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Sekikaic acid and lobaric acid target a dynamic interface of the coactivator CBP/p300.
Majmudar CY, Højfeldt JW, Arevang CJ, Pomerantz WC, Gagnon JK, Schultz PJ, Cesa LC, Doss CH, Rowe SP, Vásquez V, Tamayo-Castillo G, Cierpicki T, Brooks CL 3rd, Sherman DH, Mapp AK. Majmudar CY, et al. Among authors: cierpicki t. Angew Chem Int Ed Engl. 2012 Nov 5;51(45):11258-62. doi: 10.1002/anie.201206815. Epub 2012 Oct 8. Angew Chem Int Ed Engl. 2012. PMID: 23042634 Free PMC article.
Conservation of coactivator engagement mechanism enables small-molecule allosteric modulators.
Henderson AR, Henley MJ, Foster NJ, Peiffer AL, Beyersdorf MS, Stanford KD, Sturlis SM, Linhares BM, Hill ZB, Wells JA, Cierpicki T, Brooks CL 3rd, Fierke CA, Mapp AK. Henderson AR, et al. Among authors: cierpicki t. Proc Natl Acad Sci U S A. 2018 Sep 4;115(36):8960-8965. doi: 10.1073/pnas.1806202115. Epub 2018 Aug 20. Proc Natl Acad Sci U S A. 2018. PMID: 30127017 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: cierpicki t. 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.
A lipopeptidomimetic of transcriptional activation domains selectively disrupts Med25 PPIs.
Pattelli ON, Valdivia EM, Beyersdorf MS, Regan CS, Rivas M, Merajver SD, Cierpicki T, Mapp AK. Pattelli ON, et al. Among authors: cierpicki t. bioRxiv [Preprint]. 2023 Mar 25:2023.03.24.534168. doi: 10.1101/2023.03.24.534168. bioRxiv. 2023. Update in: Angew Chem Int Ed Engl. 2024 May 21;63(21):e202400781. doi: 10.1002/anie.202400781 PMID: 36993479 Free PMC article. Updated. Preprint.
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: cierpicki 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.
110 results