مورد إلكتروني
P-glycoprotein Inhibition: The Past, the Present and the Future
| العنوان: | P-glycoprotein Inhibition: The Past, the Present and the Future |
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| المصدر: | Current Drug Metabolism |
| بيانات النشر: | Bentham Science Publishers 2011 |
| تفاصيل مُضافة: | Darby, Richard A. J. McMahon, Roisin M. Callaghan, Richard |
| نوع الوثيقة: | Electronic Resource |
| مستخلص: | The multidrug resistant phenotype of cancer cells can often result from the over-production of a number of ATP binding cassette (ABC) transporters, including P-glycoprotein (P-gp). These multidrug efflux transporters expel administered anti-cancer drugs from the cancer cell, preventing sufficient intracellular drug accumulation and ultimately, drug efficacy. The co-administration of compounds that can impede the efflux of chemotherapeutic agents by these ABC transporters can concomitantly modulate various cytochrome P450 (CYP450) enzymes, consequently impacting upon anti-cancer drug metabolism. This can further result in unfavourable drug-drug interactions and altered pharmacokinetic properties of the administered anti-cancer drugs with knock-on adverse cytotoxic side effects. This review will discuss some of the P-gp inhibitors designed and employed to date, as well as expressing our views of the shortcomings of their design strategy. We present a medicinal chemist's wish list for the paradigmatic P-gp inhibitor molecule and examine the possible future strategies that could be implemented to achieve its design. |
| مصطلحات الفهرس: | Keywords: cremophor; cyclosporin A; dexamethasone; doxorubicin; elacridar; Fructus schizandrae extract; glycoprotein P; glycoprotein P inhibitor; paclitaxel; plant extract; silibinin; tariquidar; unclassified drug; valspodar; verapamil; vincristine; zosuquidar; bon ABC transporter; Chemotherapy; Cytochrome P450; Drug metabolism; Multidrug resistance; P-gp, Journal article |
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| الإتاحة: | Open access content. Open access content |
| أرقام أخرى: | AUANP oai:openresearch-repository.anu.edu.au:1885/24722 1389-2002 1291757480 |
| المصدر المساهم: | AUSTRALIAN NAT UNIV - PRINT REPOSITORY From OAIster®, provided by the OCLC Cooperative. |
| رقم الأكسشن: | edsoai.on1291757480 |
| قاعدة البيانات: | OAIster |
| الوصف غير متاح. |