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Expanded profiling of WD repeat domain 5 inhibitors reveals actionable strategies for the treatment of hematologic malignancies.
Meyer CT, Smith BN, Wang J, Teuscher KB, Grieb BC, Howard GC, Silver AJ, Lorey SL, Stott GM, Moore WJ, Lee T, Savona MR, Weissmiller AM, Liu Q, Quaranta V, Fesik SW, Tansey WP. Meyer CT, et al. Among authors: lorey sl. Proc Natl Acad Sci U S A. 2024 Aug 27;121(35):e2408889121. doi: 10.1073/pnas.2408889121. Epub 2024 Aug 21. Proc Natl Acad Sci U S A. 2024. PMID: 39167600
WIN site inhibition disrupts a subset of WDR5 function.
Siladi AJ, Wang J, Florian AC, Thomas LR, Creighton JH, Matlock BK, Flaherty DK, Lorey SL, Howard GC, Fesik SW, Weissmiller AM, Liu Q, Tansey WP. Siladi AJ, et al. Among authors: lorey sl. Sci Rep. 2022 Feb 3;12(1):1848. doi: 10.1038/s41598-022-05947-9. Sci Rep. 2022. PMID: 35115608 Free PMC article.
Structure-based discovery of potent WD repeat domain 5 inhibitors that demonstrate efficacy and safety in preclinical animal models.
Teuscher KB, Chowdhury S, Meyers KM, Tian J, Sai J, Van Meveren M, South TM, Sensintaffar JL, Rietz TA, Goswami S, Wang J, Grieb BC, Lorey SL, Howard GC, Liu Q, Moore WJ, Stott GM, Tansey WP, Lee T, Fesik SW. Teuscher KB, et al. Among authors: lorey sl. Proc Natl Acad Sci U S A. 2023 Jan 3;120(1):e2211297120. doi: 10.1073/pnas.2211297120. Epub 2022 Dec 27. Proc Natl Acad Sci U S A. 2023. PMID: 36574664 Free PMC article.
Ribosome subunit attrition and activation of the p53-MDM4 axis dominate the response of MLL-rearranged cancer cells to WDR5 WIN site inhibition.
Howard GC, Wang J, Rose KL, Jones C, Patel P, Tsui T, Florian AC, Vlach L, Lorey SL, Grieb BC, Smith BN, Slota MJ, Reynolds EM, Goswami S, Savona MR, Mason FM, Lee T, Fesik S, Liu Q, Tansey WP. Howard GC, et al. Among authors: lorey sl. Elife. 2024 Apr 29;12:RP90683. doi: 10.7554/eLife.90683. Elife. 2024. PMID: 38682900 Free PMC article.
Displacement of WDR5 from Chromatin by a WIN Site Inhibitor with Picomolar Affinity.
Aho ER, Wang J, Gogliotti RD, Howard GC, Phan J, Acharya P, Macdonald JD, Cheng K, Lorey SL, Lu B, Wenzel S, Foshage AM, Alvarado J, Wang F, Shaw JG, Zhao B, Weissmiller AM, Thomas LR, Vakoc CR, Hall MD, Hiebert SW, Liu Q, Stauffer SR, Fesik SW, Tansey WP. Aho ER, et al. Among authors: lorey sl. Cell Rep. 2019 Mar 12;26(11):2916-2928.e13. doi: 10.1016/j.celrep.2019.02.047. Cell Rep. 2019. PMID: 30865883 Free PMC article.
Inhibition of MYC by the SMARCB1 tumor suppressor.
Weissmiller AM, Wang J, Lorey SL, Howard GC, Martinez E, Liu Q, Tansey WP. Weissmiller AM, et al. Among authors: lorey sl. Nat Commun. 2019 May 1;10(1):2014. doi: 10.1038/s41467-019-10022-5. Nat Commun. 2019. PMID: 31043611 Free PMC article.
WDR5 is a conserved regulator of protein synthesis gene expression.
Bryan AF, Wang J, Howard GC, Guarnaccia AD, Woodley CM, Aho ER, Rellinger EJ, Matlock BK, Flaherty DK, Lorey SL, Chung DH, Fesik SW, Liu Q, Weissmiller AM, Tansey WP. Bryan AF, et al. Among authors: lorey sl. Nucleic Acids Res. 2020 Apr 6;48(6):2924-2941. doi: 10.1093/nar/gkaa051. Nucleic Acids Res. 2020. PMID: 31996893 Free PMC article.
Impact of WIN site inhibitor on the WDR5 interactome.
Guarnaccia AD, Rose KL, Wang J, Zhao B, Popay TM, Wang CE, Guerrazzi K, Hill S, Woodley CM, Hansen TJ, Lorey SL, Shaw JG, Payne WG, Weissmiller AM, Olejniczak ET, Fesik SW, Liu Q, Tansey WP. Guarnaccia AD, et al. Among authors: lorey sl. Cell Rep. 2021 Jan 19;34(3):108636. doi: 10.1016/j.celrep.2020.108636. Cell Rep. 2021. PMID: 33472061 Free PMC article.
26 results