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Discovery of 5-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-(tert-butyl)pyridine-3-sulfonamide (CZC24758), as a potent, orally bioavailable and selective inhibitor of PI3K for the treatment of inflammatory disease.
Sunose M, Bell K, Ellard K, Bergamini G, Neubauer G, Werner T, Ramsden N. Sunose M, et al. Among authors: bergamini g. Bioorg Med Chem Lett. 2012 Jul 15;22(14):4613-8. doi: 10.1016/j.bmcl.2012.05.090. Epub 2012 Jun 5. Bioorg Med Chem Lett. 2012. PMID: 22726925
Chemoproteomics profiling of HDAC inhibitors reveals selective targeting of HDAC complexes.
Bantscheff M, Hopf C, Savitski MM, Dittmann A, Grandi P, Michon AM, Schlegl J, Abraham Y, Becher I, Bergamini G, Boesche M, Delling M, Dümpelfeld B, Eberhard D, Huthmacher C, Mathieson T, Poeckel D, Reader V, Strunk K, Sweetman G, Kruse U, Neubauer G, Ramsden NG, Drewes G. Bantscheff M, et al. Among authors: bergamini g. Nat Biotechnol. 2011 Mar;29(3):255-65. doi: 10.1038/nbt.1759. Epub 2011 Jan 23. Nat Biotechnol. 2011. PMID: 21258344
A selective inhibitor reveals PI3Kγ dependence of T(H)17 cell differentiation.
Bergamini G, Bell K, Shimamura S, Werner T, Cansfield A, Müller K, Perrin J, Rau C, Ellard K, Hopf C, Doce C, Leggate D, Mangano R, Mathieson T, O'Mahony A, Plavec I, Rharbaoui F, Reinhard F, Savitski MM, Ramsden N, Hirsch E, Drewes G, Rausch O, Bantscheff M, Neubauer G. Bergamini G, et al. Nat Chem Biol. 2012 Apr 29;8(6):576-82. doi: 10.1038/nchembio.957. Nat Chem Biol. 2012. PMID: 22544264
CZ415, a Highly Selective mTOR Inhibitor Showing in Vivo Efficacy in a Collagen Induced Arthritis Model.
Cansfield AD, Ladduwahetty T, Sunose M, Ellard K, Lynch R, Newton AL, Lewis A, Bennett G, Zinn N, Thomson DW, Rüger AJ, Feutrill JT, Rausch O, Watt AP, Bergamini G. Cansfield AD, et al. Among authors: bergamini g. ACS Med Chem Lett. 2016 Jun 10;7(8):768-73. doi: 10.1021/acsmedchemlett.6b00149. eCollection 2016 Aug 11. ACS Med Chem Lett. 2016. PMID: 27563401 Free PMC article.
Discovery of GSK8612, a Highly Selective and Potent TBK1 Inhibitor.
Thomson DW, Poeckel D, Zinn N, Rau C, Strohmer K, Wagner AJ, Graves AP, Perrin J, Bantscheff M, Duempelfeld B, Kasparcova V, Ramanjulu JM, Pesiridis GS, Muelbaier M, Bergamini G. Thomson DW, et al. Among authors: bergamini g. ACS Med Chem Lett. 2019 Mar 11;10(5):780-785. doi: 10.1021/acsmedchemlett.9b00027. eCollection 2019 May 9. ACS Med Chem Lett. 2019. PMID: 31097999 Free PMC article.
Optimization of Orally Bioavailable PI3Kδ Inhibitors and Identification of Vps34 as a Key Selectivity Target.
Henley ZA, Amour A, Barton N, Bantscheff M, Bergamini G, Bertrand SM, Convery M, Down K, Dümpelfeld B, Edwards CD, Grandi P, Gore PM, Keeling S, Livia S, Mallett D, Maxwell A, Price M, Rau C, Reinhard FBM, Rowedder J, Rowland P, Taylor JA, Thomas DA, Hessel EM, Hamblin JN. Henley ZA, et al. Among authors: bergamini g. J Med Chem. 2020 Jan 23;63(2):638-655. doi: 10.1021/acs.jmedchem.9b01585. Epub 2020 Jan 8. J Med Chem. 2020. PMID: 31855425
Identifying drug targets in tissues and whole blood with thermal-shift profiling.
Perrin J, Werner T, Kurzawa N, Rutkowska A, Childs DD, Kalxdorf M, Poeckel D, Stonehouse E, Strohmer K, Heller B, Thomson DW, Krause J, Becher I, Eberl HC, Vappiani J, Sevin DC, Rau CE, Franken H, Huber W, Faelth-Savitski M, Savitski MM, Bantscheff M, Bergamini G. Perrin J, et al. Among authors: bergamini g. Nat Biotechnol. 2020 Mar;38(3):303-308. doi: 10.1038/s41587-019-0388-4. Epub 2020 Jan 20. Nat Biotechnol. 2020. PMID: 31959954
208 results