Drug retention, efflux, and resistance in tumor cells

Krishan, Awtar; Fitz, Catherine Morgan; Andritsch, Ilia

doi:10.1002/(sici)1097-0320(19971201)29:4<279::aid-cyto3>3.0.co;2-5

Cited by 56 publications

(29 citation statements)

References 44 publications

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“…Cancers with the MDR phenotype over-express efflux transporters belonging to a superfamily of ATP binding cassette proteins, such as P-gp and MDR-associated proteins that pump drugs out of cells [34,35]. It was reported that PBCs can inhibit P-gp function [2,13].…”

Section: Cell Uptake Studymentioning

confidence: 99%

Shell-crosslinked Pluronic L121 micelles as a drug delivery vehicle

et al. 2007

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Section: Cell Uptake Studymentioning

confidence: 99%

Shell-crosslinked Pluronic L121 micelles as a drug delivery vehicle

et al. 2007

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“…Several classes of pharmacologically active compounds share transport pathways with nutrients. [10] A substantial role has been recognized for transport proteins in oral absorption and drug bioavailability; [11] drug resistance, e.g., efflux of antineoplastic compounds from tumor cells mediated by multidrug resistance (MDR) gene products; [12,13] excretion of drugs and their metabolites, mediated by transporters in the kidney and liver; drug toxicity; [14] and drug pharmacokinetics and pharmacodynamics. [15 -17] Furthermore, the pathophysiology of several hereditary diseases (i.e., clearly defined phenotypes shown to be inherited as a monogenic Mendelian traits) have been attributed to mutations in transport proteins.…”

Section: Clinical Pharmacology Of Slc Proteinsmentioning

confidence: 99%

“…So far, several molecules have been found to possess this effect in animal studies. [13,169] The first such inhibitors comprised the coupling of two bile acid molecules via a spacer to allow simultaneous interaction with more than one transporter site, resulting in an efficient inhibition of bile acid reabsorption without or with only low absorption of the inhibitor itself [3] (Fig. 8; R14).…”

Section: Cholesterol-reducing Agentsmentioning

confidence: 99%

Structural Biology and Function of Solute Transporters: Implications for Identifying and Designing Substrates

Zhang

Knipp

Ekins

et al. 2002

Drug Metabolism Reviews

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Solute carrier (SLC) proteins have critical physiological roles in nutrient transport and may be utilized as a mechanism to increase drug absorption. However, we have little understanding of these proteins at the molecular level due to the absence of high-resolution crystal structures. Numerous efforts have been made in characterizing the peptide transporter (PepT1) and the apical sodium dependent bile acid transporter (ASBT) that are important for both their native transporter function as well as targets to increase absorption and act as therapeutic targets. In vitro and computational approaches have been applied to gain some insight into these transporters with some success. This represents an opportunity for optimizing molecules as substrates for the solute transporters and providing a further screening system for drug discovery. Clearly the future growth in knowledge of SLC function will be led by integrated in vitro and in silico approaches.

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“…The cells (1-2 ϫ 10 6 ml -1 ) were cultured in 5 ml polystyrene tubes, in R10 containing 5 µg ml -1 Rh123 [17,34] and 1 µg ml -1 PI. If indicated, the medium was supplemented with various Strahlenther Onkol 2003 · No.…”

Section: Rh123 Accumulation Assaymentioning

confidence: 99%