FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2300566088> ?p ?o ?g. }

• W2300566088 endingPage "3162" @default.
• W2300566088 startingPage "3152" @default.
• W2300566088 abstract "No α-helical mimetic that exhibits Bcl-2/MDM2 dual inhibition has been rationally designed due to the different helicities of the α-helixes at their binding interfaces. Herein, we extracted a one-turn α-helix-mimicking ortho-triarene unit from o-phenylene foldamers. Linking benzamide substrates with a rotatable C–N bond, we constructed a novel semirigid pyramid-like scaffold that could support its two-turn α-helix mimicry without aromatic stacking interactions and could adopt the different dihedral angles of the key residues of p53 and BH3-only peptides. On the basis of this universal scaffold, a series of substituent groups were installed to capture the key residues of both p53TAD and BimBH3 and balance the differences of the bulks between them. Identified by FP, ITC, and NMR spectroscopy, a compound 6e (zq-1) that directly binds to Mcl-1, Bcl-2, and MDM2 with balanced submicromolar affinities was obtained. Cell-based experiments demonstrated its antitumor ability through Bcl-2/MDM2 dual inhibition simultaneously." @default.
• W2300566088 created "2016-06-24" @default.
• W2300566088 creator A5003115340 @default.
• W2300566088 creator A5010215768 @default.
• W2300566088 creator A5028856871 @default.
• W2300566088 creator A5038057139 @default.
• W2300566088 creator A5038318377 @default.
• W2300566088 creator A5043882363 @default.
• W2300566088 creator A5049264813 @default.
• W2300566088 creator A5055341182 @default.
• W2300566088 creator A5086716026 @default.
• W2300566088 date "2016-03-22" @default.
• W2300566088 modified "2023-10-17" @default.
• W2300566088 title "Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics" @default.
• W2300566088 cites W1835922068 @default.
• W2300566088 cites W1967697238 @default.
• W2300566088 cites W1976261939 @default.
• W2300566088 cites W1976295398 @default.
• W2300566088 cites W1978924350 @default.
• W2300566088 cites W1988913922 @default.
• W2300566088 cites W1997800761 @default.
• W2300566088 cites W1999606433 @default.
• W2300566088 cites W1999978441 @default.
• W2300566088 cites W2000880755 @default.
• W2300566088 cites W2005659815 @default.
• W2300566088 cites W2006718263 @default.
• W2300566088 cites W2007107879 @default.
• W2300566088 cites W2012024423 @default.
• W2300566088 cites W2020112177 @default.
• W2300566088 cites W2056283033 @default.
• W2300566088 cites W2056508746 @default.
• W2300566088 cites W2064496336 @default.
• W2300566088 cites W2085419794 @default.
• W2300566088 cites W2097933346 @default.
• W2300566088 cites W2104296519 @default.
• W2300566088 cites W2112425650 @default.
• W2300566088 cites W2138414870 @default.
• W2300566088 cites W2139268587 @default.
• W2300566088 cites W2141777898 @default.
• W2300566088 cites W2147495370 @default.
• W2300566088 cites W2150048195 @default.
• W2300566088 cites W2162899430 @default.
• W2300566088 cites W2164316626 @default.
• W2300566088 cites W2168166668 @default.
• W2300566088 cites W2174725453 @default.
• W2300566088 cites W2329780347 @default.
• W2300566088 cites W4234803768 @default.
• W2300566088 doi "https://doi.org/10.1021/acs.jmedchem.5b01913" @default.
• W2300566088 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/26982372" @default.
• W2300566088 hasPublicationYear "2016" @default.
• W2300566088 type Work @default.
• W2300566088 sameAs 2300566088 @default.
• W2300566088 citedByCount "19" @default.
• W2300566088 countsByYear W23005660882016 @default.
• W2300566088 countsByYear W23005660882017 @default.
• W2300566088 countsByYear W23005660882018 @default.
• W2300566088 countsByYear W23005660882019 @default.
• W2300566088 countsByYear W23005660882020 @default.
• W2300566088 countsByYear W23005660882021 @default.
• W2300566088 countsByYear W23005660882022 @default.
• W2300566088 countsByYear W23005660882023 @default.
• W2300566088 crossrefType "journal-article" @default.
• W2300566088 hasAuthorship W2300566088A5003115340 @default.
• W2300566088 hasAuthorship W2300566088A5010215768 @default.
• W2300566088 hasAuthorship W2300566088A5028856871 @default.
• W2300566088 hasAuthorship W2300566088A5038057139 @default.
• W2300566088 hasAuthorship W2300566088A5038318377 @default.
• W2300566088 hasAuthorship W2300566088A5043882363 @default.
• W2300566088 hasAuthorship W2300566088A5049264813 @default.
• W2300566088 hasAuthorship W2300566088A5055341182 @default.
• W2300566088 hasAuthorship W2300566088A5086716026 @default.
• W2300566088 hasConcept C112887158 @default.
• W2300566088 hasConcept C178790620 @default.
• W2300566088 hasConcept C185592680 @default.
• W2300566088 hasConcept C19549132 @default.
• W2300566088 hasConcept C21951064 @default.
• W2300566088 hasConcept C2778689049 @default.
• W2300566088 hasConcept C2780231548 @default.
• W2300566088 hasConcept C2780283098 @default.
• W2300566088 hasConcept C32909587 @default.
• W2300566088 hasConcept C33347731 @default.
• W2300566088 hasConcept C66974803 @default.
• W2300566088 hasConcept C71240020 @default.
• W2300566088 hasConcept C8010536 @default.
• W2300566088 hasConcept C89025888 @default.
• W2300566088 hasConceptScore W2300566088C112887158 @default.
• W2300566088 hasConceptScore W2300566088C178790620 @default.
• W2300566088 hasConceptScore W2300566088C185592680 @default.
• W2300566088 hasConceptScore W2300566088C19549132 @default.
• W2300566088 hasConceptScore W2300566088C21951064 @default.
• W2300566088 hasConceptScore W2300566088C2778689049 @default.
• W2300566088 hasConceptScore W2300566088C2780231548 @default.
• W2300566088 hasConceptScore W2300566088C2780283098 @default.
• W2300566088 hasConceptScore W2300566088C32909587 @default.
• W2300566088 hasConceptScore W2300566088C33347731 @default.
• W2300566088 hasConceptScore W2300566088C66974803 @default.
• W2300566088 hasConceptScore W2300566088C71240020 @default.
• W2300566088 hasConceptScore W2300566088C8010536 @default.

• next