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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: howard gc. 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: 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.
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.
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.
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: howard gc. 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: howard gc. 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: howard gc. Nucleic Acids Res. 2020 Apr 6;48(6):2924-2941. doi: 10.1093/nar/gkaa051. Nucleic Acids Res. 2020. PMID: 31996893 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.
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.
Interaction with WDR5 promotes target gene recognition and tumorigenesis by MYC.
Thomas LR, Wang Q, Grieb BC, Phan J, Foshage AM, Sun Q, Olejniczak ET, Clark T, Dey S, Lorey S, Alicie B, Howard GC, Cawthon B, Ess KC, Eischen CM, Zhao Z, Fesik SW, Tansey WP. Thomas LR, et al. Among authors: howard gc. Mol Cell. 2015 May 7;58(3):440-52. doi: 10.1016/j.molcel.2015.02.028. Epub 2015 Mar 26. Mol Cell. 2015. PMID: 25818646 Free PMC article.
83 results