作者: Paula Calvert , Kang-Shen Yao , Thomas C Hamilton , Peter J O’Dwyer
DOI: 10.1016/S0009-2797(98)00008-8
关键词: Buthionine sulfoximine 、 Glutathione 、 Cancer cell 、 Homeostasis 、 Cellular homeostasis 、 Pharmacology 、 Mechanism (biology) 、 Biology 、 Cisplatin 、 Drug resistance
摘要: The greater affinity of electrophiles for thiol groups than hydroxyl or amine provides a teleological basis the evolution this mechanism to assist in maintenance cellular homeostasis. As most abundant non-protein thiol, glutathione (GSH) is pivotal protection cells from created during normal respiration and after exposure environmental mutagens. Mutagens many anti-cancer drugs, e.g. cisplatin alkylating agents, have same target, i.e. DNA. This suggested that one by which cancer might circumvent action chemotherapeutic agents would be increasing their GSH and/or enhanced conjugation these drugs tripeptide. chapter describes preclinical data support resistance platinum agents. was rationale development pharmacologic strategies lower inactivate gluathione-S-transferases make more effective. positive outcome studies enhance activity melaphalan are described as status on going clinical trials built around data.