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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. Elife. 2024 Apr 29;12:RP90683. doi: 10.7554/eLife.90683. Elife. 2024. PMID: 38682900 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 SW, Liu Q, Tansey WP. Howard GC, et al. bioRxiv [Preprint]. 2024 Jan 10:2023.07.26.550648. doi: 10.1101/2023.07.26.550648. bioRxiv. 2024. Update in: Elife. 2024 Apr 29;12:RP90683. doi: 10.7554/eLife.90683. PMID: 37546802 Free PMC article. Updated. Preprint.
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: howard gc. 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.
Synergistic action of WDR5 and HDM2 inhibitors in SMARCB1-deficient cancer cells.
Florian AC, Woodley CM, Wang J, Grieb BC, Slota MJ, Guerrazzi K, Hsu CY, Matlock BK, Flaherty DK, Lorey SL, Fesik SW, Howard GC, Liu Q, Weissmiller AM, Tansey WP. Florian AC, et al. Among authors: howard gc. NAR Cancer. 2022 Mar 3;4(1):zcac007. doi: 10.1093/narcan/zcac007. eCollection 2022 Mar. NAR Cancer. 2022. PMID: 35252869 Free PMC article.
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: howard gc. Sci Rep. 2022 Feb 3;12(1):1848. doi: 10.1038/s41598-022-05947-9. Sci Rep. 2022. PMID: 35115608 Free PMC article.
82 results