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Page 1
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: stauffer sr. 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.
Exploration of allosteric agonism structure-activity relationships within an acetylene series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs): discovery of 5-((3-fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl)picolinamide (ML254).
Turlington M, Noetzel MJ, Chun A, Zhou Y, Gogliotti RD, Nguyen ED, Gregory KJ, Vinson PN, Rook JM, Gogi KK, Xiang Z, Bridges TM, Daniels JS, Jones C, Niswender CM, Meiler J, Conn PJ, Lindsley CW, Stauffer SR. Turlington M, et al. Among authors: stauffer sr. J Med Chem. 2013 Oct 24;56(20):7976-96. doi: 10.1021/jm401028t. Epub 2013 Oct 9. J Med Chem. 2013. PMID: 24050755 Free PMC article.
Discovery and SAR of muscarinic receptor subtype 1 (M1) allosteric activators from a molecular libraries high throughput screen. Part 1: 2,5-dibenzyl-2H-pyrazolo[4,3-c]quinolin-3(5H)-ones as positive allosteric modulators.
Han C, Chatterjee A, Noetzel MJ, Panarese JD, Smith E, Chase P, Hodder P, Niswender C, Conn PJ, Lindsley CW, Stauffer SR. Han C, et al. Among authors: stauffer sr. Bioorg Med Chem Lett. 2015 Jan 15;25(2):384-8. doi: 10.1016/j.bmcl.2014.11.011. Epub 2014 Nov 18. Bioorg Med Chem Lett. 2015. PMID: 25435150 Free PMC article.
Development of a Series of (1-Benzyl-3-(6-methoxypyrimidin-3-yl)-5-(trifluoromethoxy)-1H-indol-2-yl)methanols as Selective Protease Activated Receptor 4 (PAR4) Antagonists with in Vivo Utility and Activity Against γ-Thrombin.
Temple KJ, Duvernay MT, Young SE, Wen W, Wu W, Maeng JG, Blobaum AL, Stauffer SR, Hamm HE, Lindsley CW. Temple KJ, et al. Among authors: stauffer sr. J Med Chem. 2016 Aug 25;59(16):7690-5. doi: 10.1021/acs.jmedchem.6b00928. Epub 2016 Aug 8. J Med Chem. 2016. PMID: 27482618 Free PMC article.
Discovery of Potent 2-Aryl-6,7-dihydro-5 H-pyrrolo[1,2- a]imidazoles as WDR5-WIN-Site Inhibitors Using Fragment-Based Methods and Structure-Based Design.
Wang F, Jeon KO, Salovich JM, Macdonald JD, Alvarado J, Gogliotti RD, Phan J, Olejniczak ET, Sun Q, Wang S, Camper D, Yuh JP, Shaw JG, Sai J, Rossanese OW, Tansey WP, Stauffer SR, Fesik SW. Wang F, et al. Among authors: stauffer sr. J Med Chem. 2018 Jul 12;61(13):5623-5642. doi: 10.1021/acs.jmedchem.8b00375. Epub 2018 Jun 29. J Med Chem. 2018. PMID: 29889518 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: stauffer sr. 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: stauffer sr. 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 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: stauffer sr. 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.
115 results