Publication
Antibody-peptide conjugates for targeted inhibition of cysteine proteases
Publications associées (33)
Development of cysteine cathepsin inhibitors combined with cell type-specific delivery for the treatment of B-cell lymphoma and solid tumors
Cysteine cathepsins proteases are enzymes that play essential physiological roles, but their activity is also associated to different aspects of cancer progression and to the development of other diseases. Therefore, cysteine cathepsins are relevant and pr ...
EPFL2024Structural Basis of the Allosteric Inhibition of Human ABCG2 by Nanobodies
Henning Paul-Julius Stahlberg, Dongchun Ni
ABCG2 is an ATP-binding cassette transporter that exports a wide range of xenobiotic compounds and has been recognized as a contributing factor for multidrug resistance in cancer cells. Substrate and inhibitor interactions with ABCG2 have been extensively ...
ACADEMIC PRESS LTD- ELSEVIER SCIENCE LTD2023Multitarget-Directed Gallium(III) Tris(acyl-pyrazolonate) Complexes Induce Ferroptosis in Cancer Cells via Dysregulation of Cell Redox Homeostasis and Inhibition of the Mevalonate Pathway
A series of Ga(Q(n))(3) coordination compounds have been synthesized, where HQ(n) is 1-phenyl-3-methyl-4-RC(=O)-pyrazolo-5-one. The complexes have been characterized through analytical data, NMR and IR spectroscopy, ESI mass spectrometry, elemental analysi ...
AMER CHEMICAL SOC2023Structures of ABCG2 under turnover conditions reveal a key step in the drug transport mechanism
Henning Paul-Julius Stahlberg, Dongchun Ni
ABCG2 is a multidrug transporter that affects drug pharmacokinetics and contributes to multidrug resistance of cancer cells. In previously reported structures, the reaction cycle was halted by the absence of substrates or ATP, mutation of catalytic residue ...
NATURE RESEARCH2021Hetero-Bis-Conjugation of Bioactive Molecules to Half-Sandwich Ruthenium(II) and Iridium(III) Complexes Provides Synergic Effects in Cancer Cell Cytotoxicity
Paul Joseph Dyson, Lucinda Kate Batchelor, Mouna Hadiji
Four bipyridine-type ligands variably derivatized with two bioactive groups (taken from ethacrynic acid, flurbiprofen, biotin, and benzylpenicillin) were prepared via sequential esterification steps from commercial 2,2'-bipyridine-4,4'-dicarboxylic acid an ...
AMER CHEMICAL SOC2021Heterobimetallic 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 ...
2019Discovery of novel competitive dihydropteridine reductase inhibitors via high throughput screening and their effect on metabolic pterin balance of fibroblast.
The development of tool compounds for the study of the tetrahydrobiopterin (BH4) metabolic network perturbation is of interest especially in the case of oxidative and nitrosative stress genesis. A semisynthetic FRET sensor was engineered in order to study ...
EPFL2018Organometallic Glutathione S-Transferase Inhibitors
Paul Joseph Dyson, Rosario Scopelliti, Mylène Soudani, Emilia Paunescu
A new family of organometallic p-cymene ruthenium(II) and osmium(II) complexes conjugated to ethacrynic acid, a glutathione transferase (GST) inhibitor, is reported. The ethacrynic acid moiety (either one or two) is tethered to the arene ruthenium(II) and ...
2017Regulated intramembrane proteolysis of the AXL receptor kinase generates an intracellular domain that localizes in the nucleus of cancer cells
Deregulation of the TAM (TYRO3, AXL, and MERTK) family of receptor tyrosine kinases (RTKs) has recently been demonstrated to predominately promote survival and chemoresistance of cancer cells. Intramembrane proteolysis mediated by presenilin/gamma-secretas ...
Federation Amer Soc Exp Biol2017Adjuvant-Loaded Subcellular Vesicles Derived From Disrupted Cancer Cells for Cancer Vaccination
Maartje Martina Cornelia Bastings
Immunogenic subcellular vesicular particles that can be used to stimulate antigen-specific immune responses in vitro and in vivo are generated from whole cancer cells. The particles retain a broad antigen repertoire similar to that of the parent cells, and ...
Wiley-Blackwell2016