H Verlag Gmbh2014

Anthracene-Tethered Ruthenium(II) Arene Complexes as Tools To Visualize the Cellular Localization of Putative Organometallic Anticancer Compounds

Paul Joseph Dyson, Rosario Scopelliti, Christian Hartinger, Wee Han Ang, Alexey Nazarov, Olivier Pierre Zava, Michael Groessl, Albert Ruggi, Frédéric Schmitt, Julie Risse

Anthracene derivatives of ruthenium(II) arene compounds with 1,3,5-triaza-7-phosphatricyclo[3.3.1.1]decane (pta) or a sugar phosphite ligand, viz., 3,5,6-bicyclophosphite1,2-O-isopropylidene-alpha-D-glucofuranoside, were prepared in order to evaluate their ...

2012

Acetal-Functionalized RAPTA Complexes for Conjugation and Labeling

Paul Joseph Dyson, Wee Han Ang

Ruthenium-arene complexes bearing the 1,3,5-triaza-7-phosphatricyclo-[3.3.1.1]decane ligand, namely, RAPTA compounds, are widely investigated as potential antimetastatic agents for cancer therapy. Although much evidence points toward covalent binding with ...

American Chemical Society2011

Characterization of New Potential Anticancer Drugs Designed To Overcome Glutathione Transferase Mediated Resistance

Paul Joseph Dyson, Wee Han Ang, Jie Zhang

Resistance against anticancer drugs remains a serious obstacle in cancer treatment. Here we used novel strategies to target microsomal glutathione transferase 1 (MGST1) and glutathione transferase pi (GSTP) that are often overexpressed in tumors and confer ...

2011

Studies of Glutathione Transferase P1-1 Bound to a Platinum(IV)-Based Anticancer Compound Reveal the Molecular Basis of Its Activation

Paul Joseph Dyson, Ursula Röthlisberger, Wee Han Ang, Pablo Campomanes Ramos

Platinum-based cancer drugs, such as cisplatin, are highly effective chemotherapeutic agents used extensively for the treatment of solid tumors. However, their effectiveness is limited by drug resistance, which, in some cancers, has been associated with an ...

Wiley-Blackwell2011

An Internal Fluorescent Probe Based on Anthracene to Evaluate Cation-Anion Interactions in Imidazolium Salts

Paul Joseph Dyson, Rosario Scopelliti, Zhaofu Fei, Wee Han Ang, Christian Hartinger, Xuemei Yang

A series of fluorescent imidazolium-based salts contg. the cation [AnCH2MeIm]+ (in which An=anthracene and Im=the imidazolium cation) with Cl-, BF4-, PF6-, SO3CF3-, [N(CN)2]-, [N(SO2CF3)2]-, or PhBF3- anions have been prepd. and characterized. X-ray diffra ...

2010

Organometallic complexes that interconvert between trimeric and monomeric structures as a function of pH and their effect on human cancer and fibroblast cells

Paul Joseph Dyson, Rosario Scopelliti, Kay Severin, Wee Han Ang, Zacharias Immanuel Grote

Organometallic half-sandwich complexes based on ruthenium with aminomethyl-substituted 3-hydroxy-2-pyridone ligands exist in aqueous solution as monomeric O,O′-chelate complexes or trimeric metallamacrocycles depending upon the pH. We hypothesized that adm ...

2009