http://orcid.org/0000-0002-1075-3781
References
- Ciechanover A. Proteolysis: from the lysosome to ubiquitin and the proteasome. Nat Rev Mol Cell Biol 2005;6:79–87.
- Inobe T, Matouschek A. Paradigms of protein degradation by the proteasome. Curr Opin Struct Biol 2014;24:156–64.
- Finley D. Recognition and processing of ubiquitin-protein conjugates by the proteasome. Annu Rev Biochem 2009;78:477–513.
- Ciechanover A. The ubiquitin-proteasome pathway: on protein death and cell life. EMBO J 1998;17:7151–60.
- Groll M, Heinemeyer W, Jäger S, et al. The catalytic sites of 20S proteasomes and their role in subunit maturation: a mutational and crystallographic study. Proc Natl Acad Sci USA 1999;96:10976–83.
- Borissenko L, Groll M. 20S proteasome and its inhibitors: crystallographic knowledge for drug development. Chem Rev 2007;107:687–717.
- Kisselev AF, Goldberg AL. Proteasome inhibitors: from research tools to drug candidates. Chem Biol 2001;8:739–58.
- Nazif T, Bogyo M. Global analysis of proteasomal substrate specificity using positional-scanning libraries of covalent inhibitors. Proc Natl Acad Sci USA 2001;98:2967–72.
- Kisselev AF, van der Linden WA, Overkleeft HS. Proteasome inhibitors: an expanding army attacking a unique target. Chem Biol 2012;19:99–115.
- Groll M, Huber R, Moroder L. The persisting challenge of selective and specific proteasome inhibition. J Pept Sci 2009;15:58–66.
- Genin E, Reboud-Ravaux M, Vidal J. Proteasome inhibitors: recent advances and new perspectives in medicinal chemistry. Curr Top Med Chem 2010;10:232–56.
- Micale N, Scarbaci K, Troiano V, et al. Peptide-based proteasome inhibitors in anticancer drug design. Med Res Rev 2014;34:1001–69.
- Dorsey BD, Iqbal M, Chatterjee S, et al. Discovery of a potent, selective, and orally active proteasome inhibitor for the treatment of cancer. J Med Chem 2008;51:1068–72.
- Mroczkiewicz M, Winkler K, Nowis D, et al. Studies of the synthesis of all stereoisomers of MG-132 proteasome inhibitors in the tumor targeting approach. J Med Chem 2010;53:1509–18.
- Bazzaro M, Anchoori RK, Mudiam MK, et al. α,β-unsaturated carbonyl system of chalcone-based derivatives is responsible for broad inhibition of proteasomal activity and preferential killing of human papilloma virus (HPV) positive cervical cancer cells. J Med Chem 2011;54:449–56.
- Desvergne A, Genin E, Maréchal X, et al. Dimerized linear mimics of a natural cyclopeptide (TMC-95A) are potent noncovalent inhibitors of the eukaryotic 20S proteasome. J Med Chem 2013;56:3367–78.
- Moreau P, Richardson PG, Cavo M, et al. Proteasome inhibitors in multiple myeloma: 10 years later. Blood 2012;120:947–59.
- Adams J. The development of proteasome inhibitors as anti-cancer drugs. Cancer Cell 2004;5:417–21.
- Demo SD, Kirk CJ, Aujay MA, et al. Antitumor activity of PR-171, a novel irreversible inhibitor of the proteasome. Cancer Res 2007;67:6383–91.
- Richardson PG, Baz R, Wang M, et al. Phase 1 study of twice-weekly ixazomib, an oral proteasome inhibitor, in re-lapsed/refractory multiple myeloma patients. Blood 2014;124:1038–46.
- Zhou HJ, Aujay MA, Bennett MK, et al. Design and synthesis of an orally bioavailable and selective peptide epoxyketone proteasome inhibitor (PR-047). J Med Chem 2009;52:3028–38.
- Marastoni M, Baldisserotto A, Canella A, et al. Arecoline tripeptide inhibitors of proteasome. J Med Chem 2004;47:1587–90.
- Baldisserotto A, Ferretti V, Destro F, et al. Alpha, beta-unsaturated N-acylpyrrole peptidyl derivatives: new proteasome inhibitors. J Med Chem 2010;53:6511–15.
- Franceschini C, Trapella C, Calia R, et al. C-terminal trans, trans-muconic acid ethyl ester partial retro-inverso pseudopeptides as proteasome inhibitors. J Enzyme Inhib Med Chem 2013;28:1034–9.
- Scotti A, Trapella C, Ferretti V, et al. Studies of C-terminal naphthoquinone dipeptides as 20S proteasome inhibitors. J Enzyme Inhib Med Chem 2016;3:456–63.
- Lawrence HR, Kazi A, Luo Y, et al. Synthesis and biological evaluation of naphthoquinone analogs as a novel class of proteasome inhibitors. Bioorg Med Chem 2010;18:5576–92.
- Xu K, Xiao Z, Tang YB, et al. Design and synthesis of naphthoquinone derivatives as antiproliferative agents and 20S proteasome inhibitors. Bioorg Med Chem Lett 2012;22:2772–4.
- Ge Y, Kazi A, Marsilio F, et al. Discovery and synthesis of hydronaphthoquinones as novel proteasome inhibitors. J Med Chem 2012;55:1978–98.
- Chadwick J, Jones M, Mercer AE, et al. Design, synthesis and antimalarial/anticancer evaluation of spermidine linked artemisinin conjugates designed to exploit polyamine transporters in Plasmodium falciparum and HL-60 cancer cell lines. Bioorg Med Chem 2010;18:2586–97.
- Yang H, Xiang J, Wang N, et al. Converse conformational control of smoothened activity by structurally related small molecules. J Biol Chem 2009;284:20876–84.
- Gavioli R, Vertuani S, Masucci MG. Proteasome inhibitors reconstitute the presentation of cytotoxic T-cell epitopes in Epstein-Barr virus-associated tumors. Int J Cancer 2002;101:532–8.
- Groll M, Kim KB, Kairies N, et al. Crystal structure of epoxomicin: 20S proteasome reveals a molecular basis for selectivity of α, β-epoxyketone proteasome inhibitor. J Am Chem Soc 2000;122:1237–8.
- Groll M, Larionov OV, Huber R, de Meijere A. Inhibitor-binding mode of homobelactosin C to proteasomes: new insights into class I MHC ligand generation. Proc Natl Acad Sci USA 2006;103:4576–9.
- Halgren TA. Merck molecular force field. I. Basis, form, scope, parameterization, and performance of MMFF94. J Comput Chem 1996;17:490–519.
- Hansen MB, Nielsen SE, Berg K. Re-examination and further development of a precise and rapid dye method for measuring cell growth/cell kill. J Immunol Methods 1989;119:203–10.