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Orally Bioavailable Macrocyclic Peptide That Inhibits Binding of PCSK9 to the Low Density Lipoprotein Receptor.
Johns DG, Campeau LC, Banka P, Bautmans A, Bueters T, Bianchi E, Branca D, Bulger PG, Crevecoeur I, Ding FX, Garbaccio RM, Guetschow ED, Guo Y, Ha SN, Johnston JM, Josien H, Kauh EA, Koeplinger KA, Kuethe JT, Lai E, Lanning CL, Lee AYH, Li L, Nair AG, O'Neill EA, Stoch SA, Thaisrivongs DA, Tucker TJ, Vachal P, van Dyck K, Vanhoutte FP, Volckaert B, Wolford DG, Xu A, Zhao T, Zhou D, Zhou S, Zhu X, Zokian HJ, Walji AM, Wood HB. Johns DG, et al. Among authors: garbaccio rm. Circulation. 2023 Jul 11;148(2):144-158. doi: 10.1161/CIRCULATIONAHA.122.063372. Epub 2023 May 1. Circulation. 2023. PMID: 37125593 Free PMC article.
Design-rules for stapled peptides with in vivo activity and their application to Mdm2/X antagonists.
Chandramohan A, Josien H, Yuen TY, Duggal R, Spiegelberg D, Yan L, Juang YA, Ge L, Aronica PG, Kaan HYK, Lim YH, Peier A, Sherborne B, Hochman J, Lin S, Biswas K, Nestor M, Verma CS, Lane DP, Sawyer TK, Garbaccio R, Henry B, Kannan S, Brown CJ, Johannes CW, Partridge AW. Chandramohan A, et al. Nat Commun. 2024 Jan 12;15(1):489. doi: 10.1038/s41467-023-43346-4. Nat Commun. 2024. PMID: 38216578 Free PMC article.
Discovery of Insulin Receptor Partial Agonists MK-5160 and MK-1092 as Novel Basal Insulins with Potential to Improve Therapeutic Index.
Pissarnitski DA, Kekec A, Yan L, Zhu Y, Feng DD, Huo P, Madsen-Duggan C, Moyes CR, Nargund RP, Kelly T, Zhang X, Carballo-Jane E, Gorski J, Zafian P, Qatanani M, Kaarsholm N, Meng F, Jia X, Lee KJ, Wang W, Xu S, Hohn MJ, Iammarino MJ, McCoy MA, Okoh GA, Liang Y, Hollingsworth SA, Erion MD, Kelley DE, Garbaccio RM, Zhang A, Mu J, Lin S. Pissarnitski DA, et al. Among authors: garbaccio rm. J Med Chem. 2022 Apr 14;65(7):5593-5605. doi: 10.1021/acs.jmedchem.1c02073. Epub 2022 Mar 17. J Med Chem. 2022. PMID: 35298158
Multiple Synthetic Routes to the Mini-Protein Omomyc and Coiled-Coil Domain Truncations.
Brown ZZ, Mapelli C, Farasat I, Shoultz AV, Johnson SA, Orvieto F, Santoprete A, Bianchi E, McCracken AB, Chen K, Zhu X, Demma MJ, Lacey BM, Canada KA, Garbaccio RM, O'Neil J, Walji A. Brown ZZ, et al. Among authors: garbaccio rm. J Org Chem. 2020 Feb 7;85(3):1466-1475. doi: 10.1021/acs.joc.9b02467. Epub 2019 Nov 25. J Org Chem. 2020. PMID: 31660743
The importance of synthetic chemistry in the pharmaceutical industry.
Campos KR, Coleman PJ, Alvarez JC, Dreher SD, Garbaccio RM, Terrett NK, Tillyer RD, Truppo MD, Parmee ER. Campos KR, et al. Among authors: garbaccio rm. Science. 2019 Jan 18;363(6424):eaat0805. doi: 10.1126/science.aat0805. Science. 2019. PMID: 30655413 Review.
Optimization of Novel Aza-benzimidazolone mGluR2 PAMs with Respect to LLE and PK Properties and Mitigation of CYP TDI.
Pero JE, Rossi MA, Kelly MJ 3rd, Lehman HD, Layton ME, Garbaccio RM, O'Brien JA, Magliaro BC, Uslaner JM, Huszar SL, Fillgrove KL, Tang C, Kuo Y, Joyce LA, Sherer EC, Jacobson MA. Pero JE, et al. Among authors: garbaccio rm. ACS Med Chem Lett. 2016 Jan 10;7(3):312-7. doi: 10.1021/acsmedchemlett.5b00459. eCollection 2016 Mar 10. ACS Med Chem Lett. 2016. PMID: 26985321 Free PMC article.
Discovery of 5-aryl-1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-ones as positive allosteric modulators of metabotropic glutamate subtype-2 (mGlu2) receptors with efficacy in a preclinical model of psychosis.
Layton ME, Reif AJ, Hartingh TJ, Rodzinak K, Dudkin V, Wang C, Arrington K, Kelly MJ 3rd, Garbaccio RM, O'Brien JA, Magliaro BC, Uslaner JM, Huszar SL, Fillgrove KL, Tang C, Kuo Y, Jacobson MA. Layton ME, et al. Among authors: garbaccio rm. Bioorg Med Chem Lett. 2016 Feb 15;26(4):1260-4. doi: 10.1016/j.bmcl.2016.01.021. Epub 2016 Jan 11. Bioorg Med Chem Lett. 2016. PMID: 26810316
Discovery of Pyrophosphate Diesters as Tunable, Soluble, and Bioorthogonal Linkers for Site-Specific Antibody-Drug Conjugates.
Kern JC, Cancilla M, Dooney D, Kwasnjuk K, Zhang R, Beaumont M, Figueroa I, Hsieh S, Liang L, Tomazela D, Zhang J, Brandish PE, Palmieri A, Stivers P, Cheng M, Feng G, Geda P, Shah S, Beck A, Bresson D, Firdos J, Gately D, Knudsen N, Manibusan A, Schultz PG, Sun Y, Garbaccio RM. Kern JC, et al. Among authors: garbaccio rm. J Am Chem Soc. 2016 Feb 3;138(4):1430-45. doi: 10.1021/jacs.5b12547. Epub 2016 Jan 25. J Am Chem Soc. 2016. PMID: 26745435
40 results