PARP Inhibitors as P-glyoprotein Substrates
نویسندگان
چکیده
منابع مشابه
PARP inhibitors
Poly (ADP-ribose) polymerases, abbreviated as PARPs, are a group of familiar proteins that play a central role in DNA repair employing the base excision repair (BER) pathway. There about 17 proteins in this family out of which the primary nuclear PARPs are PARP-1, PARP-2, PARP-3, and tankyrases 1 and 2 (PARP-5a and -5b) .The PARP family members are known to engage in a wide range of cellular ac...
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Poly (ADP-ribose) polymerase (PARP) is a novel therapeutic target in cancer. Preclinical studies demonstrate that PARP inhibitors selectively kill BRCAdeficient cells and potentiate the effects of DNA-damaging agents. There are several PARP inhibitors in clinical development, including olaparib, iniparib, veliparib, PF01367338, and MK-4827. Phase II studies of single-agent olaparib demonstrate ...
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Polyadenosine diphosphate (ADP) ribose polymerase (PARP) lends a panoramic view to the inner mystery of protection of integrity of deoxyribonucleic acid (DNA) in a cell genome. They are a balancing part of an even more dynamic equilibrium of normalcy against daily assaults. PARP finds its companion candidates in other tumor suppressors, with the most prominent and glaring one being breast cance...
متن کاملSuicide Substrates as Irreversible Inhibitors of Aavoenzymes
SUMMARY An increasing number of flavin dependent enzymes have recently been found to be inhibited by substrate analogs which fulfill the requirements set forth for suicide inhibitors. In most cases in-activation results from covalent modification of the flavin coenzyme; in other cases protein alkylation at the enzyme active center is involved. Examples of the first are the inactivation of gener...
متن کاملPARP inhibitors in breast cancer.
The therapeutic implications of DNA damage in cancer therapy have long been appreciated and form the basis of many successful cytotoxic chemotherapy and radiotherapy treatment strategies. A novel class of DNA repair defect targeted therapeutics that inhibit poly (ADP-Ribose) polymerase (PARP) are being rapidly developed in breast cancer based on exciting preliminary clinical activity as single ...
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ژورنال
عنوان ژورنال: Journal of Pharmaceutical Sciences
سال: 2014
ISSN: 0022-3549
DOI: 10.1002/jps.23952