Antibody-peptide conjugates for targeted inhibition of cysteine proteases
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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 ...
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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 ...
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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 ...
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 ...
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 ...
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 ...