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Targeting the CoREST complex with dual histone deacetylase and demethylase inhibitors.
Kalin JH, Wu M, Gomez AV, Song Y, Das J, Hayward D, Adejola N, Wu M, Panova I, Chung HJ, Kim E, Roberts HJ, Roberts JM, Prusevich P, Jeliazkov JR, Roy Burman SS, Fairall L, Milano C, Eroglu A, Proby CM, Dinkova-Kostova AT, Hancock WW, Gray JJ, Bradner JE, Valente S, Mai A, Anders NM, Rudek MA, Hu Y, Ryu B, Schwabe JWR, Mattevi A, Alani RM, Cole PA. Kalin JH, et al. Nat Commun. 2018 Jan 4;9(1):53. doi: 10.1038/s41467-017-02242-4. Nat Commun. 2018. PMID: 29302039 Free PMC article.
Enzymologic analysis reveals that corin potently targets the CoREST complex and shows more sustained inhibition of CoREST complex HDAC activity compared with entinostat. Cell-based experiments demonstrate that corin exhibits a superior anti-prol …
Enzymologic analysis reveals that corin potently targets the CoREST complex and shows more sustained inhibition of C
Novel polyamine-based Histone deacetylases-Lysine demethylase 1 dual binding inhibitors.
Milelli A, Marchetti C, Turrini E, Catanzaro E, Mazzone R, Tomaselli D, Fimognari C, Tumiatti V, Minarini A. Milelli A, et al. Bioorg Med Chem Lett. 2018 Apr 1;28(6):1001-1004. doi: 10.1016/j.bmcl.2018.02.034. Epub 2018 Feb 17. Bioorg Med Chem Lett. 2018. PMID: 29496367
Epigenetic modulators Histone deacetylases (HDACs) and Lysine demethylase (LSD1) are validated targets for anticancer therapy. ...Combined modulation of both targets results in a synergistic antiproliferative activity. In the present investigati …
Epigenetic modulators Histone deacetylases (HDACs) and Lysine demethylase (LSD1) are validated targets for antic …