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Page 1
Targeted degradation via direct 26S proteasome recruitment.
Bashore C, Prakash S, Johnson MC, Conrad RJ, Kekessie IA, Scales SJ, Ishisoko N, Kleinheinz T, Liu PS, Popovych N, Wecksler AT, Zhou L, Tam C, Zilberleyb I, Srinivasan R, Blake RA, Song A, Staben ST, Zhang Y, Arnott D, Fairbrother WJ, Foster SA, Wertz IE, Ciferri C, Dueber EC. Bashore C, et al. Among authors: staben st. Nat Chem Biol. 2023 Jan;19(1):55-63. doi: 10.1038/s41589-022-01218-w. Epub 2022 Dec 28. Nat Chem Biol. 2023. PMID: 36577875 Free PMC article.
Antibody-mediated delivery of chimeric protein degraders which target estrogen receptor alpha (ERα).
Dragovich PS, Adhikari P, Blake RA, Blaquiere N, Chen J, Cheng YX, den Besten W, Han J, Hartman SJ, He J, He M, Rei Ingalla E, Kamath AV, Kleinheinz T, Lai T, Leipold DD, Li CS, Liu Q, Lu J, Lu Y, Meng F, Meng L, Ng C, Peng K, Lewis Phillips G, Pillow TH, Rowntree RK, Sadowsky JD, Sampath D, Staben L, Staben ST, Wai J, Wan K, Wang X, Wei B, Wertz IE, Xin J, Xu K, Yao H, Zang R, Zhang D, Zhou H, Zhao Y. Dragovich PS, et al. Among authors: staben l, staben st. Bioorg Med Chem Lett. 2020 Feb 15;30(4):126907. doi: 10.1016/j.bmcl.2019.126907. Epub 2019 Dec 18. Bioorg Med Chem Lett. 2020. PMID: 31902710
Monomeric Targeted Protein Degraders.
Hanan EJ, Liang J, Wang X, Blake RA, Blaquiere N, Staben ST. Hanan EJ, et al. Among authors: staben st. J Med Chem. 2020 Oct 22;63(20):11330-11361. doi: 10.1021/acs.jmedchem.0c00093. Epub 2020 Jun 15. J Med Chem. 2020. PMID: 32352776 Review.
Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 1: Exploration of Antibody Linker, Payload Loading, and Payload Molecular Properties.
Dragovich PS, Pillow TH, Blake RA, Sadowsky JD, Adaligil E, Adhikari P, Bhakta S, Blaquiere N, Chen J, Dela Cruz-Chuh J, Gascoigne KE, Hartman SJ, He M, Kaufman S, Kleinheinz T, Kozak KR, Liu L, Liu L, Liu Q, Lu Y, Meng F, Mulvihill MM, O'Donohue A, Rowntree RK, Staben LR, Staben ST, Wai J, Wang J, Wei B, Wilson C, Xin J, Xu Z, Yao H, Zhang D, Zhang H, Zhou H, Zhu X. Dragovich PS, et al. Among authors: staben lr, staben st. J Med Chem. 2021 Mar 11;64(5):2534-2575. doi: 10.1021/acs.jmedchem.0c01845. Epub 2021 Feb 17. J Med Chem. 2021. PMID: 33596065
Primary Amine Tethered Small Molecules Promote the Degradation of X-Linked Inhibitor of Apoptosis Protein.
den Besten W, Verma K, Yamazoe S, Blaquiere N, Phung W, Izrael-Tomasevic A, Mulvihill MM, Helgason E, Prakash S, Goncharov T, Vucic D, Dueber E, Fairbrother WJ, Wertz I, Yu K, Staben ST. den Besten W, et al. Among authors: staben st. J Am Chem Soc. 2021 Jul 21;143(28):10571-10575. doi: 10.1021/jacs.1c05269. Epub 2021 Jul 8. J Am Chem Soc. 2021. PMID: 34236858
Identifying transcriptional programs underlying cancer drug response with TraCe-seq.
Chang MT, Shanahan F, Nguyen TTT, Staben ST, Gazzard L, Yamazoe S, Wertz IE, Piskol R, Yang YA, Modrusan Z, Haley B, Evangelista M, Malek S, Foster SA, Ye X. Chang MT, et al. Among authors: staben st. Nat Biotechnol. 2022 Jan;40(1):86-93. doi: 10.1038/s41587-021-01005-3. Epub 2021 Sep 16. Nat Biotechnol. 2022. PMID: 34531539
A Multifaceted Hit-Finding Approach Reveals Novel LC3 Family Ligands.
Steffek M, Helgason E, Popovych N, Rougé L, Bruning JM, Li KS, Burdick DJ, Cai J, Crawford T, Xue J, Decurtins W, Fang C, Grubers F, Holliday MJ, Langley A, Petersen A, Satz AL, Song A, Stoffler D, Strebel Q, Tom JYK, Skelton N, Staben ST, Wichert M, Mulvihill MM, Dueber EC. Steffek M, et al. Among authors: staben st. Biochemistry. 2023 Feb 7;62(3):633-644. doi: 10.1021/acs.biochem.1c00682. Epub 2022 Jan 5. Biochemistry. 2023. PMID: 34985287 Free article.
Overcoming Preclinical Safety Obstacles to Discover (S)-N-((1,2,3,5,6,7-Hexahydro-s-indacen-4-yl)carbamoyl)-6-(methylamino)-6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-3-sulfonamide (GDC-2394): A Potent and Selective NLRP3 Inhibitor.
McBride C, Trzoss L, Povero D, Lazic M, Ambrus-Aikelin G, Santini A, Pranadinata R, Bain G, Stansfield R, Stafford JA, Veal J, Takahashi R, Ly J, Chen S, Liu L, Nespi M, Blake R, Katewa A, Kleinheinz T, Sujatha-Bhaskar S, Ramamoorthi N, Sims J, McKenzie B, Chen M, Ultsch M, Johnson M, Murray J, Ciferri C, Staben ST, Townsend MJ, Stivala CE. McBride C, et al. Among authors: staben st. J Med Chem. 2022 Nov 10;65(21):14721-14739. doi: 10.1021/acs.jmedchem.2c01250. Epub 2022 Oct 24. J Med Chem. 2022. PMID: 36279149
Ternary complex dissociation kinetics contribute to mutant-selective EGFR degradation.
Rosenberg SC, Shanahan F, Yamazoe S, Kschonsak M, Zeng YJ, Lee J, Plise E, Yen I, Rose CM, Quinn JG, Gazzard LJ, Walters BT, Kirkpatrick DS, Staben ST, Foster SA, Malek S. Rosenberg SC, et al. Among authors: staben st. Cell Chem Biol. 2023 Feb 8:S2451-9456(23)00030-2. doi: 10.1016/j.chembiol.2023.01.007. Online ahead of print. Cell Chem Biol. 2023. PMID: 36773603 Free article.
Back pocket flexibility provides group II p21-activated kinase (PAK) selectivity for type I 1/2 kinase inhibitors.
Staben ST, Feng JA, Lyle K, Belvin M, Boggs J, Burch JD, Chua CC, Cui H, DiPasquale AG, Friedman LS, Heise C, Koeppen H, Kotey A, Mintzer R, Oh A, Roberts DA, Rouge L, Rudolph J, Tam C, Wang W, Xiao Y, Young A, Zhang Y, Hoeflich KP. Staben ST, et al. J Med Chem. 2014 Feb 13;57(3):1033-45. doi: 10.1021/jm401768t. Epub 2014 Feb 4. J Med Chem. 2014. PMID: 24432870
46 results