Matches in SemOpenAlex for { <https://semopenalex.org/work/W4386102020> ?p ?o ?g. }
- W4386102020 endingPage "117455" @default.
- W4386102020 startingPage "117455" @default.
- W4386102020 abstract "Human sirtuin 5 (SIRT5) participates in a variety of metabolic disorder-associated diseases, including cancer. Inhibition of SIRT5 has been confirmed to provide a new strategy for treatment of related diseases. Previously, we discovered a pyrimidine skeleton inhibitor XIV, which showed low micromolar inhibitory activity against SIRT5. Herein, we utilized the scaffold-hopping strategy to design and synthesize a series of 2,4,6- trisubstituted triazine derivatives. The SAR analysis led to the discovery of several new SIRT5 inhibitors with low micromolar inhibition levels. The most potent compounds 10 (IC50 = 5.38 µM), and 14 (IC50 = 4.07 µM) were further confirmed to be the substrate-competitive SIRT5 inhibitors through enzyme kinetic assays, which is consistent with the molecular docking analyses. Fluorescence-based thermal shift assays proved that these compounds may stabilize SIRT5 by binding withprotein.. In addition, compounds 10 and 14 were also revealed to have moderate selectivity to SIRT5 over SIRT1-3. This study will aid further efforts to develop highly potent and selective SIRT5 inhibitors for the treatment of cancer and other related diseases." @default.
- W4386102020 created "2023-08-24" @default.
- W4386102020 creator A5017585392 @default.
- W4386102020 creator A5020487629 @default.
- W4386102020 creator A5031604598 @default.
- W4386102020 creator A5033599023 @default.
- W4386102020 creator A5042275051 @default.
- W4386102020 creator A5042494757 @default.
- W4386102020 creator A5042986217 @default.
- W4386102020 creator A5050905118 @default.
- W4386102020 creator A5059963500 @default.
- W4386102020 creator A5065113978 @default.
- W4386102020 creator A5067010958 @default.
- W4386102020 creator A5067046405 @default.
- W4386102020 creator A5081610367 @default.
- W4386102020 creator A5090237325 @default.
- W4386102020 creator A5090462767 @default.
- W4386102020 date "2023-10-01" @default.
- W4386102020 modified "2023-09-23" @default.
- W4386102020 title "Design, synthesis and biological evaluation of 2,4,6- trisubstituted triazine derivatives as new nonpeptide small-molecule SIRT5 inhibitors" @default.
- W4386102020 cites W1955146052 @default.
- W4386102020 cites W1978702638 @default.
- W4386102020 cites W1984658022 @default.
- W4386102020 cites W1992864508 @default.
- W4386102020 cites W1994729757 @default.
- W4386102020 cites W2028178274 @default.
- W4386102020 cites W2041959419 @default.
- W4386102020 cites W2059750004 @default.
- W4386102020 cites W2062573153 @default.
- W4386102020 cites W2071219719 @default.
- W4386102020 cites W2122948771 @default.
- W4386102020 cites W2169880855 @default.
- W4386102020 cites W2172716795 @default.
- W4386102020 cites W2425374734 @default.
- W4386102020 cites W2735340872 @default.
- W4386102020 cites W2740697399 @default.
- W4386102020 cites W2793313601 @default.
- W4386102020 cites W2793563787 @default.
- W4386102020 cites W2799579025 @default.
- W4386102020 cites W2892574479 @default.
- W4386102020 cites W2900576674 @default.
- W4386102020 cites W2940254466 @default.
- W4386102020 cites W2948447106 @default.
- W4386102020 cites W2965445632 @default.
- W4386102020 cites W2978876764 @default.
- W4386102020 cites W3009832977 @default.
- W4386102020 cites W3046757836 @default.
- W4386102020 cites W3193740443 @default.
- W4386102020 cites W4220662745 @default.
- W4386102020 cites W4284897890 @default.
- W4386102020 cites W4284965472 @default.
- W4386102020 cites W4286436529 @default.
- W4386102020 cites W4311779306 @default.
- W4386102020 doi "https://doi.org/10.1016/j.bmc.2023.117455" @default.
- W4386102020 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/37643500" @default.
- W4386102020 hasPublicationYear "2023" @default.
- W4386102020 type Work @default.
- W4386102020 citedByCount "0" @default.
- W4386102020 crossrefType "journal-article" @default.
- W4386102020 hasAuthorship W4386102020A5017585392 @default.
- W4386102020 hasAuthorship W4386102020A5020487629 @default.
- W4386102020 hasAuthorship W4386102020A5031604598 @default.
- W4386102020 hasAuthorship W4386102020A5033599023 @default.
- W4386102020 hasAuthorship W4386102020A5042275051 @default.
- W4386102020 hasAuthorship W4386102020A5042494757 @default.
- W4386102020 hasAuthorship W4386102020A5042986217 @default.
- W4386102020 hasAuthorship W4386102020A5050905118 @default.
- W4386102020 hasAuthorship W4386102020A5059963500 @default.
- W4386102020 hasAuthorship W4386102020A5065113978 @default.
- W4386102020 hasAuthorship W4386102020A5067010958 @default.
- W4386102020 hasAuthorship W4386102020A5067046405 @default.
- W4386102020 hasAuthorship W4386102020A5081610367 @default.
- W4386102020 hasAuthorship W4386102020A5090237325 @default.
- W4386102020 hasAuthorship W4386102020A5090462767 @default.
- W4386102020 hasConcept C161624437 @default.
- W4386102020 hasConcept C178790620 @default.
- W4386102020 hasConcept C181199279 @default.
- W4386102020 hasConcept C185592680 @default.
- W4386102020 hasConcept C202751555 @default.
- W4386102020 hasConcept C21951064 @default.
- W4386102020 hasConcept C2776303721 @default.
- W4386102020 hasConcept C2777752112 @default.
- W4386102020 hasConcept C2779321679 @default.
- W4386102020 hasConcept C2780561631 @default.
- W4386102020 hasConcept C55493867 @default.
- W4386102020 hasConcept C71240020 @default.
- W4386102020 hasConcept C75520062 @default.
- W4386102020 hasConceptScore W4386102020C161624437 @default.
- W4386102020 hasConceptScore W4386102020C178790620 @default.
- W4386102020 hasConceptScore W4386102020C181199279 @default.
- W4386102020 hasConceptScore W4386102020C185592680 @default.
- W4386102020 hasConceptScore W4386102020C202751555 @default.
- W4386102020 hasConceptScore W4386102020C21951064 @default.
- W4386102020 hasConceptScore W4386102020C2776303721 @default.
- W4386102020 hasConceptScore W4386102020C2777752112 @default.
- W4386102020 hasConceptScore W4386102020C2779321679 @default.
- W4386102020 hasConceptScore W4386102020C2780561631 @default.
- W4386102020 hasConceptScore W4386102020C55493867 @default.