FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2472318494> ?p ?o ?g. }

• W2472318494 endingPage "3349" @default.
• W2472318494 startingPage "3341" @default.
• W2472318494 abstract "Cancer-targeting alkylphosphocholine (APC) analogues are being clinically developed for diagnostic imaging, intraoperative visualization, and therapeutic applications. These APC analogues derived from chemically synthesized phospholipid ethers were identified and optimized for cancer-targeting specificity using extensive structure–activity studies. While they strongly label human brain cancers associated with disrupted blood–brain barriers (BBB), APC permeability across intact BBB remains unknown. Three of our APC analogues, CLR1404 (PET radiotracer), CLR1501 (green fluorescence), and CLR1502 (near-infrared fluorescence), were tested for permeability across a BBB model composed of human induced pluripotent stem cell-derived brain microvascular endothelial cells (iPSC-derived BMECs). This in vitro BBB system has reproducibly consistent high barrier integrity marked by high transendothelial electrical resistance (TEER > 1500 Ω-cm2) and functional expression of drug efflux transporters. The radioiodinated and fluorescent APC analogues demonstrated fairly low permeability across the iPSC-BMEC (35 ± 5.7 (CLR1404), 54 ± 3.2 (CLR1501), and 26 ± 4.9 (CLR1502) × 10–5 cm/min) compared with BBB-impermeable sucrose (13 ± 2.5) and BBB-permeable diazepam (170 ± 29). Only the fluorescent APC analogues (CLR1501, CLR1502) underwent BCRP and MRP polarized drug efflux transport in the brain-to-blood direction of the BBB model, and this efflux can be specifically blocked with pharmacological inhibition. None of the tested APC analogues appeared to undergo substantial P-gp transport. Limited permeability of the APC analogues across an intact BBB into normal brain likely contributes to the high tumor to background ratios observed in initial human trials. Moreover, addition of fluorescent moieties to APCs resulted in greater BMEC efflux via MRP and BCRP, and may affect fluorescence-guided applications. Overall, the characterization of APC analogue permeability across human BBB is significant for advancing future brain tumor-targeted applications of these agents." @default.
• W2472318494 created "2016-07-22" @default.
• W2472318494 creator A5013731126 @default.
• W2472318494 creator A5017967519 @default.
• W2472318494 creator A5018164562 @default.
• W2472318494 creator A5025343176 @default.
• W2472318494 creator A5054371127 @default.
• W2472318494 creator A5057900193 @default.
• W2472318494 creator A5062284472 @default.
• W2472318494 creator A5062631287 @default.
• W2472318494 creator A5068994351 @default.
• W2472318494 date "2016-08-04" @default.
• W2472318494 modified "2023-10-06" @default.
• W2472318494 title "Analysis of Cancer-Targeting Alkylphosphocholine Analogue Permeability Characteristics Using a Human Induced Pluripotent Stem Cell Blood–Brain Barrier Model" @default.
• W2472318494 cites W1493590273 @default.
• W2472318494 cites W1582107311 @default.
• W2472318494 cites W1902114397 @default.
• W2472318494 cites W1935203071 @default.
• W2472318494 cites W1967913742 @default.
• W2472318494 cites W1976622833 @default.
• W2472318494 cites W1988998405 @default.
• W2472318494 cites W1995632100 @default.
• W2472318494 cites W1996123970 @default.
• W2472318494 cites W1996441995 @default.
• W2472318494 cites W2000525583 @default.
• W2472318494 cites W2001726213 @default.
• W2472318494 cites W2007658730 @default.
• W2472318494 cites W2013280216 @default.
• W2472318494 cites W2024476294 @default.
• W2472318494 cites W2030098805 @default.
• W2472318494 cites W2031237950 @default.
• W2472318494 cites W2042883482 @default.
• W2472318494 cites W2042897518 @default.
• W2472318494 cites W2046826638 @default.
• W2472318494 cites W2053657477 @default.
• W2472318494 cites W2055948888 @default.
• W2472318494 cites W2056252635 @default.
• W2472318494 cites W2058649893 @default.
• W2472318494 cites W2059636317 @default.
• W2472318494 cites W2067468321 @default.
• W2472318494 cites W2069000409 @default.
• W2472318494 cites W2073764485 @default.
• W2472318494 cites W2087420035 @default.
• W2472318494 cites W2094788202 @default.
• W2472318494 cites W2096287682 @default.
• W2472318494 cites W2100886724 @default.
• W2472318494 cites W2110475445 @default.
• W2472318494 cites W2110790042 @default.
• W2472318494 cites W2117553516 @default.
• W2472318494 cites W2126799977 @default.
• W2472318494 cites W2135465849 @default.
• W2472318494 cites W2136487679 @default.
• W2472318494 cites W2142046859 @default.
• W2472318494 cites W2142839245 @default.
• W2472318494 cites W2148977460 @default.
• W2472318494 cites W2152172559 @default.
• W2472318494 cites W2157907127 @default.
• W2472318494 cites W2164322384 @default.
• W2472318494 cites W2168414172 @default.
• W2472318494 cites W2202001486 @default.
• W2472318494 cites W2265134273 @default.
• W2472318494 cites W2321980425 @default.
• W2472318494 cites W2412022044 @default.
• W2472318494 cites W2413659186 @default.
• W2472318494 cites W2623436983 @default.
• W2472318494 cites W4245392732 @default.
• W2472318494 cites W4248585778 @default.
• W2472318494 doi "https://doi.org/10.1021/acs.molpharmaceut.6b00441" @default.
• W2472318494 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/5014630" @default.
• W2472318494 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/27421304" @default.
• W2472318494 hasPublicationYear "2016" @default.
• W2472318494 type Work @default.
• W2472318494 sameAs 2472318494 @default.
• W2472318494 citedByCount "29" @default.
• W2472318494 countsByYear W24723184942016 @default.
• W2472318494 countsByYear W24723184942017 @default.
• W2472318494 countsByYear W24723184942018 @default.
• W2472318494 countsByYear W24723184942019 @default.
• W2472318494 countsByYear W24723184942020 @default.
• W2472318494 countsByYear W24723184942021 @default.
• W2472318494 countsByYear W24723184942022 @default.
• W2472318494 countsByYear W24723184942023 @default.
• W2472318494 crossrefType "journal-article" @default.
• W2472318494 hasAuthorship W2472318494A5013731126 @default.
• W2472318494 hasAuthorship W2472318494A5017967519 @default.
• W2472318494 hasAuthorship W2472318494A5018164562 @default.
• W2472318494 hasAuthorship W2472318494A5025343176 @default.
• W2472318494 hasAuthorship W2472318494A5054371127 @default.
• W2472318494 hasAuthorship W2472318494A5057900193 @default.
• W2472318494 hasAuthorship W2472318494A5062284472 @default.
• W2472318494 hasAuthorship W2472318494A5062631287 @default.
• W2472318494 hasAuthorship W2472318494A5068994351 @default.
• W2472318494 hasBestOaLocation W24723184942 @default.
• W2472318494 hasConcept C104317684 @default.
• W2472318494 hasConcept C107459253 @default.
• W2472318494 hasConcept C120882062 @default.
• W2472318494 hasConcept C121608353 @default.
• W2472318494 hasConcept C12554922 @default.

• next