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Page 1
Structure-Based Optimization of Small Molecule Human Galactokinase Inhibitors.
Liu L, Tang M, Pragani R, Whitby FG, Zhang YQ, Balakrishnan B, Fang Y, Karavadhi S, Tao D, LeClair CA, Hall MD, Marugan JJ, Boxer M, Shen M, Hill CP, Lai K, Patnaik S. Liu L, et al. Among authors: pragani r. J Med Chem. 2021 Sep 23;64(18):13551-13571. doi: 10.1021/acs.jmedchem.1c00945. Epub 2021 Sep 7. J Med Chem. 2021. PMID: 34491744 Free PMC article.
Biochemical, cellular, and biophysical characterization of a potent inhibitor of mutant isocitrate dehydrogenase IDH1.
Davis MI, Gross S, Shen M, Straley KS, Pragani R, Lea WA, Popovici-Muller J, DeLaBarre B, Artin E, Thorne N, Auld DS, Li Z, Dang L, Boxer MB, Simeonov A. Davis MI, et al. Among authors: pragani r. J Biol Chem. 2014 May 16;289(20):13717-25. doi: 10.1074/jbc.M113.511030. Epub 2014 Mar 25. J Biol Chem. 2014. PMID: 24668804 Free PMC article.
Structure activity relationships of human galactokinase inhibitors.
Liu L, Tang M, Walsh MJ, Brimacombe KR, Pragani R, Tanega C, Rohde JM, Baker HL, Fernandez E, Blackman B, Bougie JM, Leister WH, Auld DS, Shen M, Lai K, Boxer MB. Liu L, et al. Among authors: pragani r. Bioorg Med Chem Lett. 2015 Feb 1;25(3):721-7. doi: 10.1016/j.bmcl.2014.11.061. Epub 2014 Dec 13. Bioorg Med Chem Lett. 2015. PMID: 25553891
Breaking Cryo-EM Resolution Barriers to Facilitate Drug Discovery.
Merk A, Bartesaghi A, Banerjee S, Falconieri V, Rao P, Davis MI, Pragani R, Boxer MB, Earl LA, Milne JLS, Subramaniam S. Merk A, et al. Among authors: pragani r. Cell. 2016 Jun 16;165(7):1698-1707. doi: 10.1016/j.cell.2016.05.040. Epub 2016 May 26. Cell. 2016. PMID: 27238019 Free PMC article.
Small Molecule Inhibition of the Ubiquitin-specific Protease USP2 Accelerates cyclin D1 Degradation and Leads to Cell Cycle Arrest in Colorectal Cancer and Mantle Cell Lymphoma Models.
Davis MI, Pragani R, Fox JT, Shen M, Parmar K, Gaudiano EF, Liu L, Tanega C, McGee L, Hall MD, McKnight C, Shinn P, Nelson H, Chattopadhyay D, D'Andrea AD, Auld DS, DeLucas LJ, Li Z, Boxer MB, Simeonov A. Davis MI, et al. Among authors: pragani r. J Biol Chem. 2016 Nov 18;291(47):24628-24640. doi: 10.1074/jbc.M116.738567. Epub 2016 Sep 28. J Biol Chem. 2016. PMID: 27681596 Free PMC article.
Assessing inhibitors of mutant isocitrate dehydrogenase using a suite of pre-clinical discovery assays.
Urban DJ, Martinez NJ, Davis MI, Brimacombe KR, Cheff DM, Lee TD, Henderson MJ, Titus SA, Pragani R, Rohde JM, Liu L, Fang Y, Karavadhi S, Shah P, Lee OW, Wang A, McIver A, Zheng H, Wang X, Xu X, Jadhav A, Simeonov A, Shen M, Boxer MB, Hall MD. Urban DJ, et al. Among authors: pragani r. Sci Rep. 2017 Oct 6;7(1):12758. doi: 10.1038/s41598-017-12630-x. Sci Rep. 2017. PMID: 28986582 Free PMC article.
Discovery and Optimization of 2H-1λ2-Pyridin-2-one Inhibitors of Mutant Isocitrate Dehydrogenase 1 for the Treatment of Cancer.
Rohde JM, Karavadhi S, Pragani R, Liu L, Fang Y, Zhang W, McIver A, Zheng H, Liu Q, Davis MI, Urban DJ, Lee TD, Cheff DM, Hollingshead M, Henderson MJ, Martinez NJ, Brimacombe KR, Yasgar A, Zhao W, Klumpp-Thomas C, Michael S, Covey J, Moore WJ, Stott GM, Li Z, Simeonov A, Jadhav A, Frye S, Hall MD, Shen M, Wang X, Patnaik S, Boxer MB. Rohde JM, et al. Among authors: pragani r. J Med Chem. 2021 Apr 22;64(8):4913-4946. doi: 10.1021/acs.jmedchem.1c00019. Epub 2021 Apr 6. J Med Chem. 2021. PMID: 33822623 Free PMC article.
Multimodal action of KRP203 on phosphoinositide kinases in vitro and in cells.
Ikeda Y, Davis MI, Sumita K, Zheng Y, Kofuji S, Sasaki M, Hirota Y, Pragani R, Shen M, Boxer MB, Takeuchi K, Senda T, Simeonov A, Sasaki AT. Ikeda Y, et al. Among authors: pragani r. Biochem Biophys Res Commun. 2023 Oct 30;679:116-121. doi: 10.1016/j.bbrc.2023.08.050. Epub 2023 Aug 26. Biochem Biophys Res Commun. 2023. PMID: 37683456 Free PMC article.
A high dose KRP203 induces cytoplasmic vacuoles associated with altered phosphoinositide segregation and endosome expansion.
Kofuji S, Wolfe K, Sumita K, Kageyama S, Yoshino H, Hirota Y, Ogawa-Iio A, Kanoh H, Sasaki M, Kofuji K, Davis MI, Pragani R, Shen M, Boxer MB, Nakatsu F, Nigorikawa K, Sasaki T, Takeuchi K, Senda T, Kim SM, Edinger AL, Simeonov A, Sasaki AT. Kofuji S, et al. Among authors: pragani r. Biochem Biophys Res Commun. 2024 Jul 23;718:149981. doi: 10.1016/j.bbrc.2024.149981. Epub 2024 Apr 27. Biochem Biophys Res Commun. 2024. PMID: 38735134
17 results