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Page 1
A selective and orally bioavailable VHL-recruiting PROTAC achieves SMARCA2 degradation in vivo.
Kofink C, Trainor N, Mair B, Wöhrle S, Wurm M, Mischerikow N, Roy MJ, Bader G, Greb P, Garavel G, Diers E, McLennan R, Whitworth C, Vetma V, Rumpel K, Scharnweber M, Fuchs JE, Gerstberger T, Cui Y, Gremel G, Chetta P, Hopf S, Budano N, Rinnenthal J, Gmaschitz G, Mayer M, Koegl M, Ciulli A, Weinstabl H, Farnaby W. Kofink C, et al. Nat Commun. 2022 Oct 10;13(1):5969. doi: 10.1038/s41467-022-33430-6. Nat Commun. 2022. PMID: 36216795 Free PMC article.
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. 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.
Structure-Based Design of a Macrocyclic PROTAC.
Testa A, Hughes SJ, Lucas X, Wright JE, Ciulli A. Testa A, et al. Angew Chem Int Ed Engl. 2020 Jan 20;59(4):1727-1734. doi: 10.1002/anie.201914396. Epub 2019 Dec 12. Angew Chem Int Ed Engl. 2020. PMID: 31746102 Free PMC article.
Expanding the Structural Diversity at the Phenylene Core of Ligands for the von Hippel-Lindau E3 Ubiquitin Ligase: Development of Highly Potent Hypoxia-Inducible Factor-1α Stabilizers.
Vu LP, Diehl CJ, Casement R, Bond AG, Steinebach C, Strašek N, Bricelj A, Perdih A, Schnakenburg G, Sosič I, Ciulli A, Gütschow M. Vu LP, et al. J Med Chem. 2023 Sep 28;66(18):12776-12811. doi: 10.1021/acs.jmedchem.3c00434. Epub 2023 Sep 14. J Med Chem. 2023. PMID: 37708384 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. ChemMedChem. 2022 Oct 19;17(20):e202200343. doi: 10.1002/cmdc.202200343. Epub 2022 Sep 15. ChemMedChem. 2022. PMID: 36040095 Free PMC article.
14 results