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Page 1
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.
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.
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
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
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
Aminopiperidine sulfonamide Cav2.2 channel inhibitors for the treatment of chronic pain.
Shao PP, Ye F, Chakravarty PK, Varughese DJ, 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. J Med Chem. 2012 Nov 26;55(22):9847-55. doi: 10.1021/jm301056k. Epub 2012 Nov 12. J Med Chem. 2012. PMID: 23098566
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.
Potent Kv1.3 inhibitors from correolide-modification of the C18 position.
Bao J, Miao S, Kayser F, Kotliar AJ, Baker RK, Doss GA, Felix JP, Bugianesi RM, Slaughter RS, Kaczorowski GJ, Garcia ML, Ha SN, Castonguay L, Koo GC, Shah K, Springer MS, Staruch MJ, Parsons WH, Rupprecht KM. Bao J, et al. Bioorg Med Chem Lett. 2005 Jan 17;15(2):447-51. doi: 10.1016/j.bmcl.2004.10.058. Bioorg Med Chem Lett. 2005. PMID: 15603971
Identification of a new class of inhibitors of the voltage-gated potassium channel, Kv1.3, with immunosuppressant properties.
Schmalhofer WA, Bao J, McManus OB, Green B, Matyskiela M, Wunderler D, Bugianesi RM, Felix JP, Hanner M, Linde-Arias AR, Ponte CG, Velasco L, Koo G, Staruch MJ, Miao S, Parsons WH, Rupprecht K, Slaughter RS, Kaczorowski GJ, Garcia ML. Schmalhofer WA, et al. Biochemistry. 2002 Jun 18;41(24):7781-94. doi: 10.1021/bi025722c. Biochemistry. 2002. PMID: 12056910
Substitution of a single residue in Stichodactyla helianthus peptide, ShK-Dap22, reveals a novel pharmacological profile.
Middleton RE, Sanchez M, Linde AR, Bugianesi RM, Dai G, Felix JP, Koprak SL, Staruch MJ, Bruguera M, Cox R, Ghosh A, Hwang J, Jones S, Kohler M, Slaughter RS, McManus OB, Kaczorowski GJ, Garcia ML. Middleton RE, et al. Among authors: bugianesi rm. Biochemistry. 2003 Nov 25;42(46):13698-707. doi: 10.1021/bi035209e. Biochemistry. 2003. PMID: 14622016
60 results