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DCAF1-based PROTACs with activity against clinically validated targets overcoming intrinsic- and acquired-degrader resistance.
Schröder M, Renatus M, Liang X, Meili F, Zoller T, Ferrand S, Gauter F, Li X, Sigoillot F, Gleim S, Stachyra TM, Thomas JR, Begue D, Khoshouei M, Lefeuvre P, Andraos-Rey R, Chung B, Ma R, Pinch B, Hofmann A, Schirle M, Schmiedeberg N, Imbach P, Gorses D, Calkins K, Bauer-Probst B, Maschlej M, Niederst M, Maher R, Henault M, Alford J, Ahrne E, Tordella L, Hollingworth G, Thomä NH, Vulpetti A, Radimerski T, Holzer P, Carbonneau S, Thoma CR. Schröder M, et al. Among authors: calkins k. Nat Commun. 2024 Jan 4;15(1):275. doi: 10.1038/s41467-023-44237-4. Nat Commun. 2024. PMID: 38177131 Free PMC article.
BRD9 degraders as chemosensitizers in acute leukemia and multiple myeloma.
Weisberg E, Chowdhury B, Meng C, Case AE, Ni W, Garg S, Sattler M, Azab AK, Sun J, Muz B, Sanchez D, Toure A, Stone RM, Galinsky I, Winer E, Gleim S, Gkountela S, Kedves A, Harrington E, Abrams T, Zoller T, Vaupel A, Manley P, Faller M, Chung B, Chen X, Busenhart P, Stephan C, Calkins K, Bonenfant D, Thoma CR, Forrester W, Griffin JD. Weisberg E, et al. Among authors: calkins k. Blood Cancer J. 2022 Jul 19;12(7):110. doi: 10.1038/s41408-022-00704-7. Blood Cancer J. 2022. PMID: 35853853 Free PMC article.
Protein destabilization underlies pathogenic missense mutations in ARID1B.
Mermet-Meillon F, Mercan S, Bauer-Probst B, Allard C, Bleu M, Calkins K, Knehr J, Altorfer M, Naumann U, Sprouffske K, Barys L, Sesterhenn F, Galli GG. Mermet-Meillon F, et al. Among authors: calkins k. Nat Struct Mol Biol. 2024 Feb 12. doi: 10.1038/s41594-024-01229-2. Online ahead of print. Nat Struct Mol Biol. 2024. PMID: 38347147
Discovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation Approach.
Chen C, Zhu H, Stauffer F, Caravatti G, Vollmer S, Machauer R, Holzer P, Möbitz H, Scheufler C, Klumpp M, Tiedt R, Beyer KS, Calkins K, Guthy D, Kiffe M, Zhang J, Gaul C. Chen C, et al. Among authors: calkins k. ACS Med Chem Lett. 2016 Jun 1;7(8):735-40. doi: 10.1021/acsmedchemlett.6b00167. eCollection 2016 Aug 11. ACS Med Chem Lett. 2016. PMID: 27563395 Free PMC article.
New Potent DOT1L Inhibitors for in Vivo Evaluation in Mouse.
Stauffer F, Weiss A, Scheufler C, Möbitz H, Ragot C, Beyer KS, Calkins K, Guthy D, Kiffe M, Van Eerdenbrugh B, Tiedt R, Gaul C. Stauffer F, et al. Among authors: calkins k. ACS Med Chem Lett. 2019 Dec 4;10(12):1655-1660. doi: 10.1021/acsmedchemlett.9b00452. eCollection 2019 Dec 12. ACS Med Chem Lett. 2019. PMID: 31857842 Free PMC article.
Maximizing the Efficacy of MAPK-Targeted Treatment in PTENLOF/BRAFMUT Melanoma through PI3K and IGF1R Inhibition.
Herkert B, Kauffmann A, Mollé S, Schnell C, Ferrat T, Voshol H, Juengert J, Erasimus H, Marszalek G, Kazic-Legueux M, Billy E, Ruddy D, Stump M, Guthy D, Ristov M, Calkins K, Maira SM, Sellers WR, Hofmann F, Hall MN, Brachmann SM. Herkert B, et al. Among authors: calkins k. Cancer Res. 2016 Jan 15;76(2):390-402. doi: 10.1158/0008-5472.CAN-14-3358. Epub 2015 Nov 17. Cancer Res. 2016. PMID: 26577700
104 results