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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: kempinska k. 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.
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: kempinska k. 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.
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: kempinska k. 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.
Complexity of Blocking Bivalent Protein-Protein Interactions: Development of a Highly Potent Inhibitor of the Menin-Mixed-Lineage Leukemia Interaction.
Borkin D, Klossowski S, Pollock J, Miao H, Linhares BM, Kempinska K, Jin Z, Purohit T, Wen B, He M, Sun D, Cierpicki T, Grembecka J. Borkin D, et al. Among authors: kempinska k. J Med Chem. 2018 Jun 14;61(11):4832-4850. doi: 10.1021/acs.jmedchem.8b00071. Epub 2018 May 23. J Med Chem. 2018. PMID: 29738674 Free PMC article.
Menin inhibitor MI-3454 induces remission in MLL1-rearranged and NPM1-mutated models of leukemia.
Klossowski S, Miao H, Kempinska K, Wu T, Purohit T, Kim E, Linhares BM, Chen D, Jih G, Perkey E, Huang H, He M, Wen B, Wang Y, Yu K, Lee SC, Danet-Desnoyers G, Trotman W, Kandarpa M, Cotton A, Abdel-Wahab O, Lei H, Dou Y, Guzman M, Peterson L, Gruber T, Choi S, Sun D, Ren P, Li LS, Liu Y, Burrows F, Maillard I, Cierpicki T, Grembecka J. Klossowski S, et al. Among authors: kempinska k. J Clin Invest. 2020 Feb 3;130(2):981-997. doi: 10.1172/JCI129126. J Clin Invest. 2020. PMID: 31855575 Free PMC article.
Covalent inhibition of NSD1 histone methyltransferase.
Huang H, Howard CA, Zari S, Cho HJ, Shukla S, Li H, Ndoj J, González-Alonso P, Nikolaidis C, Abbott J, Rogawski DS, Potopnyk MA, Kempinska K, Miao H, Purohit T, Henderson A, Mapp A, Sulis ML, Ferrando A, Grembecka J, Cierpicki T. Huang H, et al. Among authors: kempinska k. Nat Chem Biol. 2020 Dec;16(12):1403-1410. doi: 10.1038/s41589-020-0626-6. Epub 2020 Aug 31. Nat Chem Biol. 2020. PMID: 32868895 Free PMC article.
[No title available]
[No authors listed] [No authors listed] PMID: 33024997
16 results