2015
DOI: 10.7287/peerj.preprints.1271v1
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The apparent permeabilities of Caco-2 cells to marketed drugs: magnitude, and independence from both biophysical properties and endogenite similarities

Abstract: Abstract15 We bring together fifteen, nonredundant, tabulated collections (amounting to 696 separate 16 measurements) of the apparent permeability (P app ) of Caco-2 cells to marketed drugs. While in some 17 cases there are some significant interlaboratory disparities, most are quite minor. Most drugs are not 18 especially permeable through Caco-2 cells, with the median P app value being some 16 . 10 -6 cm.s -1 . This 19 value is considerably lower than those (1310 and 230 . 10 -6 cm.s -1 ) recently used in so… Show more

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Cited by 6 publications
(9 citation statements)
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“…However, by contrast, we find that as many as 80 % of natural products show such a similarity when surveyed extensively. This is consistent with the earlier, pilot findings ( Figure 5C of [22]), and with the fact that Caco-2 permeability was poorly correlated with (the MACCS encoding of) endogenite-likeness [15].…”
Section: Natural Products That Are Nutrients or Bioactive Drugs Must supporting
confidence: 92%
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“…However, by contrast, we find that as many as 80 % of natural products show such a similarity when surveyed extensively. This is consistent with the earlier, pilot findings ( Figure 5C of [22]), and with the fact that Caco-2 permeability was poorly correlated with (the MACCS encoding of) endogenite-likeness [15].…”
Section: Natural Products That Are Nutrients or Bioactive Drugs Must supporting
confidence: 92%
“…However, when the TYPICAL encoding used, each of the 1381 drugs was closer to (or equal with) at least one exogenous natural product that is in either or both of UNPD and DNP than it is to an endogenite (data not shown). Finally, in previous work [15], we had compared a meta-analysis of 680 Caco-2 cell permeabilities of 187 marketed drugs with their endogenitelikeness (finding none). Neither did we find any relationship between Caco-2 permeability and any analysis of closeness to the union of the UNPD and DNP databases; as an illustration, Figure 11F compares the same permeabilities with the maximum pattern TS.…”
Section: The Union Of the Unpd And Dnp Databasesmentioning
confidence: 99%
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“…However, the newly acquired abilities to manipulate transporter expression levels systematically and in a high-throughput manner, whether by genome editing or other means 2,4,5 , will no doubt allow us to make considerable progress in answering the question of which transporters are used by specific drugs. Coupling this with progress in the understanding of the endogenous biological roles of transporters could have a key role in identifying drug candidates that have the ability to cross biological membranes at the relatively modest rates necessary 9 to exert the desired pharmacological effect at the desired location, using principles based on those of natural selection 10 .…”
mentioning
confidence: 99%