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106 results

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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: tansey wp. 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
Discovery and Structure-Based Optimization of Potent and Selective WD Repeat Domain 5 (WDR5) Inhibitors Containing a Dihydroisoquinolinone Bicyclic Core.
Tian J, Teuscher KB, Aho ER, Alvarado JR, Mills JJ, Meyers KM, Gogliotti RD, Han C, Macdonald JD, Sai J, Shaw JG, Sensintaffar JL, Zhao B, Rietz TA, Thomas LR, Payne WG, Moore WJ, Stott GM, Kondo J, Inoue M, Coffey RJ, Tansey WP, Stauffer SR, Lee T, Fesik SW. Tian J, et al. Among authors: tansey wp. J Med Chem. 2020 Jan 23;63(2):656-675. doi: 10.1021/acs.jmedchem.9b01608. Epub 2020 Jan 7. J Med Chem. 2020. PMID: 31858797 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: tansey wp. 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: tansey wp. 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: tansey wp. Elife. 2024 Apr 29;12:RP90683. doi: 10.7554/eLife.90683. Elife. 2024. PMID: 38682900 Free PMC article.
The MYC-WDR5 Nexus and Cancer.
Thomas LR, Foshage AM, Weissmiller AM, Tansey WP. Thomas LR, et al. Among authors: tansey wp. Cancer Res. 2015 Oct 1;75(19):4012-5. doi: 10.1158/0008-5472.CAN-15-1216. Epub 2015 Sep 17. Cancer Res. 2015. PMID: 26383167 Free PMC article. Review.
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: tansey wp. 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: tansey wp. Nat Commun. 2019 May 1;10(1):2014. doi: 10.1038/s41467-019-10022-5. Nat Commun. 2019. PMID: 31043611 Free PMC article.
106 results