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An allosteric pan-TEAD inhibitor blocks oncogenic YAP/TAZ signaling and overcomes KRAS G12C inhibitor resistance.
Hagenbeek TJ, Zbieg JR, Hafner M, Mroue R, Lacap JA, Sodir NM, Noland CL, Afghani S, Kishore A, Bhat KP, Yao X, Schmidt S, Clausen S, Steffek M, Lee W, Beroza P, Martin S, Lin E, Fong R, Di Lello P, Kubala MH, Yang MN, Lau JT, Chan E, Arrazate A, An L, Levy E, Lorenzo MN, Lee HJ, Pham TH, Modrusan Z, Zang R, Chen YC, Kabza M, Ahmed M, Li J, Chang MT, Maddalo D, Evangelista M, Ye X, Crawford JJ, Dey A. Hagenbeek TJ, et al. Among authors: steffek m. Nat Cancer. 2023 Jun;4(6):812-828. doi: 10.1038/s43018-023-00577-0. Epub 2023 Jun 5. Nat Cancer. 2023. PMID: 37277530 Free PMC article.
Small Molecule Dysregulation of TEAD Lipidation Induces a Dominant-Negative Inhibition of Hippo Pathway Signaling.
Holden JK, Crawford JJ, Noland CL, Schmidt S, Zbieg JR, Lacap JA, Zang R, Miller GM, Zhang Y, Beroza P, Reja R, Lee W, Tom JYK, Fong R, Steffek M, Clausen S, Hagenbeek TJ, Hu T, Zhou Z, Shen HC, Cunningham CN. Holden JK, et al. Among authors: steffek m. Cell Rep. 2020 Jun 23;31(12):107809. doi: 10.1016/j.celrep.2020.107809. Cell Rep. 2020. PMID: 32579935 Free article.
Conformation-locking antibodies for the discovery and characterization of KRAS inhibitors.
Davies CW, Oh AJ, Mroue R, Steffek M, Bruning JM, Xiao Y, Feng S, Jayakar S, Chan E, Arumugam V, Uribe SC, Drummond J, Frommlet A, Lu C, Franke Y, Merchant M, Koeppen H, Quinn JG, Malhotra S, Do S, Gazzard L, Purkey HE, Rudolph J, Mulvihill MM, Koerber JT, Wang W, Evangelista M. Davies CW, et al. Among authors: steffek m. Nat Biotechnol. 2022 May;40(5):769-778. doi: 10.1038/s41587-021-01126-9. Epub 2022 Jan 6. Nat Biotechnol. 2022. PMID: 34992247
Allosteric peptides bind a caspase zymogen and mediate caspase tetramerization.
Stanger K, Steffek M, Zhou L, Pozniak CD, Quan C, Franke Y, Tom J, Tam C, Krylova I, Elliott JM, Lewcock JW, Zhang Y, Murray J, Hannoush RN. Stanger K, et al. Among authors: steffek m. Nat Chem Biol. 2012 Jul;8(7):655-60. doi: 10.1038/nchembio.967. Epub 2012 Jun 10. Nat Chem Biol. 2012. PMID: 22683611
Conformational dynamics control ubiquitin-deubiquitinase interactions and influence in vivo signaling.
Phillips AH, Zhang Y, Cunningham CN, Zhou L, Forrest WF, Liu PS, Steffek M, Lee J, Tam C, Helgason E, Murray JM, Kirkpatrick DS, Fairbrother WJ, Corn JE. Phillips AH, et al. Among authors: steffek m. Proc Natl Acad Sci U S A. 2013 Jul 9;110(28):11379-84. doi: 10.1073/pnas.1302407110. Epub 2013 Jun 25. Proc Natl Acad Sci U S A. 2013. PMID: 23801757 Free PMC article.
Tailoring small molecules for an allosteric site on procaspase-6.
Murray J, Giannetti AM, Steffek M, Gibbons P, Hearn BR, Cohen F, Tam C, Pozniak C, Bravo B, Lewcock J, Jaishankar P, Ly CQ, Zhao X, Tang Y, Chugha P, Arkin MR, Flygare J, Renslo AR. Murray J, et al. Among authors: steffek m. ChemMedChem. 2014 Jan;9(1):73-7, 2. doi: 10.1002/cmdc.201300424. Epub 2013 Nov 20. ChemMedChem. 2014. PMID: 24259468
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. Biochemistry. 2023 Feb 7;62(3):633-644. doi: 10.1021/acs.biochem.1c00682. Epub 2022 Jan 5. Biochemistry. 2023. PMID: 34985287 Free article.
40 results