FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2433234551> ?p ?o ?g. }

• W2433234551 endingPage "233" @default.
• W2433234551 startingPage "216" @default.
• W2433234551 abstract "Multidrug resistance (MDR) and drug transporter P-glycoprotein (P-gp) represent major obstacles in cancer chemotherapy. We investigated 19 synthetic curcumin derivatives in drug-sensitive acute lymphoblastic CCRF-CEM leukemia cells and their multidrug-resistant P-gp-overexpressing subline, CEM/ADR5000.Cytotoxicity was tested by resazurin assays. Doxorubicin uptake was assessed by flow cytometry. Binding modes of compounds to P-gp were analyzed by molecular docking. Chemical features responsible for bioactivity were studied by quantitative structure activity relationship (QSAR) analyses. A 7-descriptor QSAR model was correlated with doxorubicin uptake values, IC50 values and binding energies.The compounds displayed IC50 values between 0.7±0.03 and 20.2±0.25μM. CEM/ADR5000 cells exhibited cross-resistance to 10 compounds, collateral sensitivity to three compounds and regular sensitivity to the remaining six curcumins. Molecular docking studies at the intra-channel transmembrane domain of human P-gp resulted in lowest binding energies ranging from -9.00±0.10 to -6.20±0.02kcal/mol and pKi values from 0.24±0.04 to 29.17±0.88μM. At the ATP-binding site of P-gp, lowest binding energies ranged from -9.78±0.17 to -6.79±0.01kcal/mol and pKi values from 0.07±0.02 to 0.03±0.03μM. CEM/ADR5000 cells accumulated approximately 4-fold less doxorubicin than CCRF-CEM cells. The control P-gp inhibitor, verapamil, partially increased doxorubicin uptake in CEM/ADR5000 cells. Six curcumins increased doxorubicin uptake in resistant cells or even exceeded uptake levels compared to sensitive one. QSAR yielded good activity prediction (R=0.797 and R=0.794 for training and test sets).Selected derivatives may serve to guide future design of novel P-gp inhibitors and collateral sensitive drugs to combat MDR." @default.
• W2433234551 created "2016-06-24" @default.
• W2433234551 creator A5003798258 @default.
• W2433234551 creator A5015214749 @default.
• W2433234551 creator A5042042057 @default.
• W2433234551 creator A5052981792 @default.
• W2433234551 creator A5071993355 @default.
• W2433234551 creator A5075626026 @default.
• W2433234551 creator A5078307836 @default.
• W2433234551 creator A5084677440 @default.
• W2433234551 date "2016-08-01" @default.
• W2433234551 modified "2023-10-02" @default.
• W2433234551 title "Modulation of P-glycoprotein activity by novel synthetic curcumin derivatives in sensitive and multidrug-resistant T-cell acute lymphoblastic leukemia cell lines" @default.
• W2433234551 cites W1271999003 @default.
• W2433234551 cites W1599388734 @default.
• W2433234551 cites W1608993354 @default.
• W2433234551 cites W1933364203 @default.
• W2433234551 cites W1967556023 @default.
• W2433234551 cites W1968171024 @default.
• W2433234551 cites W1972408290 @default.
• W2433234551 cites W1973068653 @default.
• W2433234551 cites W1976194786 @default.
• W2433234551 cites W1977594275 @default.
• W2433234551 cites W1977672095 @default.
• W2433234551 cites W1983739445 @default.
• W2433234551 cites W1984381506 @default.
• W2433234551 cites W1989335851 @default.
• W2433234551 cites W1992811886 @default.
• W2433234551 cites W1994769604 @default.
• W2433234551 cites W1998813367 @default.
• W2433234551 cites W1999312756 @default.
• W2433234551 cites W1999702104 @default.
• W2433234551 cites W2003323323 @default.
• W2433234551 cites W2010573152 @default.
• W2433234551 cites W2015331321 @default.
• W2433234551 cites W2015996393 @default.
• W2433234551 cites W2021018857 @default.
• W2433234551 cites W2021711019 @default.
• W2433234551 cites W2022387872 @default.
• W2433234551 cites W2027682810 @default.
• W2433234551 cites W2029519554 @default.
• W2433234551 cites W2035308484 @default.
• W2433234551 cites W2037423947 @default.
• W2433234551 cites W2037690301 @default.
• W2433234551 cites W2042182152 @default.
• W2433234551 cites W2052369675 @default.
• W2433234551 cites W2053933453 @default.
• W2433234551 cites W2060259273 @default.
• W2433234551 cites W2061107603 @default.
• W2433234551 cites W2061695655 @default.
• W2433234551 cites W2064095058 @default.
• W2433234551 cites W2065068389 @default.
• W2433234551 cites W2073156788 @default.
• W2433234551 cites W2075054009 @default.
• W2433234551 cites W2077532200 @default.
• W2433234551 cites W2079479745 @default.
• W2433234551 cites W2081794970 @default.
• W2433234551 cites W2084777758 @default.
• W2433234551 cites W2085186686 @default.
• W2433234551 cites W2092118786 @default.
• W2433234551 cites W2094493150 @default.
• W2433234551 cites W2096962297 @default.
• W2433234551 cites W2098142549 @default.
• W2433234551 cites W2098376669 @default.
• W2433234551 cites W2100736039 @default.
• W2433234551 cites W2108525782 @default.
• W2433234551 cites W2111160771 @default.
• W2433234551 cites W2118234018 @default.
• W2433234551 cites W2125598794 @default.
• W2433234551 cites W2126214807 @default.
• W2433234551 cites W2126283892 @default.
• W2433234551 cites W2131280407 @default.
• W2433234551 cites W2134174082 @default.
• W2433234551 cites W2137631271 @default.
• W2433234551 cites W2142777712 @default.
• W2433234551 cites W2148982368 @default.
• W2433234551 cites W2151300092 @default.
• W2433234551 cites W2156327396 @default.
• W2433234551 cites W2157393167 @default.
• W2433234551 cites W2157463354 @default.
• W2433234551 cites W2159768584 @default.
• W2433234551 cites W2166344128 @default.
• W2433234551 cites W2167319421 @default.
• W2433234551 cites W2169302611 @default.
• W2433234551 cites W2171345996 @default.
• W2433234551 cites W4239476948 @default.
• W2433234551 doi "https://doi.org/10.1016/j.taap.2016.06.002" @default.
• W2433234551 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/27318188" @default.
• W2433234551 hasPublicationYear "2016" @default.
• W2433234551 type Work @default.
• W2433234551 sameAs 2433234551 @default.
• W2433234551 citedByCount "27" @default.
• W2433234551 countsByYear W24332345512016 @default.
• W2433234551 countsByYear W24332345512017 @default.
• W2433234551 countsByYear W24332345512018 @default.
• W2433234551 countsByYear W24332345512019 @default.
• W2433234551 countsByYear W24332345512020 @default.
• W2433234551 countsByYear W24332345512021 @default.

• next