THE ROLE OF INHIBITORS OF POLY(ADP-RIBOSE) POLYMERASE AS RESISTANCE-MODIFYING AGENTS IN CANCER-THERAPY

被引:106
作者
GRIFFIN, RJ [1 ]
CURTIN, NJ [1 ]
NEWELL, DR [1 ]
GOLDING, BT [1 ]
DURKACZ, BW [1 ]
CALVERT, AH [1 ]
机构
[1] UNIV NEWCASTLE UPON TYNE, CANC RES UNIT, NEWCASTLE UPON TYNE NE1 7RU, TYNE & WEAR, ENGLAND
关键词
POLY(ADP-RIBOSE) POLYMERASE; INHIBITORS; CANCER THERAPY; RESISTANCE-MODIFYING AGENTS; RADIOPOTENTIATION;
D O I
10.1016/0300-9084(96)88154-5
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Poly(ADP-ribose) polymerase (PARP) plays an important role in a number of cellular processes including DNA repair. Since poly(ADP-ribosyl)ation occurs in response to radiation- or drug-induced DNA damage, inhibitors of the enzyme may enhance the antitumour activity of radiotherapy or cytotoxic drug treatment. Ln this review the development of PARP inhibitors is discussed, and structure-activity relationships amongst inhibitors of the enzyme are presented. Studies to date regarding the in vitro and in vivo activity of PARP inhibitors, as resistance modifying agents in cancer therapy, are also overviewed.
引用
收藏
页码:408 / 422
页数:15
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