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Page 1
Discovery and Optimization of a Novel Triazole Series of GPR142 Agonists for the Treatment of Type 2 Diabetes.
Guo L, Parker DL, Zang Y, Sweis RF, Liu W, Sherer EC, Buist N, Terebetski J, Kelly T, Bugianesi R, Priest BT, Dingley KH, Li X, Mitelman S, Salituro G, Trujillo ME, Pachanski M, Kirkland M, Powles MA, Eiermann GJ, Feng Y, Shang J, Howard AD, Ujjainwalla F, Sinz CJ, Debenham JS, Edmondson SD, Nargund RP, Hagmann WK, Li D. Guo L, et al. Among authors: bugianesi r. ACS Med Chem Lett. 2016 Oct 12;7(12):1107-1111. doi: 10.1021/acsmedchemlett.6b00314. eCollection 2016 Dec 8. ACS Med Chem Lett. 2016. PMID: 27994747 Free PMC article.
Discovery and development of benzo-[1,2,4]-triazolo-[1,4]-oxazepine GPR142 agonists for the treatment of diabetes.
Wilson JE, Kurukulasuriya R, Sinz C, Lombardo M, Bender K, Parker D, Sherer EC, Costa M, Dingley K, Li X, Mitelman S, Tong S, Bugianesi R, Ehrhardt A, Priest B, Ratliff K, Ujjainwalla F, Nargund R, Hagmann WK, Edmondson S. Wilson JE, et al. Among authors: bugianesi r. Bioorg Med Chem Lett. 2016 Jun 15;26(12):2947-2951. doi: 10.1016/j.bmcl.2016.04.018. Bioorg Med Chem Lett. 2016. PMID: 27240550
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: bugianesi r. 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.
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: bugianesi r. 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
Definitive Metabolite Identification Coupled with Automated Ligand Identification System (ALIS) Technology: A Novel Approach to Uncover Structure-Activity Relationships and Guide Drug Design in a Factor IXa Inhibitor Program.
Zhang T, Liu Y, Yang X, Martin GE, Yao H, Shang J, Bugianesi RM, Ellsworth KP, Sonatore LM, Nizner P, Sherer EC, Hill SE, Knemeyer IW, Geissler WM, Dandliker PJ, Helmy R, Wood HB. Zhang T, et al. Among authors: bugianesi rm. J Med Chem. 2016 Mar 10;59(5):1818-29. doi: 10.1021/acs.jmedchem.5b01293. Epub 2016 Feb 22. J Med Chem. 2016. PMID: 26871940
Improved Cav2.2 Channel Inhibitors through a gem-Dimethylsulfone Bioisostere Replacement of a Labile Sulfonamide.
Shao PP, Ye F, Chakravarty PK, Herrington JB, Dai G, Bugianesi RM, Haedo RJ, Swensen AM, Warren VA, Smith MM, Garcia ML, McManus OB, Lyons KA, Li X, Green M, Jochnowitz N, McGowan E, Mistry S, Sun SY, Abbadie C, Kaczorowski GJ, Duffy JL. Shao PP, et al. Among authors: bugianesi rm. ACS Med Chem Lett. 2013 Sep 8;4(11):1064-8. doi: 10.1021/ml4002612. eCollection 2013 Nov 14. ACS Med Chem Lett. 2013. PMID: 24900606 Free PMC article.
Blockers of the delayed-rectifier potassium current in pancreatic beta-cells enhance glucose-dependent insulin secretion.
Herrington J, Zhou YP, Bugianesi RM, Dulski PM, Feng Y, Warren VA, Smith MM, Kohler MG, Garsky VM, Sanchez M, Wagner M, Raphaelli K, Banerjee P, Ahaghotu C, Wunderler D, Priest BT, Mehl JT, Garcia ML, McManus OB, Kaczorowski GJ, Slaughter RS. Herrington J, et al. Diabetes. 2006 Apr;55(4):1034-42. doi: 10.2337/diabetes.55.04.06.db05-0788. Diabetes. 2006. PMID: 16567526
A high-capacity membrane potential FRET-based assay for NaV1.8 channels.
Liu CJ, Priest BT, Bugianesi RM, Dulski PM, Felix JP, Dick IE, Brochu RM, Knaus HG, Middleton RE, Kaczorowski GJ, Slaughter RS, Garcia ML, Köhler MG. Liu CJ, et al. Assay Drug Dev Technol. 2006 Feb;4(1):37-48. doi: 10.1089/adt.2006.4.37. Assay Drug Dev Technol. 2006. PMID: 16506887
60 results