Abstract：
:Efflux out of cells by P-glycoprotein (P-gp) represents a serious liability for pharmaceuticals, particularly for anti-cancer drugs. Consequently, identification of compounds as potential substrates is important for understanding their bioavailability. Also, the development of agents which reverse this multi-drug resistance phenotype has received considerable attention. Assays for determining these activities are reviewed. Recent literature and studies into the structure-activity relationships (SAR) of the resulting data are discussed. Multiple binding sites and other complicating factors have prevented the development of a truly general, conclusive SAR either for substrate or inhibitory activities. Consequently, many models have tended to address only very general properties, such as lipophilicity and size. However, progress has been made in the last few years toward more specific SAR suggesting well-defined structural features responsible for both activities. The future of understanding the details of P-gp SAR lies in more specific assays that target specific binding sites and mechanisms of action.
journal_name
Adv Drug Deliv Revjournal_title
Advanced drug delivery reviewsauthors
Stouch TR,Gudmundsson Odoi
10.1016/s0169-409x(02)00006-6subject
Has Abstractpub_date
2002-03-31 00:00:00pages
315-28issue
3eissn
0169-409Xissn
1872-8294pii
S0169409X02000066journal_volume
54pub_type
杂志文章,评审abstract：:Infectious diseases are prevalent in the developing world and are one of the developing world's major sources of morbidity and mortality. While infectious diseases can initiate in a localized region, they can spread rapidly at any moment due to the ease of traveling from one part of the world to the next. This could l...
journal_title：Advanced drug delivery reviews
pub_type： 杂志文章,评审
doi：10.1016/j.addr.2009.11.015
更新日期：2010-03-18 00:00:00
abstract：:Cells cultured in vitro will tend to retain their differentiated phenotype under conditions that resemble their natural in vivo environment, for example, when cultured on polymer scaffolds in tissue culture bioreactors. In this chapter, we define organized cell communities as three-dimensional in vitro grown cell-poly...
journal_title：Advanced drug delivery reviews
pub_type： 杂志文章
doi：10.1016/s0169-409x(98)00017-9
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abstract：:The selection of drug candidates early in development has become increasingly important to minimize the use of animals and to avoid costly failures of drugs later in development. In vitro systems to predict and assess organ toxicity have so far been of limited value due to difficulties in demonstrating in vivo-relevan...
journal_title：Advanced drug delivery reviews
pub_type： 杂志文章,评审
doi：10.1016/j.addr.2013.12.005
更新日期：2014-04-01 00:00:00
abstract：:The early impact of nanotechnology on medicine is beginning to get realized, with novel nanoscale therapeutic and diagnostic modalities under development or in clinical practice today. In this commentary the field of "nanomedicine" is briefly reviewed form the perspective of where we were; where we are today; and wher...
journal_title：Advanced drug delivery reviews
pub_type： 杂志文章,评审
doi：10.1016/j.addr.2006.09.011
更新日期：2006-12-01 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.2018.06.020
更新日期：2018-07-01 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.2004.05.003
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journal_title：Advanced drug delivery reviews
pub_type： 杂志文章,评审
doi：10.1016/j.addr.2007.03.017
更新日期：2007-05-30 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.2006.01.025
更新日期：2006-08-07 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.2020.12.008
更新日期：2021-02-01 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.2016.04.007
更新日期：2016-06-01 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.2014.02.002
更新日期：2014-11-30 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.2018.01.017
更新日期：2018-01-01 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.2013.04.002
更新日期：2013-08-01 00:00:00
abstract：:Thioredoxin 1 (Trx 1) is a redox-active small protein ubiquitously present in human body. It is one of the defensive proteins induced in response to various stress conditions. In addition to its anti-oxidative effect by dithiol-disulfide exchange in its active site, Trx 1 has anti-apoptotic and anti-inflammatory effec...
journal_title：Advanced drug delivery reviews
pub_type： 杂志文章,评审
doi：10.1016/j.addr.2009.01.003
更新日期：2009-04-28 00:00:00
abstract：:Recent pre-clinical and clinical studies have shown that stem cell-based therapies hold tremendous promise for the treatment of human disease. Mesenchymal stem cells (MSC) are emerging as promising anti-cancer agents which have an enormous potential to be utilized to treat a number of different cancer types. MSC have ...
journal_title：Advanced drug delivery reviews
pub_type： 杂志文章,评审
doi：10.1016/j.addr.2011.06.010
更新日期：2012-06-01 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.2010.04.011
更新日期：2010-07-31 00:00:00
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journal_title：Advanced drug delivery reviews
pub_type： 杂志文章
doi：10.1016/j.addr.2013.11.003
更新日期：2014-06-01 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.2004.01.003
更新日期：2004-04-29 00:00:00
abstract：:A site-directed method of joining proteins to poly(ethylene glycol) is presented which allows for the preparation of essentially homogeneous PEG-protein derivatives with a single PEG chain conjugated to the amine terminus of the protein. This selectivity is achieved by conducting the reductive alkylation of proteins w...
journal_title：Advanced drug delivery reviews
pub_type： 杂志文章,评审
doi：10.1016/s0169-409x(02)00023-6
更新日期：2002-06-17 00:00:00
abstract：:Mitochondria represent both the main source and target of reactive oxygen and nitrogen species (RONS). In view of the large energy expenditure made by neurons during neurotransmission, an intact mitochondrial function is of paramount importance for the correct function of the brain. Accordingly, the search of therapeu...
journal_title：Advanced drug delivery reviews
pub_type： 杂志文章,评审
doi：10.1016/j.addr.2009.05.009
更新日期：2009-11-30 00:00:00
abstract：:A recombinant C-terminal truncated form of the human soluble tumor necrosis factor receptor type I (sTNF-RI) was produced in E. coli. This soluble receptor contains the first 2.6 of the 4 domains of the intact sTNF-RI molecule. A monoPEGylated form of this molecule was produced using a 30 kD methoxyPEG aldehyde with a...
journal_title：Advanced drug delivery reviews
pub_type： 杂志文章,评审
doi：10.1016/s0169-409x(03)00112-1
更新日期：2003-09-26 00:00:00
abstract：:Patients with critical limb ischemia constitute a potential target population for therapeutic angiogenesis. Because the growth of new collateral vessels can be achieved in a time interval of 1 month or less, these patients are suitable candidates for treatment with non-viral vectors intended to yield short-term gene e...
journal_title：Advanced drug delivery reviews
pub_type： 杂志文章
doi：10.1016/s0169-409x(97)00115-4
更新日期：1998-03-02 00:00:00
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journal_title：Advanced drug delivery reviews
pub_type： 杂志文章
doi：10.1016/s0169-409x(98)00028-3
更新日期：1998-09-07 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.2015.04.008
更新日期：2015-08-30 00:00:00
abstract：:The percentage of new chemical entities synthesised with low aqueous solubility and high therapeutic efficacy is growing, this presents major challenges for the drug delivery scientists. The role of physicochemical properties in identification of suitable drug candidates for oral lipid-based delivery systems is discus...
journal_title：Advanced drug delivery reviews
pub_type： 杂志文章
doi：10.1016/j.addr.2007.10.012
更新日期：2008-03-17 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.2015.09.001
更新日期：2016-01-15 00:00:00
abstract：:Cytochrome P450 enzymes (CYPs) form one of the most important enzyme families involved in the metabolism of xenobiotics. CYPs comprise many isoforms, which catalyze a wide variety of reactions, and potentially, a large number of different metabolites can be formed. However, it is often hard to rationalize what metabol...
journal_title：Advanced drug delivery reviews
pub_type： 杂志文章,评审
doi：10.1016/j.addr.2015.04.020
更新日期：2015-06-23 00:00:00
abstract：:The encapsulation of liquids and semi-solids provides solutions for convenient delivery through improved oral absorption of poorly water-soluble drugs. In addition, low dose (content uniformity), highly potent (containment), low melting point drugs, those with a critical stability profile and those for which a delayed...
journal_title：Advanced drug delivery reviews
pub_type： 杂志文章,评审
doi：10.1016/j.addr.2007.09.009
更新日期：2008-03-17 00:00:00
abstract：:Novel drug delivery systems based on microtechnology have advanced tremendously, but yet face some technological and societal hurdles to fully achieve their potential. The novel drug delivery systems aim to deliver drugs in a spatiotemporal- and dosage-controlled manner with a goal to address the unmet medical needs f...
journal_title：Advanced drug delivery reviews
pub_type： 杂志文章,评审
doi：10.1016/j.addr.2017.11.003
更新日期：2018-03-15 00:00:00
abstract：:Polycystic kidney disease (PKD) is characterized by progressive cyst growth and is a leading cause of renal failure worldwide. Currently, there are limited therapeutic options available to PKD patients, and only one drug, tolvaptan, has been FDA-approved to slow cyst progression. Similar to other small molecule drugs,...
journal_title：Advanced drug delivery reviews
pub_type： 杂志文章,评审
doi：10.1016/j.addr.2020.08.011
更新日期：2020-01-01 00:00:00
