FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W3135691966> ?p ?o ?g. }

• W3135691966 abstract "Abstract Enhanced/prolonged cAMP signalling has been suggested as a suppressor of cancer proliferation. Interestingly, two key modulators that elevate cAMP, the A 2A receptor (A 2A R) and phosphodiesterase 10A (PDE10A), are differentially co-expressed in various types of non-small lung cancer (NSCLC) cell-lines. Thus, finding dual-target compounds, which are simultaneously agonists at the A 2A R whilst also inhibiting PDE10A, could be a novel anti-proliferative approach. Using ligand- and structure-based modelling combined with MD simulations (which identified Val 84 displacement as a novel conformational descriptor of A 2A R activation), a series of known PDE10A inhibitors were shown to dock to the orthosteric site of the A 2A R. Subsequent in-vitro analysis confirmed that these compounds bind to the A 2A R and exhibit dual-activity at both the A 2A R and PDE10A. Furthermore, many of the compounds exhibited promising anti-proliferative effects upon NSCLC cell-lines, which directly correlated with the expression of both PDE10A and the A 2A R. Thus, we propose a structure-based methodology, which has been validated in in-vitro binding and functional assays, and demonstrated a promising therapeutic value." @default.
• W3135691966 created "2021-03-15" @default.
• W3135691966 creator A5013807967 @default.
• W3135691966 creator A5014283781 @default.
• W3135691966 creator A5026643759 @default.
• W3135691966 creator A5057661647 @default.
• W3135691966 creator A5059033623 @default.
• W3135691966 creator A5062696225 @default.
• W3135691966 creator A5071304314 @default.
• W3135691966 creator A5076475814 @default.
• W3135691966 date "2021-03-03" @default.
• W3135691966 modified "2023-09-25" @default.
• W3135691966 title "Structure‐based identification of dual ligands at the A2AR and PDE10A with anti‐proliferative effects in lung cancer cell‐lines" @default.
• W3135691966 cites W1858241001 @default.
• W3135691966 cites W1933158260 @default.
• W3135691966 cites W1967889357 @default.
• W3135691966 cites W1968745182 @default.
• W3135691966 cites W1969591740 @default.
• W3135691966 cites W1969641018 @default.
• W3135691966 cites W1976975058 @default.
• W3135691966 cites W1977417864 @default.
• W3135691966 cites W1980962873 @default.
• W3135691966 cites W2003750251 @default.
• W3135691966 cites W2009423060 @default.
• W3135691966 cites W2023020566 @default.
• W3135691966 cites W2027061080 @default.
• W3135691966 cites W2027423337 @default.
• W3135691966 cites W2031168104 @default.
• W3135691966 cites W2034649274 @default.
• W3135691966 cites W2038622549 @default.
• W3135691966 cites W2044832362 @default.
• W3135691966 cites W2052914592 @default.
• W3135691966 cites W2059538452 @default.
• W3135691966 cites W2075739824 @default.
• W3135691966 cites W2077262614 @default.
• W3135691966 cites W2095373531 @default.
• W3135691966 cites W2102513649 @default.
• W3135691966 cites W2116757514 @default.
• W3135691966 cites W2121443918 @default.
• W3135691966 cites W2123388283 @default.
• W3135691966 cites W2129153475 @default.
• W3135691966 cites W2140831051 @default.
• W3135691966 cites W2165747500 @default.
• W3135691966 cites W2167381827 @default.
• W3135691966 cites W2234295074 @default.
• W3135691966 cites W2280969907 @default.
• W3135691966 cites W2398669046 @default.
• W3135691966 cites W2417679656 @default.
• W3135691966 cites W2561263099 @default.
• W3135691966 cites W2586253560 @default.
• W3135691966 cites W2594829311 @default.
• W3135691966 cites W2602759026 @default.
• W3135691966 cites W2615296077 @default.
• W3135691966 cites W2746440664 @default.
• W3135691966 cites W2775170184 @default.
• W3135691966 cites W2779854606 @default.
• W3135691966 cites W2804831779 @default.
• W3135691966 cites W2910962561 @default.
• W3135691966 cites W2945328740 @default.
• W3135691966 cites W2949688987 @default.
• W3135691966 cites W2958625601 @default.
• W3135691966 cites W2978185019 @default.
• W3135691966 cites W2985087194 @default.
• W3135691966 cites W3001422834 @default.
• W3135691966 cites W3149078497 @default.
• W3135691966 doi "https://doi.org/10.1186/s13321-021-00492-5" @default.
• W3135691966 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/7927403" @default.
• W3135691966 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/33658076" @default.
• W3135691966 hasPublicationYear "2021" @default.
• W3135691966 type Work @default.
• W3135691966 sameAs 3135691966 @default.
• W3135691966 citedByCount "1" @default.
• W3135691966 countsByYear W31356919662023 @default.
• W3135691966 crossrefType "journal-article" @default.
• W3135691966 hasAuthorship W3135691966A5013807967 @default.
• W3135691966 hasAuthorship W3135691966A5014283781 @default.
• W3135691966 hasAuthorship W3135691966A5026643759 @default.
• W3135691966 hasAuthorship W3135691966A5057661647 @default.
• W3135691966 hasAuthorship W3135691966A5059033623 @default.
• W3135691966 hasAuthorship W3135691966A5062696225 @default.
• W3135691966 hasAuthorship W3135691966A5071304314 @default.
• W3135691966 hasAuthorship W3135691966A5076475814 @default.
• W3135691966 hasBestOaLocation W31356919661 @default.
• W3135691966 hasConcept C116569031 @default.
• W3135691966 hasConcept C121608353 @default.
• W3135691966 hasConcept C126322002 @default.
• W3135691966 hasConcept C170493617 @default.
• W3135691966 hasConcept C181199279 @default.
• W3135691966 hasConcept C185592680 @default.
• W3135691966 hasConcept C202751555 @default.
• W3135691966 hasConcept C2776256026 @default.
• W3135691966 hasConcept C502942594 @default.
• W3135691966 hasConcept C54355233 @default.
• W3135691966 hasConcept C55493867 @default.
• W3135691966 hasConcept C62826618 @default.
• W3135691966 hasConcept C70721500 @default.
• W3135691966 hasConcept C71924100 @default.
• W3135691966 hasConcept C81885089 @default.
• W3135691966 hasConcept C86803240 @default.
• W3135691966 hasConcept C95444343 @default.

• next