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Discovery of first-in-class inhibitors of ASH1L histone methyltransferase with anti-leukemic activity.
Rogawski DS, Deng J, Li H, Miao H, Borkin D, Purohit T, Song J, Chase J, Li S, Ndoj J, Klossowski S, Kim E, Mao F, Zhou B, Ropa J, Krotoska MZ, Jin Z, Ernst P, Feng X, Huang G, Nishioka K, Kelly S, He M, Wen B, Sun D, Muntean A, Dou Y, Maillard I, Cierpicki T, Grembecka J. Rogawski DS, et al. Among authors: purohit t. Nat Commun. 2021 May 14;12(1):2792. doi: 10.1038/s41467-021-23152-6. Nat Commun. 2021. PMID: 33990599 Free PMC article.
Menin-MLL inhibitors reverse oncogenic activity of MLL fusion proteins in leukemia.
Grembecka J, He S, Shi A, Purohit T, Muntean AG, Sorenson RJ, Showalter HD, Murai MJ, Belcher AM, Hartley T, Hess JL, Cierpicki T. Grembecka J, et al. Among authors: purohit t. Nat Chem Biol. 2012 Jan 29;8(3):277-84. doi: 10.1038/nchembio.773. Nat Chem Biol. 2012. PMID: 22286128 Free PMC article.
Pharmacologic inhibition of the Menin-MLL interaction blocks progression of MLL leukemia in vivo.
Borkin D, He S, Miao H, Kempinska K, Pollock J, Chase J, Purohit T, Malik B, Zhao T, Wang J, Wen B, Zong H, Jones M, Danet-Desnoyers G, Guzman ML, Talpaz M, Bixby DL, Sun D, Hess JL, Muntean AG, Maillard I, Cierpicki T, Grembecka J. Borkin D, et al. Among authors: purohit t. Cancer Cell. 2015 Apr 13;27(4):589-602. doi: 10.1016/j.ccell.2015.02.016. Epub 2015 Mar 26. Cancer Cell. 2015. PMID: 25817203 Free PMC article.
Menin-MLL inhibitors block oncogenic transformation by MLL-fusion proteins in a fusion partner-independent manner.
He S, Malik B, Borkin D, Miao H, Shukla S, Kempinska K, Purohit T, Wang J, Chen L, Parkin B, Malek SN, Danet-Desnoyers G, Muntean AG, Cierpicki T, Grembecka J. He S, et al. Among authors: purohit t. Leukemia. 2016 Feb;30(2):508-13. doi: 10.1038/leu.2015.144. Epub 2015 Jun 18. Leukemia. 2016. PMID: 26084867 Free PMC article. No abstract available.
Property Focused Structure-Based Optimization of Small Molecule Inhibitors of the Protein-Protein Interaction between Menin and Mixed Lineage Leukemia (MLL).
Borkin D, Pollock J, Kempinska K, Purohit T, Li X, Wen B, Zhao T, Miao H, Shukla S, He M, Sun D, Cierpicki T, Grembecka J. Borkin D, et al. Among authors: purohit t. J Med Chem. 2016 Feb 11;59(3):892-913. doi: 10.1021/acs.jmedchem.5b01305. Epub 2016 Jan 25. J Med Chem. 2016. PMID: 26744767 Free PMC article.
47 results