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Identification of a fragment-like small molecule ligand for the methyl-lysine binding protein, 53BP1.
Perfetti MT, Baughman BM, Dickson BM, Mu Y, Cui G, Mader P, Dong A, Norris JL, Rothbart SB, Strahl BD, Brown PJ, Janzen WP, Arrowsmith CH, Mer G, McBride KM, James LI, Frye SV. Perfetti MT, et al. Among authors: mader p. ACS Chem Biol. 2015 Apr 17;10(4):1072-81. doi: 10.1021/cb500956g. Epub 2015 Jan 28. ACS Chem Biol. 2015. PMID: 25590533 Free PMC article.
Identification and characterization of the first fragment hits for SETDB1 Tudor domain.
Mader P, Mendoza-Sanchez R, Iqbal A, Dong A, Dobrovetsky E, Corless VB, Liew SK, Houliston SR, De Freitas RF, Smil D, Sena CCD, Kennedy S, Diaz DB, Wu H, Dombrovski L, Allali-Hassani A, Min J, Schapira M, Vedadi M, Brown PJ, Santhakumar V, Yudin AK, Arrowsmith CH. Mader P, et al. Bioorg Med Chem. 2019 Sep 1;27(17):3866-3878. doi: 10.1016/j.bmc.2019.07.020. Epub 2019 Jul 12. Bioorg Med Chem. 2019. PMID: 31327677
Functional characterization of a PROTAC directed against BRAF mutant V600E.
Posternak G, Tang X, Maisonneuve P, Jin T, Lavoie H, Daou S, Orlicky S, Goullet de Rugy T, Caldwell L, Chan K, Aman A, Prakesch M, Poda G, Mader P, Wong C, Maier S, Kitaygorodsky J, Larsen B, Colwill K, Yin Z, Ceccarelli DF, Batey RA, Taipale M, Kurinov I, Uehling D, Wrana J, Durocher D, Gingras AC, Al-Awar R, Therrien M, Sicheri F. Posternak G, et al. Among authors: mader p. Nat Chem Biol. 2020 Nov;16(11):1170-1178. doi: 10.1038/s41589-020-0609-7. Epub 2020 Aug 10. Nat Chem Biol. 2020. PMID: 32778845 Free PMC article.
Bora phosphorylation substitutes in trans for T-loop phosphorylation in Aurora A to promote mitotic entry.
Tavernier N, Thomas Y, Vigneron S, Maisonneuve P, Orlicky S, Mader P, Regmi SG, Van Hove L, Levinson NM, Gasmi-Seabrook G, Joly N, Poteau M, Velez-Aguilera G, Gavet O, Castro A, Dasso M, Lorca T, Sicheri F, Pintard L. Tavernier N, et al. Among authors: mader p. Nat Commun. 2021 Mar 26;12(1):1899. doi: 10.1038/s41467-021-21922-w. Nat Commun. 2021. PMID: 33771996 Free PMC article.
Carborane-based carbonic anhydrase inhibitors.
Brynda J, Mader P, Šícha V, Fábry M, Poncová K, Bakardiev M, Grüner B, Cígler P, Řezáčová P. Brynda J, et al. Among authors: mader p. Angew Chem Int Ed Engl. 2013 Dec 16;52(51):13760-3. doi: 10.1002/anie.201307583. Epub 2013 Nov 4. Angew Chem Int Ed Engl. 2013. PMID: 24307504
136 results