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Page 1
Discovery of XL01126: A Potent, Fast, Cooperative, Selective, Orally Bioavailable, and Blood-Brain Barrier Penetrant PROTAC Degrader of Leucine-Rich Repeat Kinase 2.
Liu X, Kalogeropulou AF, Domingos S, Makukhin N, Nirujogi RS, Singh F, Shpiro N, Saalfrank A, Sammler E, Ganley IG, Moreira R, Alessi DR, Ciulli A. Liu X, et al. Among authors: makukhin n. J Am Chem Soc. 2022 Sep 21;144(37):16930-16952. doi: 10.1021/jacs.2c05499. Epub 2022 Aug 25. J Am Chem Soc. 2022. PMID: 36007011 Free PMC article.
Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity.
Imaide S, Riching KM, Makukhin N, Vetma V, Whitworth C, Hughes SJ, Trainor N, Mahan SD, Murphy N, Cowan AD, Chan KH, Craigon C, Testa A, Maniaci C, Urh M, Daniels DL, Ciulli A. Imaide S, et al. Among authors: makukhin n. Nat Chem Biol. 2021 Nov;17(11):1157-1167. doi: 10.1038/s41589-021-00878-4. Epub 2021 Oct 21. Nat Chem Biol. 2021. PMID: 34675414 Free PMC article.
Discovery of Benzo[d]imidazole-6-sulfonamides as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the First Bromodomain.
Cipriano A, Milite C, Feoli A, Viviano M, Pepe G, Campiglia P, Sarno G, Picaud S, Imaide S, Makukhin N, Filippakopoulos P, Ciulli A, Castellano S, Sbardella G. Cipriano A, et al. Among authors: makukhin n. ChemMedChem. 2022 Oct 19;17(20):e202200343. doi: 10.1002/cmdc.202200343. Epub 2022 Sep 15. ChemMedChem. 2022. PMID: 36040095 Free PMC article.
Targeting non-canonical activation of GLI1 by the SOX2-BRD4 transcriptional complex improves the efficacy of HEDGEHOG pathway inhibition in melanoma.
Pietrobono S, Gaudio E, Gagliardi S, Zitani M, Carrassa L, Migliorini F, Petricci E, Manetti F, Makukhin N, Bond AG, Paradise BD, Ciulli A, Fernandez-Zapico ME, Bertoni F, Stecca B. Pietrobono S, et al. Among authors: makukhin n. Oncogene. 2021 Jun;40(22):3799-3814. doi: 10.1038/s41388-021-01783-9. Epub 2021 May 6. Oncogene. 2021. PMID: 33958721 Free PMC article.