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Discovery of HDAC6-Selective Inhibitor NN-390 with in Vitro Efficacy in Group 3 Medulloblastoma.
Nawar N, Bukhari S, Adile AA, Suk Y, Manaswiyoungkul P, Toutah K, Olaoye OO, Raouf YS, Sedighi A, Garcha HK, Hassan MM, Gwynne W, Israelian J, Radu TB, Geletu M, Abdeldayem A, Gawel JM, Cabral AD, Venugopal C, de Araujo ED, Singh SK, Gunning PT. Nawar N, et al. Among authors: geletu m. J Med Chem. 2022 Feb 24;65(4):3193-3217. doi: 10.1021/acs.jmedchem.1c01585. Epub 2022 Feb 4. J Med Chem. 2022. PMID: 35119267
Unique Molecular Interaction with the Histone Deacetylase 6 Catalytic Tunnel: Crystallographic and Biological Characterization of a Model Chemotype.
Olaoye OO, Watson PR, Nawar N, Geletu M, Sedighi A, Bukhari S, Raouf YS, Manaswiyoungkul P, Erdogan F, Abdeldayem A, Cabral AD, Hassan MM, Toutah K, Shouksmith AE, Gawel JM, Israelian J, Radu TB, Kachhiyapatel N, de Araujo ED, Christianson DW, Gunning PT. Olaoye OO, et al. Among authors: geletu m. J Med Chem. 2021 Mar 11;64(5):2691-2704. doi: 10.1021/acs.jmedchem.0c01922. Epub 2021 Feb 12. J Med Chem. 2021. PMID: 33576627 Free PMC article.
Development of HDAC Inhibitors Exhibiting Therapeutic Potential in T-Cell Prolymphocytic Leukemia.
Toutah K, Nawar N, Timonen S, Sorger H, Raouf YS, Bukhari S, von Jan J, Ianevski A, Gawel JM, Olaoye OO, Geletu M, Abdeldayem A, Israelian J, Radu TB, Sedighi A, Bhatti MN, Hassan MM, Manaswiyoungkul P, Shouksmith AE, Neubauer HA, de Araujo ED, Aittokallio T, Krämer OH, Moriggl R, Mustjoki S, Herling M, Gunning PT. Toutah K, et al. Among authors: geletu m. J Med Chem. 2021 Jun 24;64(12):8486-8509. doi: 10.1021/acs.jmedchem.1c00420. Epub 2021 Jun 8. J Med Chem. 2021. PMID: 34101461 Free PMC article.
A selective inhibitor of the UFM1-activating enzyme, UBA5.
da Silva SR, Paiva SL, Bancerz M, Geletu M, Lewis AM, Chen J, Cai Y, Lukkarila JL, Li H, Gunning PT. da Silva SR, et al. Among authors: geletu m. Bioorg Med Chem Lett. 2016 Sep 15;26(18):4542-4547. doi: 10.1016/j.bmcl.2015.10.015. Epub 2015 Oct 8. Bioorg Med Chem Lett. 2016. PMID: 27520940
Identification and Characterization of AES-135, a Hydroxamic Acid-Based HDAC Inhibitor That Prolongs Survival in an Orthotopic Mouse Model of Pancreatic Cancer.
Shouksmith AE, Shah F, Grimard ML, Gawel JM, Raouf YS, Geletu M, Berger-Becvar A, de Araujo ED, Luchman HA, Heaton WL, Bakhshinyan D, Adile AA, Venugopal C, O'Hare T, Deininger MW, Singh SK, Konieczny SF, Weiss S, Fishel ML, Gunning PT. Shouksmith AE, et al. Among authors: geletu m. J Med Chem. 2019 Mar 14;62(5):2651-2665. doi: 10.1021/acs.jmedchem.8b01957. Epub 2019 Mar 6. J Med Chem. 2019. PMID: 30776234 Free PMC article.
Nanomolar-Potency Small Molecule Inhibitor of STAT5 Protein.
Cumaraswamy AA, Lewis AM, Geletu M, Todic A, Diaz DB, Cheng XR, Brown CE, Laister RC, Muench D, Kerman K, Grimes HL, Minden MD, Gunning PT. Cumaraswamy AA, et al. Among authors: geletu m. ACS Med Chem Lett. 2014 Sep 19;5(11):1202-1206. doi: 10.1021/ml500165r. eCollection 2014 Nov 13. ACS Med Chem Lett. 2014. PMID: 25419444 Free PMC article.
STAT3 pathway regulates lung-derived brain metastasis initiating cell capacity through miR-21 activation.
Singh M, Garg N, Venugopal C, Hallett R, Tokar T, McFarlane N, Mahendram S, Bakhshinyan D, Manoranjan B, Vora P, Qazi M, Arpin CC, Page B, Haftchenary S, Rosa DA, Lai PS, Gómez-Biagi RF, Ali AM, Lewis A, Geletu M, Murty NK, Hassell JA, Jurisica I, Gunning PT, Singh SK. Singh M, et al. Among authors: geletu m. Oncotarget. 2015 Sep 29;6(29):27461-77. doi: 10.18632/oncotarget.4742. Oncotarget. 2015. PMID: 26314961 Free PMC article.
44 results