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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: josien h. 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. Among authors: josien h. Nat Commun. 2024 Jan 12;15(1):489. doi: 10.1038/s41467-023-43346-4. Nat Commun. 2024. PMID: 38216578 Free PMC article.
A high-throughput microfluidic mechanoporation platform to enable intracellular delivery of cyclic peptides in cell-based assays.
Kasper SH, Otten S, Squadroni B, Orr-Terry C, Kuang Y, Mussallem L, Ge L, Yan L, Kannan S, Verma CS, Brown CJ, Johannes CW, Lane DP, Chandramohan A, Partridge AW, Roberts LR, Josien H, Therien AG, Hett EC, Howell BJ, Peier A, Ai X, Cassaday J. Kasper SH, et al. Among authors: josien h. Bioeng Transl Med. 2023 May 13;8(5):e10542. doi: 10.1002/btm2.10542. eCollection 2023 Sep. Bioeng Transl Med. 2023. PMID: 37693049 Free PMC article.
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
Pio B, Chobanian HR, Guo Y, Josien H, Hagmann WK, Miller M, Trujillo ME, Kirkland M, Kosinski D, Mane J, Pachanski M, Cheewatrakoolpong B, Ashley E, Orr R, Wright MJ, Bugianesi R, Souza S, Zhang X, Di Salvo J, Weinglass AB, Tschirret-Guth R, Samuel K, Chen Q, Shang J, Lamca J, Ehrhart J, Nargund R, Howard AD, Colletti SL. Pio B, et al. Among authors: josien h. Bioorg Med Chem Lett. 2019 Jul 15;29(14):1842-1848. doi: 10.1016/j.bmcl.2019.04.050. Epub 2019 May 2. Bioorg Med Chem Lett. 2019. PMID: 31109791
Structural basis for the cooperative allosteric activation of the free fatty acid receptor GPR40.
Lu J, Byrne N, Wang J, Bricogne G, Brown FK, Chobanian HR, Colletti SL, Di Salvo J, Thomas-Fowlkes B, Guo Y, Hall DL, Hadix J, Hastings NB, Hermes JD, Ho T, Howard AD, Josien H, Kornienko M, Lumb KJ, Miller MW, Patel SB, Pio B, Plummer CW, Sherborne BS, Sheth P, Souza S, Tummala S, Vonrhein C, Webb M, Allen SJ, Johnston JM, Weinglass AB, Sharma S, Soisson SM. Lu J, et al. Among authors: josien h. Nat Struct Mol Biol. 2017 Jul;24(7):570-577. doi: 10.1038/nsmb.3417. Epub 2017 Jun 5. Nat Struct Mol Biol. 2017. PMID: 28581512
Design and Synthesis of Novel, Selective GPR40 AgoPAMs.
Plummer CW, Clements MJ, Chen H, Rajagopalan M, Josien H, Hagmann WK, Miller M, Trujillo ME, Kirkland M, Kosinski D, Mane J, Pachanski M, Cheewatrakoolpong B, Nolting AF, Orr R, Christensen M, Campeau LC, Wright MJ, Bugianesi R, Souza S, Zhang X, Di Salvo J, Weinglass AB, Tschirret-Guth R, Nargund R, Howard AD, Colletti SL. Plummer CW, et al. Among authors: josien h. ACS Med Chem Lett. 2017 Jan 23;8(2):221-226. doi: 10.1021/acsmedchemlett.6b00443. eCollection 2017 Feb 9. ACS Med Chem Lett. 2017. PMID: 28197316 Free PMC article.
Substituted 4-morpholine N-arylsulfonamides as γ-secretase inhibitors.
Zhao Z, Pissarnitski DA, Josien HB, Bara TA, Clader JW, Li H, McBriar MD, Rajagopalan M, Xu R, Terracina G, Hyde L, Song L, Zhang L, Parker EM, Osterman R, Buevich AV. Zhao Z, et al. Among authors: josien hb. Eur J Med Chem. 2016 Nov 29;124:36-48. doi: 10.1016/j.ejmech.2016.08.024. Epub 2016 Aug 13. Eur J Med Chem. 2016. PMID: 27560281
Discovery of MK-8831, A Novel Spiro-Proline Macrocycle as a Pan-Genotypic HCV-NS3/4a Protease Inhibitor.
Neelamkavil SF, Agrawal S, Bara T, Bennett C, Bhat S, Biswas D, Brockunier L, Buist N, Burnette D, Cartwright M, Chackalamannil S, Chase R, Chelliah M, Chen A, Clasby M, Colandrea VJ, Davies IW, Eagen K, Guo Z, Han Y, Howe J, Jayne C, Josien H, Kargman S, Marcantonio K, Miao S, Miller R, Nolting A, Pinto P, Rajagopalan M, Ruck RT, Shah U, Soriano A, Sperbeck D, Velazquez F, Wu J, Xia Y, Venkatraman S. Neelamkavil SF, et al. Among authors: josien h. ACS Med Chem Lett. 2015 Dec 22;7(1):111-6. doi: 10.1021/acsmedchemlett.5b00425. eCollection 2016 Jan 14. ACS Med Chem Lett. 2015. PMID: 26819676 Free PMC article.
Discovery of a Novel, Potent Spirocyclic Series of γ-Secretase Inhibitors.
Zhao Z, Pissarnitski DA, Josien HB, Wu WL, Xu R, Li H, Clader JW, Burnett DA, Terracina G, Hyde L, Lee J, Song L, Zhang L, Parker EM. Zhao Z, et al. Among authors: josien hb. J Med Chem. 2015 Nov 25;58(22):8806-17. doi: 10.1021/acs.jmedchem.5b00774. Epub 2015 Nov 6. J Med Chem. 2015. PMID: 26496070
35 results