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Page 1
Combined Peptide and Small-Molecule Approach toward Nonacidic THIQ Inhibitors of the KEAP1/NRF2 Interaction.
Ontoria JM, Biancofiore I, Fezzardi P, Ferrigno F, Torrente E, Colarusso S, Bianchi E, Andreini M, Patsilinakos A, Kempf G, Augustin M, Steinbacher S, Summa V, Pacifici R, Muñoz-Sanjuan I, Park L, Bresciani A, Dominguez C, Sherman LT, Harper S. Ontoria JM, et al. Among authors: augustin m. ACS Med Chem Lett. 2020 Apr 3;11(5):740-746. doi: 10.1021/acsmedchemlett.9b00594. eCollection 2020 May 14. ACS Med Chem Lett. 2020. PMID: 32435379 Free PMC article.
Dipeptidyl nitrile inhibitors of Cathepsin L.
Asaad N, Bethel PA, Coulson MD, Dawson JE, Ford SJ, Gerhardt S, Grist M, Hamlin GA, James MJ, Jones EV, Karoutchi GI, Kenny PW, Morley AD, Oldham K, Rankine N, Ryan D, Wells SL, Wood L, Augustin M, Krapp S, Simader H, Steinbacher S. Asaad N, et al. Among authors: augustin m. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4280-3. doi: 10.1016/j.bmcl.2009.05.071. Epub 2009 May 27. Bioorg Med Chem Lett. 2009. PMID: 19515558
Design of selective Cathepsin inhibitors.
Bethel PA, Gerhardt S, Jones EV, Kenny PW, Karoutchi GI, Morley AD, Oldham K, Rankine N, Augustin M, Krapp S, Simader H, Steinbacher S. Bethel PA, et al. Among authors: augustin m. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4622-5. doi: 10.1016/j.bmcl.2009.06.090. Epub 2009 Jun 27. Bioorg Med Chem Lett. 2009. PMID: 19616430
Discovery and optimization of a novel series of potent mutant B-Raf(V600E) selective kinase inhibitors.
Vasbinder MM, Aquila B, Augustin M, Chen H, Cheung T, Cook D, Drew L, Fauber BP, Glossop S, Grondine M, Hennessy E, Johannes J, Lee S, Lyne P, Mörtl M, Omer C, Palakurthi S, Pontz T, Read J, Sha L, Shen M, Steinbacher S, Wang H, Wu A, Ye M. Vasbinder MM, et al. Among authors: augustin m. J Med Chem. 2013 Mar 14;56(5):1996-2015. doi: 10.1021/jm301658d. Epub 2013 Feb 27. J Med Chem. 2013. PMID: 23398453
Identification of azabenzimidazoles as potent JAK1 selective inhibitors.
Vasbinder MM, Alimzhanov M, Augustin M, Bebernitz G, Bell K, Chuaqui C, Deegan T, Ferguson AD, Goodwin K, Huszar D, Kawatkar A, Kawatkar S, Read J, Shi J, Steinbacher S, Steuber H, Su Q, Toader D, Wang H, Woessner R, Wu A, Ye M, Zinda M. Vasbinder MM, et al. Among authors: augustin m. Bioorg Med Chem Lett. 2016 Jan 1;26(1):60-7. doi: 10.1016/j.bmcl.2015.11.031. Epub 2015 Nov 12. Bioorg Med Chem Lett. 2016. PMID: 26614408
Discovery of a Potent, Orally Bioavailable PI4KIIIβ Inhibitor (UCB9608) Able To Significantly Prolong Allogeneic Organ Engraftment in Vivo.
Reuberson J, Horsley H, Franklin RJ, Ford D, Neuss J, Brookings D, Huang Q, Vanderhoydonck B, Gao LJ, Jang MY, Herdewijn P, Ghawalkar A, Fallah-Arani F, Khan AR, Henshall J, Jairaj M, Malcolm S, Ward E, Shuttleworth L, Lin Y, Li S, Louat T, Waer M, Herman J, Payne A, Ceska T, Doyle C, Pitt W, Calmiano M, Augustin M, Steinbacher S, Lammens A, Allen R. Reuberson J, et al. Among authors: augustin m. J Med Chem. 2018 Aug 9;61(15):6705-6723. doi: 10.1021/acs.jmedchem.8b00521. Epub 2018 Jul 19. J Med Chem. 2018. PMID: 29952567
Design and Evaluation of Highly Selective Human Immunoproteasome Inhibitors Reveal a Compensatory Process That Preserves Immune Cell Viability.
Ladi E, Everett C, Stivala CE, Daniels BE, Durk MR, Harris SF, Huestis MP, Purkey HE, Staben ST, Augustin M, Blaesse M, Steinbacher S, Eidenschenk C, Pappu R, Siu M. Ladi E, et al. Among authors: augustin m. J Med Chem. 2019 Aug 8;62(15):7032-7041. doi: 10.1021/acs.jmedchem.9b00509. Epub 2019 Jul 29. J Med Chem. 2019. PMID: 31283222
Strategic Incorporation of Polarity in Heme-Displacing Inhibitors of Indoleamine-2,3-dioxygenase-1 (IDO1).
White C, McGowan MA, Zhou H, Sciammetta N, Fradera X, Lim J, Joshi EM, Andrews C, Nickbarg EB, Cowley P, Trewick S, Augustin M, von Köenig K, Lesburg CA, Otte K, Knemeyer I, Woo H, Yu W, Cheng M, Spacciapoli P, Geda P, Song X, Smotrov N, Curran P, Heo MR, Abeywickrema P, Miller JR, Bennett DJ, Han Y. White C, et al. Among authors: augustin m. ACS Med Chem Lett. 2020 Mar 10;11(4):550-557. doi: 10.1021/acsmedchemlett.0c00010. eCollection 2020 Apr 9. ACS Med Chem Lett. 2020. PMID: 32292563 Free PMC article.
Optimization of linear and cyclic peptide inhibitors of KEAP1-NRF2 protein-protein interaction.
Colarusso S, De Simone D, Frattarelli T, Andreini M, Cerretani M, Missineo A, Moretti D, Tambone S, Kempf G, Augustin M, Steinbacher S, Munoz-Sanjuan I, Park L, Summa V, Tomei L, Bresciani A, Dominguez C, Toledo-Sherman L, Bianchi E. Colarusso S, et al. Among authors: augustin m. Bioorg Med Chem. 2020 Nov 1;28(21):115738. doi: 10.1016/j.bmc.2020.115738. Epub 2020 Aug 30. Bioorg Med Chem. 2020. PMID: 33065433
1,182 results