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Page 1
A chemoenzymatic strategy for site-selective functionalization of native peptides and proteins.
Fryszkowska A, An C, Alvizo O, Banerjee G, Canada KA, Cao Y, DeMong D, Devine PN, Duan D, Elgart DM, Farasat I, Gauthier DR, Guidry EN, Jia X, Kong J, Kruse N, Lexa KW, Makarov AA, Mann BF, Milczek EM, Mitchell V, Nazor J, Neri C, Orr RK, Orth P, Phillips EM, Riggins JN, Schafer WA, Silverman SM, Strulson CA, Subramanian N, Voladri R, Yang H, Yang J, Yi X, Zhang X, Zhong W. Fryszkowska A, et al. Among authors: orth p. Science. 2022 Jun 17;376(6599):1321-1327. doi: 10.1126/science.abn2009. Epub 2022 Jun 16. Science. 2022. PMID: 35709255
Discovery of cell active macrocyclic peptides with on-target inhibition of KRAS signaling.
Lim S, Boyer N, Boo N, Huang C, Venkatachalam G, Angela Juang YC, Garrigou M, Kaan HYK, Duggal R, Peh KM, Sadruddin A, Gopal P, Yuen TY, Ng S, Kannan S, Brown CJ, Verma CS, Orth P, Peier A, Ge L, Yu X, Bhatt B, Chen F, Wang E, Li NJ, Gonzales RJ, Stoeck A, Henry B, Sawyer TK, Lane DP, Johannes CW, Biswas K, Partridge AW. Lim S, et al. Among authors: orth p. Chem Sci. 2021 Nov 25;12(48):15975-15987. doi: 10.1039/d1sc05187c. eCollection 2021 Dec 15. Chem Sci. 2021. PMID: 35024121 Free PMC article.
Design and discovery of C2-fluoroalkyl iminothiazine dioxides as BACE inhibitors.
Taoka BM, Wu WL, Hao J, Dolmaski M, Wang H, Levorse D, Orth P, Hyde LA, Smith B, Michener MS, Kennedy ME, Parker EM, Cumming JN. Taoka BM, et al. Among authors: orth p. Bioorg Med Chem Lett. 2022 Jan 15;56:128463. doi: 10.1016/j.bmcl.2021.128463. Epub 2021 Nov 24. Bioorg Med Chem Lett. 2022. PMID: 34838652
Piperazine sulfonamide BACE1 inhibitors: design, synthesis, and in vivo characterization.
Cumming J, Babu S, Huang Y, Carrol C, Chen X, Favreau L, Greenlee W, Guo T, Kennedy M, Kuvelkar R, Le T, Li G, McHugh N, Orth P, Ozgur L, Parker E, Saionz K, Stamford A, Strickland C, Tadesse D, Voigt J, Zhang L, Zhang Q. Cumming J, et al. Among authors: orth p. Bioorg Med Chem Lett. 2010 May 1;20(9):2837-42. doi: 10.1016/j.bmcl.2010.03.050. Epub 2010 Mar 12. Bioorg Med Chem Lett. 2010. PMID: 20347593
Design and validation of bicyclic iminopyrimidinones as beta amyloid cleaving enzyme-1 (BACE1) inhibitors: conformational constraint to favor a bioactive conformation.
Mandal M, Zhu Z, Cumming JN, Liu X, Strickland C, Mazzola RD, Caldwell JP, Leach P, Grzelak M, Hyde L, Zhang Q, Terracina G, Zhang L, Chen X, Kuvelkar R, Kennedy ME, Favreau L, Cox K, Orth P, Buevich A, Voigt J, Wang H, Kazakevich I, McKittrick BA, Greenlee W, Parker EM, Stamford AW. Mandal M, et al. Among authors: orth p. J Med Chem. 2012 Nov 8;55(21):9331-45. doi: 10.1021/jm301039c. Epub 2012 Oct 1. J Med Chem. 2012. PMID: 22989333
Discovery of potent iminoheterocycle BACE1 inhibitors.
Caldwell JP, Mazzola RD, Durkin J, Chen J, Chen X, Favreau L, Kennedy M, Kuvelkar R, Lee J, McHugh N, McKittrick B, Orth P, Stamford A, Strickland C, Voigt J, Wang L, Zhang L, Zhang Q, Zhu Z. Caldwell JP, et al. Among authors: orth p. Bioorg Med Chem Lett. 2014 Dec 1;24(23):5455-9. doi: 10.1016/j.bmcl.2014.10.006. Epub 2014 Oct 23. Bioorg Med Chem Lett. 2014. PMID: 25455483
Structure-Based Design of an Iminoheterocyclic β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central Aβ in Nonhuman Primates.
Mandal M, Wu Y, Misiaszek J, Li G, Buevich A, Caldwell JP, Liu X, Mazzola RD, Orth P, Strickland C, Voigt J, Wang H, Zhu Z, Chen X, Grzelak M, Hyde LA, Kuvelkar R, Leach PT, Terracina G, Zhang L, Zhang Q, Michener MS, Smith B, Cox K, Grotz D, Favreau L, Mitra K, Kazakevich I, McKittrick BA, Greenlee W, Kennedy ME, Parker EM, Cumming JN, Stamford AW. Mandal M, et al. Among authors: orth p. J Med Chem. 2016 Apr 14;59(7):3231-48. doi: 10.1021/acs.jmedchem.5b01995. Epub 2016 Mar 22. J Med Chem. 2016. PMID: 26937601
Discovery of an Orally Available, Brain Penetrant BACE1 Inhibitor that Affords Robust CNS Aβ Reduction.
Stamford AW, Scott JD, Li SW, Babu S, Tadesse D, Hunter R, Wu Y, Misiaszek J, Cumming JN, Gilbert EJ, Huang C, McKittrick BA, Hong L, Guo T, Zhu Z, Strickland C, Orth P, Voigt JH, Kennedy ME, Chen X, Kuvelkar R, Hodgson R, Hyde LA, Cox K, Favreau L, Parker EM, Greenlee WJ. Stamford AW, et al. Among authors: orth p. ACS Med Chem Lett. 2012 Nov 8;3(11):897-902. doi: 10.1021/ml3001165. Epub 2012 Jul 12. ACS Med Chem Lett. 2012. PMID: 23412139 Free PMC article.
Discovery of the 3-Imino-1,2,4-thiadiazinane 1,1-Dioxide Derivative Verubecestat (MK-8931)-A β-Site Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor for the Treatment of Alzheimer's Disease.
Scott JD, Li SW, Brunskill AP, Chen X, Cox K, Cumming JN, Forman M, Gilbert EJ, Hodgson RA, Hyde LA, Jiang Q, Iserloh U, Kazakevich I, Kuvelkar R, Mei H, Meredith J, Misiaszek J, Orth P, Rossiter LM, Slater M, Stone J, Strickland CO, Voigt JH, Wang G, Wang H, Wu Y, Greenlee WJ, Parker EM, Kennedy ME, Stamford AW. Scott JD, et al. Among authors: orth p. J Med Chem. 2016 Dec 8;59(23):10435-10450. doi: 10.1021/acs.jmedchem.6b00307. Epub 2016 Nov 18. J Med Chem. 2016. PMID: 27933948
155 results