Facile protein conjugation of platinum for light-activated cytotoxic payload release†
Cinzia
Imberti, 
*a
Frederik
Lermyte,
ab
Emily P.
Friar,
a
Peter B.
O'Connor
a
and
Peter J.
Sadler
*a
*a
Frederik
Lermyte,
ab
Emily P.
Friar,
a
Peter B.
O'Connor
a
and
Peter J.
Sadler
*a
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.
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