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Items: 1 to 50 of 59

1.

MEN1309/OBT076, a First-In-Class Antibody-Drug Conjugate Targeting CD205 in Solid Tumors.

Merlino G, Fiascarelli A, Bigioni M, Bressan A, Carrisi C, Bellarosa D, Salerno M, Bugianesi R, Manno R, Bernadó Morales C, Arribas J, Dusek RL, Ackroyd JE, Pham PH, Awdew R, Aud D, Trang M, Lynch CM, Terrett J, Wilson KE, Rohlff C, Manzini S, Pellacani A, Binaschi M.

Mol Cancer Ther. 2019 Sep;18(9):1533-1543. doi: 10.1158/1535-7163.MCT-18-0624. Epub 2019 Jun 21.

PMID:
31227646
2.

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.

Bioorg Med Chem Lett. 2019 Jul 15;29(14):1842-1848. doi: 10.1016/j.bmcl.2019.04.050. Epub 2019 May 2.

PMID:
31109791
3.

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.

ACS Med Chem Lett. 2017 Jan 23;8(2):221-226. doi: 10.1021/acsmedchemlett.6b00443. eCollection 2017 Feb 9.

4.

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.

ACS Med Chem Lett. 2016 Oct 12;7(12):1107-1111. eCollection 2016 Dec 8.

5.

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.

Bioorg Med Chem Lett. 2016 Jun 15;26(12):2947-2951. doi: 10.1016/j.bmcl.2016.04.018.

PMID:
27240550
6.

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.

J Med Chem. 2016 Mar 10;59(5):1818-29. doi: 10.1021/acs.jmedchem.5b01293. Epub 2016 Feb 22.

PMID:
26871940
7.

Gender-related differential effect of tachykinin NK2 receptor-mediated visceral hyperalgesia in guinea pig colon.

Bellucci F, Buéno L, Bugianesi R, Crea A, D'Aranno V, Meini S, Santicioli P, Tramontana M, Maggi CA.

Br J Pharmacol. 2016 Apr;173(8):1329-38. doi: 10.1111/bph.13427. Epub 2016 Mar 7.

8.

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.

ACS Med Chem Lett. 2013 Sep 8;4(11):1064-8. doi: 10.1021/ml4002612. eCollection 2013 Nov 14.

9.

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.

J Med Chem. 2012 Nov 26;55(22):9847-55. doi: 10.1021/jm301056k. Epub 2012 Nov 12.

PMID:
23098566
10.

Characterization of the substituted N-triazole oxindole TROX-1, a small-molecule, state-dependent inhibitor of Ca(V)2 calcium channels.

Swensen AM, Herrington J, Bugianesi RM, Dai G, Haedo RJ, Ratliff KS, Smith MM, Warren VA, Arneric SP, Eduljee C, Parker D, Snutch TP, Hoyt SB, London C, Duffy JL, Kaczorowski GJ, McManus OB.

Mol Pharmacol. 2012 Mar;81(3):488-97. doi: 10.1124/mol.111.075226. Epub 2011 Dec 21.

PMID:
22188924
11.

A potent and selective indole N-type calcium channel (Ca(v)2.2) blocker for the treatment of pain.

Tyagarajan S, Chakravarty PK, Park M, Zhou B, Herrington JB, Ratliff K, Bugianesi RM, Williams B, Haedo RJ, Swensen AM, Warren VA, Smith M, Garcia M, Kaczorowski GJ, McManus OB, Lyons KA, Li X, Madeira M, Karanam B, Green M, Forrest MJ, Abbadie C, McGowan E, Mistry S, Jochnowitz N, Duffy JL.

Bioorg Med Chem Lett. 2011 Jan 15;21(2):869-73. doi: 10.1016/j.bmcl.2010.11.067. Epub 2010 Nov 21.

PMID:
21195616
12.

Analgesic effects of a substituted N-triazole oxindole (TROX-1), a state-dependent, voltage-gated calcium channel 2 blocker.

Abbadie C, McManus OB, Sun SY, Bugianesi RM, Dai G, Haedo RJ, Herrington JB, Kaczorowski GJ, Smith MM, Swensen AM, Warren VA, Williams B, Arneric SP, Eduljee C, Snutch TP, Tringham EW, Jochnowitz N, Liang A, Euan MacIntyre D, McGowan E, Mistry S, White VV, Hoyt SB, London C, Lyons KA, Bunting PB, Volksdorf S, Duffy JL.

J Pharmacol Exp Ther. 2010 Aug;334(2):545-55. doi: 10.1124/jpet.110.166363. Epub 2010 May 3.

PMID:
20439438
13.

Antitumor activity of delimotecan against human metastatic melanoma: pharmacokinetics and molecular determinants.

Bigioni M, Parlani M, Bressan A, Bellarosa D, Rivoltini L, Animati F, Crea A, Bugianesi R, Maggi CA, Manzini S, Binaschi M.

Int J Cancer. 2009 Nov 15;125(10):2456-64. doi: 10.1002/ijc.24661.

14.

A high-throughput assay for evaluating state dependence and subtype selectivity of Cav2 calcium channel inhibitors.

Dai G, Haedo RJ, Warren VA, Ratliff KS, Bugianesi RM, Rush A, Williams ME, Herrington J, Smith MM, McManus OB, Swensen AM.

Assay Drug Dev Technol. 2008 Apr;6(2):195-212. doi: 10.1089/adt.2008.136.

PMID:
18471074
15.

Absorption and metabolism of bioactive molecules after oral consumption of cooked edible heads of Cynara scolymus L. (cultivar Violetto di Provenza) in human subjects: a pilot study.

Azzini E, Bugianesi R, Romano F, Di Venere D, Miccadei S, Durazzo A, Foddai MS, Catasta G, Linsalata V, Maiani G.

Br J Nutr. 2007 May;97(5):963-9.

PMID:
17408528
16.

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.

Diabetes. 2006 Apr;55(4):1034-42. Erratum in: Diabetes. 2006 Jun;55(6):1904.

17.

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.

Assay Drug Dev Technol. 2006 Feb;4(1):37-48.

PMID:
16506887
18.

A cell-sparing electric field stimulation technique for high-throughput screening of voltage-gated ion channels.

Bugianesi RM, Augustine PR, Azer K, Dufresne C, Herrington J, Kath GS, McManus OB, Napolitano CS, Rush A, Sachs J, Simpson N, Wismer MK, Kaczorowski GJ, Slaughter RS.

Assay Drug Dev Technol. 2006 Feb;4(1):21-35.

PMID:
16506886
19.

Biophysical and pharmacological properties of the voltage-gated potassium current of human pancreatic beta-cells.

Herrington J, Sanchez M, Wunderler D, Yan L, Bugianesi RM, Dick IE, Clark SA, Brochu RM, Priest BT, Kohler MG, McManus OB.

J Physiol. 2005 Aug 15;567(Pt 1):159-75. Epub 2005 Jun 2.

20.

Synthesis and SAR of 2,3-diarylpyrrole inhibitors of parasite cGMP-dependent protein kinase as novel anticoccidial agents.

Biftu T, Feng D, Ponpipom M, Girotra N, Liang GB, Qian X, Bugianesi R, Simeone J, Chang L, Gurnett A, Liberator P, Dulski P, Leavitt PS, Crumley T, Misura A, Murphy T, Rattray S, Samaras S, Tamas T, Mathew J, Brown C, Thompson D, Schmatz D, Fisher M, Wyvratt M.

Bioorg Med Chem Lett. 2005 Jul 1;15(13):3296-301.

PMID:
15922595
21.

Stichodactyla helianthus peptide, a pharmacological tool for studying Kv3.2 channels.

Yan L, Herrington J, Goldberg E, Dulski PM, Bugianesi RM, Slaughter RS, Banerjee P, Brochu RM, Priest BT, Kaczorowski GJ, Rudy B, Garcia ML.

Mol Pharmacol. 2005 May;67(5):1513-21. Epub 2005 Feb 11.

PMID:
15709110
22.

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.

Bioorg Med Chem Lett. 2005 Jan 17;15(2):447-51.

PMID:
15603971
23.

Effect of domestic cooking on human bioavailability of naringenin, chlorogenic acid, lycopene and beta-carotene in cherry tomatoes.

Bugianesi R, Salucci M, Leonardi C, Ferracane R, Catasta G, Azzini E, Maiani G.

Eur J Nutr. 2004 Dec;43(6):360-6. Epub 2004 Apr 5.

PMID:
15309458
24.

Expression of voltage-gated potassium channels in human and rhesus pancreatic islets.

Yan L, Figueroa DJ, Austin CP, Liu Y, Bugianesi RM, Slaughter RS, Kaczorowski GJ, Kohler MG.

Diabetes. 2004 Mar;53(3):597-607.

25.

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.

Biochemistry. 2003 Nov 25;42(46):13698-707.

PMID:
14622016
26.

Plasma antioxidants from chocolate.

Serafini M, Bugianesi R, Maiani G, Valtuena S, De Santis S, Crozier A.

Nature. 2003 Aug 28;424(6952):1013. No abstract available.

PMID:
12944955
27.

Effect of acute ingestion of fresh and stored lettuce (Lactuca sativa) on plasma total antioxidant capacity and antioxidant levels in human subjects.

Serafini M, Bugianesi R, Salucci M, Azzini E, Raguzzini A, Maiani G.

Br J Nutr. 2002 Dec;88(6):615-23.

PMID:
12493083
28.

Naringenin from cooked tomato paste is bioavailable in men.

Bugianesi R, Catasta G, Spigno P, D'Uva A, Maiani G.

J Nutr. 2002 Nov;132(11):3349-52.

PMID:
12421849
29.

Modification of the pyridine moiety of non-peptidyl indole GnRH receptor antagonists.

Simeone JP, Bugianesi RL, Ponpipom MM, Yang YT, Lo JL, Yudkovitz JB, Cui J, Mount GR, Ren RN, Creighton M, Mao AH, Vincent SH, Cheng K, Goulet MT.

Bioorg Med Chem Lett. 2002 Nov 18;12(22):3329-32.

PMID:
12392744
30.

Nutritional value of cherry tomatoes (Lycopersicon esculentum Cv. Naomi F1) harvested at different ripening stages.

Raffo A, Leonardi C, Fogliano V, Ambrosino P, Salucci M, Gennaro L, Bugianesi R, Giuffrida F, Quaglia G.

J Agric Food Chem. 2002 Oct 23;50(22):6550-6.

PMID:
12381148
31.

Flavonoids uptake and their effect on cell cycle of human colon adenocarcinoma cells (Caco2).

Salucci M, Stivala LA, Maiani G, Bugianesi R, Vannini V.

Br J Cancer. 2002 May 20;86(10):1645-51.

32.

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.

Biochemistry. 2002 Jun 18;41(24):7781-94.

PMID:
12056910
33.

Accumulation and interactions of beta-carotene and alpha-tocopherol in patients with adenomatous polyps.

Simone F, Pappalardo G, Maiani G, Guadalaxara A, Bugianesi R, Conte AM, Azzini E, Mobarhan S.

Eur J Clin Nutr. 2002 Jun;56(6):546-50.

34.

High-performance liquid chromatography with coulometric electrode array detector for the determination of quercetin levels in cells of the immune system.

Bugianesi R, Serafini M, Simone F, Wu D, Meydani S, Ferro-Luzzi A, Azzini E, Maiani G.

Anal Biochem. 2000 Sep 10;284(2):296-300.

PMID:
10964412
35.

Identification and biochemical characterization of a novel nortriterpene inhibitor of the human lymphocyte voltage-gated potassium channel, Kv1.3.

Felix JP, Bugianesi RM, Schmalhofer WA, Borris R, Goetz MA, Hensens OD, Bao JM, Kayser F, Parsons WH, Rupprecht K, Garcia ML, Kaczorowski GJ, Slaughter RS.

Biochemistry. 1999 Apr 20;38(16):4922-30.

PMID:
10213593
36.

Subunit composition of brain voltage-gated potassium channels determined by hongotoxin-1, a novel peptide derived from Centruroides limbatus venom.

Koschak A, Bugianesi RM, Mitterdorfer J, Kaczorowski GJ, Garcia ML, Knaus HG.

J Biol Chem. 1998 Jan 30;273(5):2639-44.

37.

Blockade of the voltage-gated potassium channel Kv1.3 inhibits immune responses in vivo.

Koo GC, Blake JT, Talento A, Nguyen M, Lin S, Sirotina A, Shah K, Mulvany K, Hora D Jr, Cunningham P, Wunderler DL, McManus OB, Slaughter R, Bugianesi R, Felix J, Garcia M, Williamson J, Kaczorowski G, Sigal NH, Springer MS, Feeney W.

J Immunol. 1997 Jun 1;158(11):5120-8.

PMID:
9164927
38.

Margatoxin binds to a homomultimer of K(V)1.3 channels in Jurkat cells. Comparison with K(V)1.3 expressed in CHO cells.

Helms LM, Felix JP, Bugianesi RM, Garcia ML, Stevens S, Leonard RJ, Knaus HG, Koch R, Wanner SG, Kaczorowski GJ, Slaughter RS.

Biochemistry. 1997 Mar 25;36(12):3737-44.

PMID:
9132027
39.

Inhibition of stromelysin-1 (MMP-3) by P1'-biphenylylethyl carboxyalkyl dipeptides.

Esser CK, Bugianesi RL, Caldwell CG, Chapman KT, Durette PL, Girotra NN, Kopka IE, Lanza TJ, Levorse DA, MacCoss M, Owens KA, Ponpipom MM, Simeone JP, Harrison RK, Niedzwiecki L, Becker JW, Marcy AI, Axel MG, Christen AJ, McDonnell J, Moore VL, Olszewski JM, Saphos C, Visco DM, Hagmann WK, et al.

J Med Chem. 1997 Mar 14;40(6):1026-40.

PMID:
9083493
40.

Structure-activity relationships of C1 and C6 side chains of zaragozic acid A derivatives.

Ponpipom MM, Girotra NN, Bugianesi RL, Roberts CD, Berger GD, Burk RM, Marquis RW, Parsons WH, Bartizal KF, Bergstom JD, et al.

J Med Chem. 1994 Nov 11;37(23):4031-51.

PMID:
7966163
41.

Chemical synthesis and structure-function studies of margatoxin, a potent inhibitor of voltage-dependent potassium channel in human T lymphocytes.

Bednarek MA, Bugianesi RM, Leonard RJ, Felix JP.

Biochem Biophys Res Commun. 1994 Jan 28;198(2):619-25.

PMID:
8297371
43.

Metabolism of the platelet-activating factor antagonist (+/-)-trans-2-(3'-methoxy-5'-methylsulphonyl-4'-propoxyphenyl)-5-(3",4" ,5"- trimethoxyphenyl)tetrahydrofuran (L-659,989) in rhesus monkeys.

Thomson KL, Chang MN, Bugianesi RL, Ponpipom MM, Arison BH, Hucker HB, Sweeney BM, White SD, Chabala JC.

Xenobiotica. 1991 May;21(5):613-25.

PMID:
1949894
44.

Biochemical and pharmacological characterization of L-659,989: an extremely potent, selective and competitive receptor antagonist of platelet-activating factor.

Hwang SB, Lam MH, Alberts AW, Bugianesi RL, Chabala JC, Ponpipom MM.

J Pharmacol Exp Ther. 1988 Aug;246(2):534-41.

PMID:
2841449
45.

(+/-)-trans-2-(3-Methoxy-5-methylsulfonyl-4-propoxyphenyl)-5-(3,4,5- trimethoxyphenyl)tetrahydrofuran (L-659,989), a novel, potent PAF receptor antagonist.

Ponpipom MM, Hwang SB, Doebber TW, Acton JJ, Alberts AW, Biftu T, Brooker DR, Bugianesi RL, Chabala JC, Gamble NL, et al.

Biochem Biophys Res Commun. 1988 Feb 15;150(3):1213-20. Erratum in: Biochem Biophys Res Commun 1988 Apr 29;152(2):949.

PMID:
2829894
46.

Inhibition of delayed hypersensitivity reactions by cinnamyl 1-thioglycosides.

Ponpipom MM, Bugianesi RL, Blake TJ.

J Med Chem. 1987 Apr;30(4):705-10.

PMID:
3494125
47.

Structure-activity relationships of kadsurenone analogues.

Ponpipom MM, Bugianesi RL, Brooker DR, Yue BZ, Hwang SB, Shen TY.

J Med Chem. 1987 Jan;30(1):136-42.

PMID:
3027330
48.

Targeting of synthetically glycosylated human placental glucocerebrosidase.

Murray GJ, Doebber TW, Shen TY, Wu MS, Ponpipom MM, Bugianesi RL, Brady RO, Barranger JA.

Biochem Med. 1985 Oct;34(2):241-6.

PMID:
4084247
49.

Enhanced macrophage uptake of synthetically glycosylated human placental beta-glucocerebrosidase.

Doebber TW, Wu MS, Bugianesi RL, Ponpipom MM, Furbish FS, Barranger JA, Brady RO, Shen TY.

J Biol Chem. 1982 Mar 10;257(5):2193-9. No abstract available.

50.

Cell-specific ligands for selective drug delivery to tissues and organs.

Ponpipom MM, Bugianesi RL, Robbins JC, Doebber TW, Shen TY.

J Med Chem. 1981 Dec;24(12):1388-95.

PMID:
7310815

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