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Azaindoles as Zinc-Binding Small-Molecule Inhibitors of the JAMM Protease CSN5.
Altmann E, Erbel P, Renatus M, Schaefer M, Schlierf A, Druet A, Kieffer L, Sorge M, Pfister K, Hassiepen U, Jones M, Ruedisser S, Ostermeier D, Martoglio B, Jefferson AB, Quancard J. Altmann E, et al. Angew Chem Int Ed Engl. 2017 Jan 24;56(5):1294-1297. doi: 10.1002/anie.201608672. Epub 2016 Dec 16. Angew Chem Int Ed Engl. 2017. PMID: 27981705
Discovery and structure-based optimization of adenain inhibitors.
Mac Sweeney A, Grosche P, Ellis D, Combrink K, Erbel P, Hughes N, Sirockin F, Melkko S, Bernardi A, Ramage P, Jarousse N, Altmann E. Mac Sweeney A, et al. Among authors: altmann e. ACS Med Chem Lett. 2014 Jun 20;5(8):937-41. doi: 10.1021/ml500224t. eCollection 2014 Aug 14. ACS Med Chem Lett. 2014. PMID: 25147618 Free PMC article.
Structure-based design and optimization of potent inhibitors of the adenoviral protease.
Grosche P, Sirockin F, Mac Sweeney A, Ramage P, Erbel P, Melkko S, Bernardi A, Hughes N, Ellis D, Combrink KD, Jarousse N, Altmann E. Grosche P, et al. Among authors: altmann e. Bioorg Med Chem Lett. 2015 Feb 1;25(3):438-43. doi: 10.1016/j.bmcl.2014.12.057. Epub 2014 Dec 24. Bioorg Med Chem Lett. 2015. PMID: 25571794
Targeted inhibition of the COP9 signalosome for treatment of cancer.
Schlierf A, Altmann E, Quancard J, Jefferson AB, Assenberg R, Renatus M, Jones M, Hassiepen U, Schaefer M, Kiffe M, Weiss A, Wiesmann C, Sedrani R, Eder J, Martoglio B. Schlierf A, et al. Among authors: altmann e. Nat Commun. 2016 Oct 24;7:13166. doi: 10.1038/ncomms13166. Nat Commun. 2016. PMID: 27774986 Free PMC article.
Structure-Based Design and Preclinical Characterization of Selective and Orally Bioavailable Factor XIa Inhibitors: Demonstrating the Power of an Integrated S1 Protease Family Approach.
Lorthiois E, Roache J, Barnes-Seeman D, Altmann E, Hassiepen U, Turner G, Duvadie R, Hornak V, Karki RG, Schiering N, Weihofen WA, Perruccio F, Calhoun A, Fazal T, Dedic D, Durand C, Dussauge S, Fettis K, Tritsch F, Dentel C, Druet A, Liu D, Kirman L, Lachal J, Namoto K, Bevan D, Mo R, Monnet G, Muller L, Zessis R, Huang X, Lindsley L, Currie T, Chiu YH, Fridrich C, Delgado P, Wang S, Hollis-Symynkywicz M, Berghausen J, Williams E, Liu H, Liang G, Kim H, Hoffmann P, Hein A, Ramage P, D'Arcy A, Harlfinger S, Renatus M, Ruedisser S, Feldman D, Elliott J, Sedrani R, Maibaum J, Adams CM. Lorthiois E, et al. Among authors: altmann e. J Med Chem. 2020 Aug 13;63(15):8088-8113. doi: 10.1021/acs.jmedchem.0c00279. Epub 2020 Jul 21. J Med Chem. 2020. PMID: 32551603
Discovery of Potent, Highly Selective, and In Vivo Efficacious, Allosteric MALT1 Inhibitors by Iterative Scaffold Morphing.
Pissot Soldermann C, Simic O, Renatus M, Erbel P, Melkko S, Wartmann M, Bigaud M, Weiss A, McSheehy P, Endres R, Santos P, Blank J, Schuffenhauer A, Bold G, Buschmann N, Zoller T, Altmann E, Manley PW, Dix I, Buchdunger E, Scesa J, Quancard J, Schlapbach A, Bornancin F, Radimerski T, Régnier CH. Pissot Soldermann C, et al. Among authors: altmann e. J Med Chem. 2020 Dec 10;63(23):14576-14593. doi: 10.1021/acs.jmedchem.0c01245. Epub 2020 Nov 30. J Med Chem. 2020. PMID: 33252239
Design and Biochemical Characterization of Peptidic Inhibitors of the Myb/p300 Interaction.
Jones M, Grosche P, Floersheimer A, André J, Gattlen R, Oser D, Tinchant J, Wille R, Chie-Leon B, Gerspacher M, Ertl P, Ostermann N, Altmann E, Manchado E, Vorherr T, Chène P. Jones M, et al. Among authors: altmann e. Biochemistry. 2023 Apr 4;62(7):1321-1329. doi: 10.1021/acs.biochem.2c00690. Epub 2023 Mar 8. Biochemistry. 2023. PMID: 36883372
Dipeptide nitrile inhibitors of cathepsin K.
Altmann E, Aichholz R, Betschart C, Buhl T, Green J, Lattmann R, Missbach M. Altmann E, et al. Bioorg Med Chem Lett. 2006 May 1;16(9):2549-54. doi: 10.1016/j.bmcl.2006.01.104. Epub 2006 Feb 9. Bioorg Med Chem Lett. 2006. PMID: 16480867
171 results