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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: bianchi e. 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.
Nuclear factor (erythroid-derived 2)-like 2 (NRF2) drug discovery: Biochemical toolbox to develop NRF2 activators by reversible binding of Kelch-like ECH-associated protein 1 (KEAP1).
Bresciani A, Missineo A, Gallo M, Cerretani M, Fezzardi P, Tomei L, Cicero DO, Altamura S, Santoprete A, Ingenito R, Bianchi E, Pacifici R, Dominguez C, Munoz-Sanjuan I, Harper S, Toledo-Sherman L, Park LC. Bresciani A, et al. Among authors: bianchi e. Arch Biochem Biophys. 2017 Oct 1;631:31-41. doi: 10.1016/j.abb.2017.08.003. Epub 2017 Aug 8. Arch Biochem Biophys. 2017. PMID: 28801166 Review.
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: bianchi e. 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
Series of Novel and Highly Potent Cyclic Peptide PCSK9 Inhibitors Derived from an mRNA Display Screen and Optimized via Structure-Based Design.
Alleyne C, Amin RP, Bhatt B, Bianchi E, Blain JC, Boyer N, Branca D, Embrey MW, Ha SN, Jette K, Johns DG, Kerekes AD, Koeplinger KA, LaPlaca D, Li N, Murphy B, Orth P, Ricardo A, Salowe S, Seyb K, Shahripour A, Stringer JR, Sun Y, Tracy R, Wu C, Xiong Y, Youm H, Zokian HJ, Tucker TJ. Alleyne C, et al. Among authors: bianchi e. J Med Chem. 2020 Nov 25;63(22):13796-13824. doi: 10.1021/acs.jmedchem.0c01084. Epub 2020 Nov 10. J Med Chem. 2020. PMID: 33170686
Identification of Potent and Long-Acting Single-Chain Peptide Mimetics of Human Relaxin-2 for Cardiovascular Diseases.
Mallart S, Ingenito R, Bianchi E, Bresciani A, Esposito S, Gallo M, Magotti P, Monteagudo E, Orsatti L, Roversi D, Santoprete A, Tucci F, Veneziano M, Bartsch R, Boehm C, Brasseur D, Bruneau P, Corbier A, Froissant J, Gauzy-Lazo L, Gervat V, Marguet F, Menguy I, Minoletti C, Nicolas MF, Pasquier O, Poirier B, Raux A, Riva L, Janiak P, Strobel H, Duclos O, Illiano S. Mallart S, et al. Among authors: bianchi e. J Med Chem. 2021 Feb 25;64(4):2139-2150. doi: 10.1021/acs.jmedchem.0c01533. Epub 2021 Feb 8. J Med Chem. 2021. PMID: 33555858
A Series of Novel, Highly Potent, and Orally Bioavailable Next-Generation Tricyclic Peptide PCSK9 Inhibitors.
Tucker TJ, Embrey MW, Alleyne C, Amin RP, Bass A, Bhatt B, Bianchi E, Branca D, Bueters T, Buist N, Ha SN, Hafey M, He H, Higgins J, Johns DG, Kerekes AD, Koeplinger KA, Kuethe JT, Li N, Murphy B, Orth P, Salowe S, Shahripour A, Tracy R, Wang W, Wu C, Xiong Y, Zokian HJ, Wood HB, Walji A. Tucker TJ, et al. Among authors: bianchi e. J Med Chem. 2021 Nov 25;64(22):16770-16800. doi: 10.1021/acs.jmedchem.1c01599. Epub 2021 Oct 27. J Med Chem. 2021. PMID: 34704436
Development of ProTx-II Analogues as Highly Selective Peptide Blockers of Nav1.7 for the Treatment of Pain.
Adams GL, Pall PS, Grauer SM, Zhou X, Ballard JE, Vavrek M, Kraus RL, Morissette P, Li N, Colarusso S, Bianchi E, Palani A, Klein R, John CT, Wang D, Tudor M, Nolting AF, Biba M, Nowak T, Makarov AA, Reibarkh M, Buevich AV, Zhong W, Regalado EL, Wang X, Gao Q, Shahripour A, Zhu Y, de Simone D, Frattarelli T, Pasquini NM, Magotti P, Iaccarino R, Li Y, Solly K, Lee KJ, Wang W, Chen F, Zeng H, Wang J, Regan H, Amin RP, Regan CP, Burgey CS, Henze DA, Sun C, Tellers DM. Adams GL, et al. Among authors: bianchi e. J Med Chem. 2022 Jan 13;65(1):485-496. doi: 10.1021/acs.jmedchem.1c01570. Epub 2021 Dec 21. J Med Chem. 2022. PMID: 34931831
SAR evolution towards potent C-terminal carboxamide peptide inhibitors of Zika virus NS2B-NS3 protease.
Colarusso S, Ferrigno F, Ponzi S, Pavone F, Conte I, Abate L, Beghetto E, Missineo A, Amaudrut J, Bresciani A, Paonessa G, Tomei L, Montalbetti C, Bianchi E, Toniatti C, Ontoria JM. Colarusso S, et al. Among authors: bianchi e. Bioorg Med Chem. 2022 Mar 1;57:116631. doi: 10.1016/j.bmc.2022.116631. Epub 2022 Jan 23. Bioorg Med Chem. 2022. PMID: 35123179
873 results