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Page 1
Molecular glues that inhibit deubiquitylase activity and inflammatory signalling.
Chandler F, Reddy PAN, Bhutda S, Ross RL, Datta A, Walden M, Walker K, Di Donato S, Cassel JA, Prakesch MA, Aman A, Datti A, Campbell LJ, Foglizzo M, Bell L, Stein DN, Ault JR, Al-Awar RS, Calabrese AN, Sicheri F, Del Galdo F, Salvino JM, Greenberg RA, Zeqiraj E. Chandler F, et al. Among authors: prakesch ma. bioRxiv [Preprint]. 2024 Nov 15:2024.09.07.611787. doi: 10.1101/2024.09.07.611787. bioRxiv. 2024. PMID: 39282282 Free PMC article. Preprint.
A drug discovery platform to identify compounds that inhibit EGFR triple mutants.
Saraon P, Snider J, Kalaidzidis Y, Wybenga-Groot LE, Weiss K, Rai A, Radulovich N, Drecun L, Vučković N, Vučetić A, Wong V, Thériault B, Pham NA, Park JH, Datti A, Wang J, Pathmanathan S, Aboualizadeh F, Lyakisheva A, Yao Z, Wang Y, Joseph B, Aman A, Moran MF, Prakesch M, Poda G, Marcellus R, Uehling D, Samaržija M, Jakopović M, Tsao MS, Shepherd FA, Sacher A, Leighl N, Akhmanova A, Al-Awar R, Zerial M, Stagljar I. Saraon P, et al. Nat Chem Biol. 2020 May;16(5):577-586. doi: 10.1038/s41589-020-0484-2. Epub 2020 Feb 24. Nat Chem Biol. 2020. PMID: 32094923 Free PMC article.
Chemical Genetics Screen Identifies COPB2 Tool Compounds That Alters ER Stress Response and Induces RTK Dysregulation in Lung Cancer Cells.
Saraon P, Snider J, Schormann W, Rai A, Radulovich N, Sánchez-Osuna M, Coulombe-Huntington J, Huard C, Mohammed M, Lima-Fernandes E, Thériault B, Halabelian L, Chan M, Joshi D, Drecun L, Yao Z, Pathmanathan S, Wong V, Lyakisheva A, Aboualizadeh F, Niu L, Li F, Kiyota T, Subramanian R, Joseph B, Aman A, Prakesch M, Isaac M, Mamai A, Poda G, Vedadi M, Marcellus R, Uehling D, Leighl N, Sacher A, Samaržija M, Jakopović M, Arrowsmith C, Tyers M, Tsao MS, Andrews D, Al-Awar R, Stagljar I. Saraon P, et al. J Mol Biol. 2021 Nov 19;433(23):167294. doi: 10.1016/j.jmb.2021.167294. Epub 2021 Oct 16. J Mol Biol. 2021. PMID: 34662547
Functional characterization of a PROTAC directed against BRAF mutant V600E.
Posternak G, Tang X, Maisonneuve P, Jin T, Lavoie H, Daou S, Orlicky S, Goullet de Rugy T, Caldwell L, Chan K, Aman A, Prakesch M, Poda G, Mader P, Wong C, Maier S, Kitaygorodsky J, Larsen B, Colwill K, Yin Z, Ceccarelli DF, Batey RA, Taipale M, Kurinov I, Uehling D, Wrana J, Durocher D, Gingras AC, Al-Awar R, Therrien M, Sicheri F. Posternak G, et al. Nat Chem Biol. 2020 Nov;16(11):1170-1178. doi: 10.1038/s41589-020-0609-7. Epub 2020 Aug 10. Nat Chem Biol. 2020. PMID: 32778845 Free PMC article.
Structure and mechanism of action of the hydroxy-aryl-aldehyde class of IRE1 endoribonuclease inhibitors.
Sanches M, Duffy NM, Talukdar M, Thevakumaran N, Chiovitti D, Canny MD, Lee K, Kurinov I, Uehling D, Al-awar R, Poda G, Prakesch M, Wilson B, Tam V, Schweitzer C, Toro A, Lucas JL, Vuga D, Lehmann L, Durocher D, Zeng Q, Patterson JB, Sicheri F. Sanches M, et al. Nat Commun. 2014 Aug 28;5:4202. doi: 10.1038/ncomms5202. Nat Commun. 2014. PMID: 25164867 Free PMC article.
Design, Synthesis, and Characterization of 4-Aminoquinazolines as Potent Inhibitors of the G Protein-Coupled Receptor Kinase 6 (GRK6) for the Treatment of Multiple Myeloma.
Uehling DE, Joseph B, Chung KC, Zhang AX, Ler S, Prakesch MA, Poda G, Grouleff J, Aman A, Kiyota T, Leung-Hagesteijn C, Konda JD, Marcellus R, Griffin C, Subramaniam R, Abibi A, Strathdee CA, Isaac MB, Al-Awar R, Tiedemann RE. Uehling DE, et al. Among authors: prakesch ma. J Med Chem. 2021 Aug 12;64(15):11129-11147. doi: 10.1021/acs.jmedchem.1c00506. Epub 2021 Jul 22. J Med Chem. 2021. PMID: 34291633
Discovery of OICR12694: A Novel, Potent, Selective, and Orally Bioavailable BCL6 BTB Inhibitor.
Mamai A, Chau AM, Wilson BJ, Watson ID, Joseph BB, Subramanian PR, Morshed MM, Morin JA, Prakesch MA, Lu T, Connolly P, Kuntz DA, Pomroy NC, Poda G, Nguyen K, Marcellus R, Strathdee G, Theriault B, Subramaniam R, Mohammed M, Abibi A, Chan M, Winston J, Kiyota T, Undzys E, Aman A, Austin N, Du Jardin M, Packman K, Phillippar U, Attar R, Edwards J, O'Meara J, Uehling DE, Al-Awar R, Privé GG, Isaac MB. Mamai A, et al. Among authors: prakesch ma. ACS Med Chem Lett. 2023 Jan 12;14(2):199-210. doi: 10.1021/acsmedchemlett.2c00502. eCollection 2023 Feb 9. ACS Med Chem Lett. 2023. PMID: 36793435 Free PMC article.
Correction to "Design, Synthesis, and Characterization of 4-Aminoquinazolines as Potent Inhibitors of the G Protein-Coupled Receptor Kinase 6 (GRK6) for the Treatment of Multiple Myeloma".
Uehling DE, Joseph B, Chung KC, Zhang AX, Ler S, Prakesch MA, Poda G, Grouleff J, Aman A, Kiyota T, Leung-Hagesteijn C, Konda JD, Marcellus R, Griffin C, Subramaniam R, Abibi A, Strathdee CA, Isaac MB, Al-Awar R, Tiedemann RE. Uehling DE, et al. Among authors: prakesch ma. J Med Chem. 2022 Jan 13;65(1):886-887. doi: 10.1021/acs.jmedchem.1c02066. Epub 2021 Dec 28. J Med Chem. 2022. PMID: 34963044 No abstract available.
13 results