Inhibit or Evade Multidrug Resistance P-Glycoprotein in Cancer Treatment
| Autor: | Qinghai Zhang, Deepali Waghray |
|---|---|
| Rok vydání: | 2017 |
| Předmět: |
0301 basic medicine
Drug biology Chemistry media_common.quotation_subject Context (language use) Drug resistance Multiple drug resistance 03 medical and health sciences 030104 developmental biology 0302 clinical medicine Drug development 030220 oncology & carcinogenesis Drug Discovery Drug delivery biology.protein Cancer research Molecular Medicine Efflux media_common P-glycoprotein |
| Zdroj: | Journal of Medicinal Chemistry. 61:5108-5121 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/acs.jmedchem.7b01457 |
| Popis: | Multidrug resistance (MDR) is a major cause of failure in cancer chemotherapy. P-glycoprotein (P-gp), a promiscuous drug efflux pump, has been extensively studied for its association with MDR due to overexpression in cancer cells. Several P-gp inhibitors or modulators have been investigated in clinical trials in hope of circumventing MDR, with only limited success. Alternative strategies are actively pursued, such as the modification of existing drugs, development of new drugs, or combination of novel drug delivery agents to evade P-gp-dependent efflux. Despite the importance and numerous studies, these efforts have mostly been undertaken without a priori knowledge of how drugs interact with P-gp at the molecular level. This review highlights and discusses progress toward and challenges impeding drug development for inhibiting or evading P-gp in the context of our improved understanding of the structural basis and mechanism of P-gp-mediated MDR. |
| Databáze: | OpenAIRE |
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