Determination of drug binding sites to proteins by electrospray ionisation mass spectrometry: the interaction of cisplatin with transferrin.
Cisplatin, cis-[PtCl2(NH3)2], is known to bind to human serum transferrin, but the binding site remains a matter of some debate. Electrospray ionisation mass spectrometry has been used to characterise the interaction of cisplatin with transferrin. The studies indicate that cisplatin initially docks with, and subsequently bonds covalently to, the hydroxyl functional group of threonine 457, with the loss of HCl affording a transferrin-O-PtCl(NH3)2 adduct.
Allardyce
Claire S
CS
Institut de chimie minérale et analytique, Ecole polytechnique fédérale de Lausanne, EPFL - BCH, CH-1015 Lausanne, Switzerland.
Dyson
Paul J
PJ
Coffey
Jonathan
J
Johnson
Neil
N
D000595:Amino Acid Sequence; D000970:Antineoplastic Agents / Q000378:metabolism*; D001665:Binding Sites; D002945:Cisplatin / Q000378:metabolism*; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D008969:Molecular Sequence Data; D010984:Platinum / Q000737:chemistry / Q000378:metabolism; D011485:Protein Binding; D011955:Receptors, Drug / Q000737:chemistry*; D021241:Spectrometry, Mass, Electrospray Ionization; D014168:Transferrin / Q000737:chemistry*
D000970:Antineoplastic Agents; D011955:Receptors, Drug; D014168:Transferrin; D010984:Platinum; D002945:Cisplatin