{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Liu Y"],"funding":["Zaozhuang University","Natural Science Foundation of Shandong Province"],"pagination":["E5660"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC6888404"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["20(22)"],"pubmed_abstract":["The development of Pt(IV) anticancer prodrugs to overcome the detrimental side effects of Pt(II)-based anticancer drugs is of current interest. The kinetics and reaction mechanisms of the reductive activation of the carboplatin Pt(IV) prodrug cis,trans-[Pt(cbdca)(NH3)2Cl2] (cbdca = cyclobutane-1,1-dicarboxylate) by the major small-molecule reductants in human plasma were analyzed in this work. The reductants included ascorbate (Asc), the thiol-containing molecules L-cysteine (Cys), DL-homocysteine (Hcy), and glutathione (GSH), and the dipeptide Cys-Gly. Overall second-order kinetics were established in all cases. At the physiological pH of 7.4, the observed second-order rate constants k' followed the order Asc << Cys-Gly ~ Hcy < GSH < Cys. This reactivity order together with the abundances"],"journal":["International journal of molecular sciences"],"pubmed_title":["Investigations of the Kinetics and Mechanism of Reduction of a Carboplatin Pt(IV) Prodrug by the Major Small-Molecule Reductants in Human Plasma."],"pmcid":["PMC6888404"],"funding_grant_id":["1020717","ZR2019MB015","2018BS060"],"pubmed_authors":["Xu L","Liu Y","Zhou L","Elding LI","Tian H","Xu B","Shi T","Liu C","Wang J"],"additional_accession":[]},"is_claimable":false,"name":"Investigations of the Kinetics and Mechanism of Reduction of a Carboplatin Pt(IV) Prodrug by the Major Small-Molecule Reductants in Human Plasma.","description":"The development of Pt(IV) anticancer prodrugs to overcome the detrimental side effects of Pt(II)-based anticancer drugs is of current interest. The kinetics and reaction mechanisms of the reductive activation of the carboplatin Pt(IV) prodrug cis,trans-[Pt(cbdca)(NH3)2Cl2] (cbdca = cyclobutane-1,1-dicarboxylate) by the major small-molecule reductants in human plasma were analyzed in this work. The reductants included ascorbate (Asc), the thiol-containing molecules L-cysteine (Cys), DL-homocysteine (Hcy), and glutathione (GSH), and the dipeptide Cys-Gly. Overall second-order kinetics were established in all cases. At the physiological pH of 7.4, the observed second-order rate constants k' followed the order Asc << Cys-Gly ~ Hcy < GSH < Cys. This reactivity order together with the abundances","dates":{"release":"2019-01-01T00:00:00Z","publication":"2019 Nov","modification":"2025-04-05T15:09:22.777Z","creation":"2020-05-21T21:20:36Z"},"accession":"S-EPMC6888404","cross_references":{"pubmed":["31726728"],"doi":["10.3390/ijms20225660"]}}