Publications related to Alkylating antineoplastic agent

Translational screening platform to evaluate chemotherapy in combination with focal therapy for retinoblastoma

Paul Joseph Dyson, Valentin Simeonov, Fabien Kuttler, Irina Sinenko, Patrik Aouad

Retinoblastoma is the most common pediatric eye cancer. It is currently treated with a limited number of drugs, adapted from other pediatric cancer treatments. Drug toxicity and relapse of the disease warrant new therapeutic strategies for these young pati ...

WILEY2023

Investigating the composition and recruitment of the mycobacterial ImuA'-ImuB-DnaE2 mutasome

John McKinney, Neeraj Dhar, Zela Alexandria-Mae Martin

A DNA damage-inducible mutagenic gene cassette has been implicated in the emergence of drug resistance in Mycobacterium tuberculosis during anti-tuberculosis (TB) chemotherapy. However, the molecular composition and operation of the encoded 'mycobacterial ...

Elife Sciences Publ Ltd2023

Engaging 1-Alkynyl Triazenes in Transition Metal-Catalyzed and Fluorinative Transformations

Jin Fay Tan

Triazenes have garnered great attention for their anti-cancer properties and versatility in organic chemistry. Recently, a novel synthesis of 1-alkynyl triazenes was reported. This thesis describes the compatibility, reactivity and applications of 1-alkyny ...

EPFL2021

TGFBI modulates tumour hypoxia and promotes breast cancer metastasis

Albert Santamaria Martinez

Breast cancer metastasis is a complex process that depends not only on intrinsic characteristics of metastatic stem cells, but also on the particular microenvironment that supports their growth and modulates the plasticity of the system. In search for micr ...

2020

Heterobimetallic Ru(mu-dppm)Fe and homobimetallic Ru(mu-dppm)Ru complexes as potential anti-cancer agents

Paul Joseph Dyson, Lucinda Kate Batchelor

Two heterobimetallic mu-dppm bridged Fe,Ru complexes, [(eta(6)-Arene)RuCl2(mu-dppm)Fe(CO)I(eta(5)-C5H5)] (Ar - C6H6 (1) and p-cymene (2), dppm-1,1-bis(diphenylphosphino)methane) were obtained in a facile reaction between [Fe(eta(5)-C5H5)I(CO)(kappa(1)-dppm ...

2019

Adverse effects of immune-checkpoint inhibitors: epidemiology, management and surveillance

Olivier Michielin, Filipe Amândio Brandão Sanches Vong Martins

Immune-checkpoint inhibitors (ICIs), including anti-cytotoxic T lymphocyte antigen 4 (CTLA-4), anti-programmed cell death 1 (PD-1) and anti-programmed cell death 1 ligand 1 (PD-L1) antibodies, are arguably the most important development in cancer therapy o ...

NATURE PUBLISHING GROUP2019

The antimicrobial peptide defensin cooperates with tumour necrosis factor to drive tumour cell death in Drosophila

Bruno Lemaitre, Anna Dostalova

Antimicrobial peptides (AMPs) are small cationic molecules best known as mediators of the innate defence against microbial infection. While in vitro and ex vivo evidence suggest AMPs' capacity to kill cancer cells, in vivo demonstration of an anti-tumour r ...

2019

Drug Repurposing Approach Identifies a Synergistic Drug Combination of an Antifungal Agent and an Experimental Organometallic Drug for Melanoma Treatment

Paul Joseph Dyson, Tina Riedel, Olivier Pierre Zava

By screening a drug library comprising FDA approved compounds, we discovered a potent interaction between the antifungal agent haloprogin and the experimental organometallic drug RAPTA-T, to synergistically induce cancer cell killing. The combination of th ...

2018

The mechanism of tumour cell death by metal-based anticancer drugs is not only a matter of DNA interactions

Paul Joseph Dyson, Gianni Sava

Platinum drugs are extensively used in the clinic to treat cancer, often leading to a palliative response rather than a cure. While DNA is considered to be the primary target of platinum drugs, there is no clear relationship between cellular platinum accum ...

2018

Oxaliplatin reacts with DMSO only in the presence of water

Paul Joseph Dyson, Laure Menin, Hristo Plamenov Varbanov

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 s ...

2017

The Differential Distribution of RAPTA-T in Non-Invasive and Invasive Breast Cancer Cells Correlates with Its Anti-Invasive and Anti-Metastatic Effects

Paul Joseph Dyson, Graham Knott, Anders Meibom, Stéphane Laurent Escrig, Catherine Maclachlan, Gianni Sava

Nanoscale secondary ion mass spectrometry (NanoSIMS) combined with transmission electron microscopy (TEM) can be a powerful approach to visualize the exact distribution of drugs at the sub-cellular level. In this work, we exploit this approach to identify ...

2017

Protein ruthenation and DNA alkylation: chlorambucil-functionalized RAPTA complexes and their anticancer activity

Paul Joseph Dyson, Christian Hartinger, Alexey Nazarov, Olivier Pierre Zava

Chemotherapeutics for the treatment of tumorigenic conditions that feature novel modes of action are highly sought after to overcome the limitations of current chemotherapies. Herein, we report the conjugation of the alkylating agent chlorambucil to the RA ...

2015

Thermoresponsive fluorinated small-molecule drugs: a new concept for efficient localized chemotherapy

Paul Joseph Dyson, Patrycja Nowak-Sliwinska, Catherine Marie Amélie Clavel, Emilia Paunescu

Hyperthermia is currently being explored as an adjuvant treatment to conventional therapies with chemotherapeutic agents based on thermoresponsive macromolecules. Although the concept of hyperthermia has existed for many years it has yet to become routinel ...

2015

Preparation and medical use of triazenes

Kay Severin, Gregor Kiefer

The present invention relates to a novel method for preparing triazenes. Further, the invention relates to novel triazenes and the use of N2O for preparing a compound comprising a triazene group. Further, the invention relates to the use of the novel triaz ...

2015

Rational design of organic and organometallic thermoresponsive or tumor-selective anticancer drugs and their in vitro and in vivo biological evaluation

Catherine Marie Amélie Clavel

Conventional chemotherapy leads to severe side-effects such as nephrotoxicity, nausea and vomiting and fatigue along with drug resistance. Alkylating agents used to treat cancer were even shown to provoke second cancers, often years after the end of chemot ...

EPFL2014

Assessing metastasis risk after pre-operative anti-angiogenic therapy

Michele De Palma, Daniela Biziato

Anti‐angiogenic drugs are approved for the treatment of several cancer types, generally in the inoperable locally advanced or metastatic setting and in combination with other anti‐cancer agents. Recent clinical studies also suggest that anti‐angiogenic dru ...

2014

Combining RNAi and in vivo confocal microscopy analysis of the photoconvertible fluorescent protein Dendra2 to study a DNA repair protein

Matteo Di Piazza

Clinical approaches for tumor treatment often rely on combination therapy where a DNA damaging agent is used in combination with a DNA repair protein inhibitor. For this reason, great efforts have been made during the last decade to identify inhibitors of ...

Biotechniques Office2013

Chemistry and Biology of Natural Products : Applications in Cancer and Infectious Diseases

Jean-Yves Wach

This thesis is divided in four independent parts related to four different research projects. Each chapter describes one of the multiple aspects covered by organic chemistry, such as the generation of functional interfaces, understanding of biological proc ...

EPFL2011

Organometallic antitumour agents with alternative modes of action

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

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

Novel dihydroxypyrrolidine derivatives as anti-cancer agents

Pierre Vogel, Claudia Bello

The present invention provides new dihydroxypyrrolidine derivatives for use as medicaments. The compounds are useful in the treatment in cancer, in particular non-solid neoplasms. ...

2010