Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation

Search Page

Filters

My NCBI Filters

Text availability

Article attribute

Article type

Publication date

Search Results

83 results

Filters applied: . Clear all
Results are displayed in a computed author sort order. The Results By Year timeline is not available.
Page 1
Discovery of WD Repeat-Containing Protein 5 (WDR5)-MYC Inhibitors Using Fragment-Based Methods and Structure-Based Design.
Chacón Simon S, Wang F, Thomas LR, Phan J, Zhao B, Olejniczak ET, Macdonald JD, Shaw JG, Schlund C, Payne W, Creighton J, Stauffer SR, Waterson AG, Tansey WP, Fesik SW. Chacón Simon S, et al. Among authors: thomas lr. J Med Chem. 2020 Apr 23;63(8):4315-4333. doi: 10.1021/acs.jmedchem.0c00224. Epub 2020 Apr 9. J Med Chem. 2020. PMID: 32223236 Free PMC article.
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. 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.
The MYC-WDR5 Nexus and Cancer.
Thomas LR, Foshage AM, Weissmiller AM, Tansey WP. Thomas LR, et al. 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: thomas lr. 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.
Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5-MYC Protein-Protein Interaction.
Macdonald JD, Chacón Simon S, Han C, Wang F, Shaw JG, Howes JE, Sai J, Yuh JP, Camper D, Alicie BM, Alvarado J, Nikhar S, Payne W, Aho ER, Bauer JA, Zhao B, Phan J, Thomas LR, Rossanese OW, Tansey WP, Waterson AG, Stauffer SR, Fesik SW. Macdonald JD, et al. Among authors: thomas lr. J Med Chem. 2019 Dec 26;62(24):11232-11259. doi: 10.1021/acs.jmedchem.9b01411. Epub 2019 Dec 5. J Med Chem. 2019. PMID: 31724864 Free PMC article.
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: thomas lr. 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.
Targeting MYC through WDR5.
Thomas LR, Adams CM, Fesik SW, Eischen CM, Tansey WP. Thomas LR, et al. Mol Cell Oncol. 2020 Jan 10;7(2):1709388. doi: 10.1080/23723556.2019.1709388. eCollection 2020. Mol Cell Oncol. 2020. PMID: 32158922 Free PMC article.
A common functional consequence of tumor-derived mutations within c-MYC.
Chakraborty AA, Scuoppo C, Dey S, Thomas LR, Lorey SL, Lowe SW, Tansey WP. Chakraborty AA, et al. Among authors: thomas lr. Oncogene. 2015 Apr 30;34(18):2406-9. doi: 10.1038/onc.2014.186. Epub 2014 Jul 7. Oncogene. 2015. PMID: 24998853 Free PMC article.
83 results