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Photoactive platinum(iv) complex conjugated to a cancer-cell-targeting cyclic peptide
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Shi, Huayun, Wang, Qian, Venkatesh, Venkatesh, Feng, Guokai, Young, Lawrence S., Romero-Canelón, Isolda, Zeng, Musheng and Sadler, P. J. (2019) Photoactive platinum(iv) complex conjugated to a cancer-cell-targeting cyclic peptide. Dalton Transactions . doi:10.1039/c9dt00909d (In Press)
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Official URL: http://dx.doi.org/10.1039/c9dt00909d
Abstract
A conjugate of cancer-cell targeting cyclic disulphide non a-peptide c(CRWYDENAC) consisting of nine L-amino acids with the photoactive succinate platinum(IV)complex trans, trans-[Pt(N3)2(py)2(OH)(succinate)] (Pt-cP) has been synthesised and characterised. The conjugate was stable in dark, but released succinate–peptide and Pt(II) species upon irradiation with visible light, and formed photoproducts with guanine. Conjugate Pt-cP exhibited higher photocytotoxicity than parent complextrans, trans, trans-[Pt(N3)2(OH)2(py)2] (FM-190) towards cancer cells, including ovarian A2780, lung A549 and prostate PC3 human cancer cells upon irradiation with blue light (465 nm, 17.28 J cm−2) with IC50values of 2.8–22.4μM and the highest potency for A549 cells. Even though the dark cellular accumulation of Pt-cP in A2780 cells was lower than that of parent FM-190, Pt from Pt-cP accumulated in cancer cells upon irradiation to a level >3× higher than that fromFM-190. In addition, the cellular accumulation of Pt from Pt-cPwas enhanced ca. 47× after irradiation.
| Item Type: | Journal Article | |||||||||||||||||||||
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| Subjects: | R Medicine > RM Therapeutics. Pharmacology | |||||||||||||||||||||
| Divisions: | Faculty of Science > Chemistry | |||||||||||||||||||||
| Library of Congress Subject Headings (LCSH): | Prodrugs, Cyclic peptides | |||||||||||||||||||||
| Journal or Publication Title: | Dalton Transactions | |||||||||||||||||||||
| Publisher: | Royal Society of Chemistry | |||||||||||||||||||||
| ISSN: | 1477-9226 | |||||||||||||||||||||
| Official Date: | 31 May 2019 | |||||||||||||||||||||
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| Date of first compliant deposit: | 3 June 2019 | |||||||||||||||||||||
| DOI: | 10.1039/c9dt00909d | |||||||||||||||||||||
| Status: | Peer Reviewed | |||||||||||||||||||||
| Publication Status: | In Press | |||||||||||||||||||||
| Access rights to Published version: | Open Access | |||||||||||||||||||||
| RIOXX Funder/Project Grant: |
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