Abstract:
:Drug resistance involves multiple mechanisms. Multidrug resistance (MDR) is the leading cause of treatment failure in cancer therapy. Elevated levels of MDR proteins [members of the ATP-binding cassette (ABC) transporter family] increase cellular efflux and decrease the effectiveness of chemotherapeutic agents. As a salvage approach to overcome drug resistance, inhibitors of MDR proteins have been developed, but have had limited success mainly due to undesired toxicities. Nuclear receptors (NRs), including pregnane X receptor (PXR), regulate the expression of proteins (including MDR proteins) involved in drug metabolism and drug clearance, suggesting that it is possible to overcome drug resistance by regulating NR. This review discusses the progress in the development of MDR inhibitors, with a focus on MDR1 inhibitors. Recent development of PXR antagonists to pharmacologically modulate PXR is also reviewed. The review proposes that selectively preventing the elevation of MDR levels by regulating NRs rather than non-selectively inhibiting the MDR activity by using MDR inhibitors can be a less toxic approach to overcome drug resistance during cancer therapy.
journal_name
Adv Drug Deliv Revjournal_title
Advanced drug delivery reviewsauthors
Chen Tdoi
10.1016/j.addr.2010.07.008subject
Has Abstractpub_date
2010-10-30 00:00:00pages
1257-64issue
13eissn
0169-409Xissn
1872-8294pii
S0169-409X(10)00163-8journal_volume
62pub_type
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journal_title:Advanced drug delivery reviews
pub_type: 杂志文章,评审
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journal_title:Advanced drug delivery reviews
pub_type: 杂志文章,评审
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journal_title:Advanced drug delivery reviews
pub_type: 杂志文章,评审
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journal_title:Advanced drug delivery reviews
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journal_title:Advanced drug delivery reviews
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journal_title:Advanced drug delivery reviews
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journal_title:Advanced drug delivery reviews
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journal_title:Advanced drug delivery reviews
pub_type: 杂志文章
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journal_title:Advanced drug delivery reviews
pub_type: 杂志文章,评审
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journal_title:Advanced drug delivery reviews
pub_type: 杂志文章,评审
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journal_title:Advanced drug delivery reviews
pub_type: 杂志文章,评审
doi:10.1016/j.addr.2015.12.013
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journal_title:Advanced drug delivery reviews
pub_type: 杂志文章,评审
doi:10.1016/j.addr.2009.06.009
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journal_title:Advanced drug delivery reviews
pub_type: 杂志文章
doi:10.1016/s0169-409x(97)00079-3
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journal_title:Advanced drug delivery reviews
pub_type: 杂志文章,评审
doi:10.1016/j.addr.2012.03.011
更新日期:2012-06-15 00:00:00
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journal_title:Advanced drug delivery reviews
pub_type: 杂志文章,评审
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更新日期:2003-08-28 00:00:00
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journal_title:Advanced drug delivery reviews
pub_type: 杂志文章,评审
doi:10.1016/j.addr.2006.03.009
更新日期:2006-07-07 00:00:00
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journal_title:Advanced drug delivery reviews
pub_type: 杂志文章,评审
doi:10.1016/j.addr.2014.07.002
更新日期:2014-12-15 00:00:00
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journal_title:Advanced drug delivery reviews
pub_type: 杂志文章,评审
doi:10.1016/j.addr.2006.07.017
更新日期:2006-09-15 00:00:00
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journal_title:Advanced drug delivery reviews
pub_type: 杂志文章,评审
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journal_title:Advanced drug delivery reviews
pub_type: 杂志文章,评审
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journal_title:Advanced drug delivery reviews
pub_type: 杂志文章,评审
doi:10.1016/j.addr.2006.08.002
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journal_title:Advanced drug delivery reviews
pub_type: 杂志文章
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journal_title:Advanced drug delivery reviews
pub_type: 杂志文章,评审
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journal_title:Advanced drug delivery reviews
pub_type: 杂志文章
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journal_title:Advanced drug delivery reviews
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journal_title:Advanced drug delivery reviews
pub_type: 杂志文章,评审
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journal_title:Advanced drug delivery reviews
pub_type: 杂志文章,评审
doi:10.1016/j.addr.2011.11.013
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journal_title:Advanced drug delivery reviews
pub_type: 杂志文章,评审
doi:10.1016/j.addr.2011.06.010
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journal_title:Advanced drug delivery reviews
pub_type: 杂志文章,评审
doi:10.1016/j.addr.2011.12.009
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journal_title:Advanced drug delivery reviews
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