Issue 62, 2021

Facile protein conjugation of platinum for light-activated cytotoxic payload release

Abstract

The novel Pt(IV) complex trans,trans-[Pt(N3)2(Py)2(OH)(OCO-(PEG)2-NHCSNH-Ph-NCS)] (Pt4) conjugates to the side chain of lysine amino acids in proteins under mild conditions. Reaction with myoglobin generated a bioconjugate that was stable in the dark, but released a Pt(IV) prodrug upon visible light irradiation. A similar procedure was used to conjugate Pt4 to the antibody trastuzumab, resulting in the first photoactivatable Pt(IV)-antibody conjugate, demonstrating potential for highly selective cancer phototherapy.

Graphical abstract: Facile protein conjugation of platinum for light-activated cytotoxic payload release

Supplementary files

Article information

Article type
Communication
Submitted
24 May 2021
Accepted
28 Jun 2021
First published
12 Jul 2021
This article is Open Access
Creative Commons BY license

Chem. Commun., 2021,57, 7645-7648

Facile protein conjugation of platinum for light-activated cytotoxic payload release

C. Imberti, F. Lermyte, E. P. Friar, P. B. O'Connor and P. J. Sadler, Chem. Commun., 2021, 57, 7645 DOI: 10.1039/D1CC02722K

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