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Items: 1 to 50 of 51

1.

Anti-diabetic efficacy and impact on amino acid metabolism of GRA1, a novel small-molecule glucagon receptor antagonist.

Mu J, Qureshi SA, Brady EJ, Muise ES, Candelore MR, Jiang G, Li Z, Wu MS, Yang X, Dallas-Yang Q, Miller C, Xiong Y, Langdon RB, Parmee ER, Zhang BB.

PLoS One. 2012;7(11):e49572. doi: 10.1371/journal.pone.0049572. Epub 2012 Nov 19.

2.

Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes.

Xiong Y, Guo J, Candelore MR, Liang R, Miller C, Dallas-Yang Q, Jiang G, McCann PE, Qureshi SA, Tong X, Xu SS, Shang J, Vincent SH, Tota LM, Wright MJ, Yang X, Zhang BB, Tata JR, Parmee ER.

J Med Chem. 2012 Jul 12;55(13):6137-48. doi: 10.1021/jm300579z. Epub 2012 Jun 28.

PMID:
22708876
3.

Discovery of novel, potent, selective, and orally active human glucagon receptor antagonists containing a pyrazole core.

Shen DM, Brady EJ, Candelore MR, Dallas-Yang Q, Ding VD, Feeney WP, Jiang G, McCann ME, Mock S, Qureshi SA, Saperstein R, Shen X, Tong X, Tota LM, Wright MJ, Yang X, Zheng S, Chapman KT, Zhang BB, Tata JR, Parmee ER.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):76-81. doi: 10.1016/j.bmcl.2010.11.074. Epub 2010 Nov 21.

PMID:
21147532
4.

Discovery of potent, orally active benzimidazole glucagon receptor antagonists.

Kim RM, Chang J, Lins AR, Brady E, Candelore MR, Dallas-Yang Q, Ding V, Dragovic J, Iliff S, Jiang G, Mock S, Qureshi S, Saperstein R, Szalkowski D, Tamvakopoulos C, Tota L, Wright M, Yang X, Tata JR, Chapman K, Zhang BB, Parmee ER.

Bioorg Med Chem Lett. 2008 Jul 1;18(13):3701-5. doi: 10.1016/j.bmcl.2008.05.072. Epub 2008 May 22.

PMID:
18539028
5.

Cloning and expression of canine glucagon receptor and its use to evaluate glucagon receptor antagonists in vitro and in vivo.

Yang X, Yates ML, Candelore MR, Feeney W, Hora D, Kim RM, Parmee ER, Berger JP, Zhang BB, Qureshi SA.

Eur J Pharmacol. 2007 Jan 19;555(1):8-16. Epub 2006 Oct 21.

PMID:
17140563
6.

Design and synthesis of conformationally constrained tri-substituted ureas as potent antagonists of the human glucagon receptor.

Liang R, Abrardo L, Brady EJ, Candelore MR, Ding V, Saperstein R, Tota LM, Wright M, Mock S, Tamvakopolous C, Tong S, Zheng S, Zhang BB, Tata JR, Parmee ER.

Bioorg Med Chem Lett. 2007 Feb 1;17(3):587-92. Epub 2006 Nov 10.

PMID:
17126016
7.

Direct observation (NMR) of the efficacy of glucagon receptor antagonists in murine liver expressing the human glucagon receptor.

Cohen SM, Duffy JL, Miller C, Kirk BA, Candelore MR, Ding VD, Kaczorowski G, Tota LM, Werrmann JG, Wright M, Parmee ER, Tata JR, Zhang BB.

Bioorg Med Chem. 2006 Mar 1;14(5):1506-17. Epub 2005 Oct 25.

PMID:
16256355
8.

Discovery of novel, potent, and orally active spiro-urea human glucagon receptor antagonists.

Shen DM, Zhang F, Brady EJ, Candelore MR, Dallas-Yang Q, Ding VD, Dragovic J, Feeney WP, Jiang G, McCann PE, Mock S, Qureshi SA, Saperstein R, Shen X, Tamvakopoulos C, Tong X, Tota LM, Wright MJ, Yang X, Zheng S, Chapman KT, Zhang BB, Tata JR, Parmee ER.

Bioorg Med Chem Lett. 2005 Oct 15;15(20):4564-9.

PMID:
16102966
9.

Discovery and investigation of a novel class of thiophene-derived antagonists of the human glucagon receptor.

Duffy JL, Kirk BA, Konteatis Z, Campbell EL, Liang R, Brady EJ, Candelore MR, Ding VD, Jiang G, Liu F, Qureshi SA, Saperstein R, Szalkowski D, Tong S, Tota LM, Xie D, Yang X, Zafian P, Zheng S, Chapman KT, Zhang BB, Tata JR.

Bioorg Med Chem Lett. 2005 Mar 1;15(5):1401-5.

PMID:
15713396
10.

Hepatic glucagon receptor binding and glucose-lowering in vivo by peptidyl and non-peptidyl glucagon receptor antagonists.

Dallas-Yang Q, Shen X, Strowski M, Brady E, Saperstein R, Gibson RE, Szalkowski D, Qureshi SA, Candelore MR, Fenyk-Melody JE, Parmee ER, Zhang BB, Jiang G.

Eur J Pharmacol. 2004 Oct 6;501(1-3):225-34.

PMID:
15464082
11.

Phytosphingosine 1-phosphate: a high affinity ligand for the S1P(4)/Edg-6 receptor.

Candelore MR, Wright MJ, Tota LM, Milligan J, Shei GJ, Bergstrom JD, Mandala SM.

Biochem Biophys Res Commun. 2002 Sep 27;297(3):600-6.

PMID:
12270137
12.

Beta(3)-adrenoceptor agonist-induced increases in lipolysis, metabolic rate, facial flushing, and reflex tachycardia in anesthetized rhesus monkeys.

Hom GJ, Forrest MJ, Bach TJ, Brady E, Candelore MR, Cascieri MA, Fletcher DJ, Fisher MH, Iliff SA, Mathvink R, Metzger J, Pecore V, Saperstein R, Shih T, Weber AE, Wyvratt M, Zafian P, MacIntyre DE.

J Pharmacol Exp Ther. 2001 Apr;297(1):299-307.

PMID:
11259557
13.

Human beta3 adrenergic receptor agonists containing cyanoguanidine and nitroethylenediamine moieties.

Brockunier LL, Candelore MR, Cascieri MA, Liu Y, Tota L, Wyvratt MJ, Fisher MH, Weber AE, Parmee ER.

Bioorg Med Chem Lett. 2001 Feb 12;11(3):379-82.

PMID:
11212115
14.

Tetrahydroisoquinoline derivatives containing a benzenesulfonamide moiety as potent, selective human beta3 adrenergic receptor agonists.

Parmee ER, Brockunier LL, He J, Singh SB, Candelore MR, Cascieri MA, Deng L, Liu Y, Tota L, Wyvratt MJ, Fisher MH, Weber AE.

Bioorg Med Chem Lett. 2000 Oct 16;10(20):2283-6.

PMID:
11055339
15.

Discovery of a potent, orally bioavailable beta(3) adrenergic receptor agonist, (R)-N-[4-[2-[[2-hydroxy-2-(3-pyridinyl)ethyl]amino]ethyl]phenyl]-4-[4 -[4-(trifluoromethyl)phenyl]thiazol-2-yl]benzenesulfonamide.

Mathvink RJ, Tolman JS, Chitty D, Candelore MR, Cascieri MA, Colwell LF Jr, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Miller RR, Stearns RA, Tota L, Wyvratt MJ, Fisher MH, Weber AE.

J Med Chem. 2000 Oct 19;43(21):3832-6.

PMID:
11052788
16.

L-750355, a human beta3-adrenoceptor agonist; in vitro pharmacology and profile of activity in vivo in the rhesus monkey.

Forrest MJ, Hom G, Bach T, Candelore MR, Cascieri MA, Strader C, Tota L, Fisher MH, Szumiloski J, Ok HO, Weber AE, Wyvratt M, Vicario P, Marko O, Deng L, Cioffe C, Hegarty-Friscino B, MacIntyre E.

Eur J Pharmacol. 2000 Oct 27;407(1-2):175-81.

PMID:
11050305
17.

Human beta3-adrenergic receptor agonists containing 1,2,3-triazole-substituted benzenesulfonamides.

Brockunier LL, Parmee ER, Ok HO, Candelore MR, Cascieri MA, Colwell LF Jr, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Tota L, Wyvratt MJ, Fisher MH, Weber AE.

Bioorg Med Chem Lett. 2000 Sep 18;10(18):2111-4.

PMID:
10999482
18.

Potent, selective 3-pyridylethanolamine beta3 adrenergic receptor agonists possessing a thiazole benzenesulfonamide pharmacophore.

Mathvink RJ, Tolman JS, Chitty D, Candelore MR, Cascieri MA, Colwell LF Jr, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Tota L, Wyvratt MJ, Fisher MH, Weber AE.

Bioorg Med Chem Lett. 2000 Sep 4;10(17):1971-3.

PMID:
10987429
19.

Substituted oxazole benzenesulfonamides as potent human beta3 adrenergic receptor agonists.

Ok HO, Reigle LB, Candelore MR, Cascieri MA, Colwell LF, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Strader CD, Tota L, Wang P, Wyvratt MJ, Fisher MH, Weber AE.

Bioorg Med Chem Lett. 2000 Jul 17;10(14):1531-4.

PMID:
10915043
20.

Synthesis and SAR of benzyl and phenoxymethylene oxadiazole benzenesulfonamides as selective beta3 adrenergic receptor agonist antiobesity agents.

Biftu T, Feng DD, Liang GB, Kuo H, Qian X, Naylor EM, Colandrea VJ, Candelore MR, Cascieri MA, Colwell LF Jr, Forrest MJ, Hom GJ, MacIntyre DE, Stearns RA, Strader CD, Wyvratt MJ, Fisher MH, Weber AE.

Bioorg Med Chem Lett. 2000 Jul 3;10(13):1431-4.

PMID:
10888325
21.

Discovery of an orally bioavailable alkyl oxadiazole beta3 adrenergic receptor agonist.

Feng DD, Biftu T, Candelore MR, Cascieri MA, Colwell LF Jr, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Miller RR, Stearns RA, Strader CD, Tota L, Wyvratt MJ, Fisher MH, Weber AE.

Bioorg Med Chem Lett. 2000 Jul 3;10(13):1427-9.

PMID:
10888324
22.

Potent and selective human beta(3)-adrenergic receptor antagonists.

Candelore MR, Deng L, Tota L, Guan XM, Amend A, Liu Y, Newbold R, Cascieri MA, Weber AE.

J Pharmacol Exp Ther. 1999 Aug;290(2):649-55.

PMID:
10411574
23.

Potent, elective human beta3 adrenergic receptor agonists containing a substituted indoline-5-sulfonamide pharmacophore.

Mathvink RJ, Barritta AM, Candelore MR, Cascieri MA, Deng L, Tota L, Strader CD, Wyvratt MJ, Fisher MH, Weber AE.

Bioorg Med Chem Lett. 1999 Jul 5;9(13):1869-74.

PMID:
10406657
24.

L-770,644: a potent and selective human beta3 adrenergic receptor agonist with improved oral bioavailability.

Shih TL, Candelore MR, Cascieri MA, Chiu SH, Colwell LF Jr, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Miller RR, Stearns RA, Strader CD, Tota L, Wyvratt MJ, Fisher MH, Weber AE.

Bioorg Med Chem Lett. 1999 May 3;9(9):1251-4.

PMID:
10340609
25.

Acute effect of ephedrine on 24-h energy balance.

Shannon JR, Gottesdiener K, Jordan J, Chen K, Flattery S, Larson PJ, Candelore MR, Gertz B, Robertson D, Sun M.

Clin Sci (Lond). 1999 May;96(5):483-91.

PMID:
10209080
26.

Human beta3 adrenergic receptor agonists containing imidazolidinone and imidazolone benzenesulfonamides.

Naylor EM, Parmee ER, Colandrea VJ, Perkins L, Brockunier L, Candelore MR, Cascieri MA, Colwell LF Jr, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Strader CD, Tota L, Wang PR, Wyvratt MJ, Fisher MH, Weber AE.

Bioorg Med Chem Lett. 1999 Mar 8;9(5):755-8.

PMID:
10201842
27.

Human beta3 adrenergic receptor agonists containing cyclic ureidobenzenesulfonamides.

Parmee ER, Naylor EM, Perkins L, Colandrea VJ, Ok HO, Candelore MR, Cascieri MA, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Miller RR, Stearns RA, Strader CD, Tota L, Wyvratt MJ, Fisher MH, Weber AE.

Bioorg Med Chem Lett. 1999 Mar 8;9(5):749-54.

PMID:
10201841
28.

3-Pyridylethanolamines: potent and selective human beta 3 adrenergic receptor agonists.

Naylor EM, Colandrea VJ, Candelore MR, Cascieri MA, Colwell LF Jr, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Strader CD, Tota L, Wang PR, Wyvratt MJ, Fisher MH, Weber AE.

Bioorg Med Chem Lett. 1998 Nov 3;8(21):3087-92.

PMID:
9873681
29.

3-Pyridyloxypropanolamine agonists of the beta 3 adrenergic receptor with improved pharmacokinetic properties.

Weber AE, Ok HO, Alvaro RF, Candelore MR, Cascieri MA, Chiu SH, Deng L, Forrest MJ, Hom GJ, Hutchins JE, Kao J, MacIntyre DE, Mathvink RJ, McLoughlin D, Miller RR, Newbold RC, Olah TV, Parmee ER, Perkins L, Stearns RA, Strader CD, Szumiloski J, Tang YS, Tota L, Fisher MH, et al.

Bioorg Med Chem Lett. 1998 Aug 18;8(16):2111-6.

PMID:
9873496
30.

Discovery of L-755,507: a subnanomolar human beta 3 adrenergic receptor agonist.

Parmee ER, Ok HO, Candelore MR, Tota L, Deng L, Strader CD, Wyvratt MJ, Fisher MH, Weber AE.

Bioorg Med Chem Lett. 1998 May 5;8(9):1107-12.

PMID:
9871717
31.

Potent, selective benzenesulfonamide agonists of the human beta 3 adrenergic receptor.

Weber AE, Mathvink RJ, Perkins L, Hutchins JE, Candelore MR, Tota L, Strader CD, Wyvratt MJ, Fisher MH.

Bioorg Med Chem Lett. 1998 May 5;8(9):1101-6.

PMID:
9871716
32.

Peroxisome proliferator-activated receptors gamma and alpha mediate in vivo regulation of uncoupling protein (UCP-1, UCP-2, UCP-3) gene expression.

Kelly LJ, Vicario PP, Thompson GM, Candelore MR, Doebber TW, Ventre J, Wu MS, Meurer R, Forrest MJ, Conner MW, Cascieri MA, Moller DE.

Endocrinology. 1998 Dec;139(12):4920-7.

PMID:
9832429
33.

Beta-3 adrenergic receptor agonists cause an increase in gastrointestinal transit time in wild-type mice, but not in mice lacking the beta-3 adrenergic receptor.

Fletcher DS, Candelore MR, Grujic D, Lowell BB, Luell S, Susulic VS, Macintyre DE.

J Pharmacol Exp Ther. 1998 Nov;287(2):720-4.

PMID:
9808702
34.

A selective human beta3 adrenergic receptor agonist increases metabolic rate in rhesus monkeys.

Fisher MH, Amend AM, Bach TJ, Barker JM, Brady EJ, Candelore MR, Carroll D, Cascieri MA, Chiu SH, Deng L, Forrest MJ, Hegarty-Friscino B, Guan XM, Hom GJ, Hutchins JE, Kelly LJ, Mathvink RJ, Metzger JM, Miller RR, Ok HO, Parmee ER, Saperstein R, Strader CD, Stearns RA, MacIntyre DE, et al.

J Clin Invest. 1998 Jun 1;101(11):2387-93.

35.

Desensitization of beta3-adrenergic receptor-stimulated adenylyl cyclase activity and lipolysis in rats.

Vicario PP, Candelore MR, Schaeffer MT, Kelly L, Thompson GM, Brady EJ, Saperstein R, MacIntyre DE, Tota LM, Cascieri MA.

Life Sci. 1998;62(7):627-38.

PMID:
9472722
36.

Molecular approaches to the discovery of new treatments for obesity.

Strader CD, MacIntyre DE, Candelore MR, Parker EM.

Curr Opin Chem Biol. 1997 Aug;1(2):204-9. Review.

PMID:
9667852
37.

Pharmacological characterization of a recently described human beta 3-adrenergic receptor mutant.

Candelore MR, Deng L, Tota LM, Kelly LJ, Cascieri MA, Strader CD.

Endocrinology. 1996 Jun;137(6):2638-41.

PMID:
8641219
38.

Isolation of a preadipocyte cell line from rat bone marrow and differentiation to adipocytes.

Marko O, Cascieri MA, Ayad N, Strader CD, Candelore MR.

Endocrinology. 1995 Oct;136(10):4582-8.

PMID:
7545105
39.

Allele-specific activation of genetically engineered receptors.

Strader CD, Gaffney T, Sugg EE, Candelore MR, Keys R, Patchett AA, Dixon RA.

J Biol Chem. 1991 Jan 5;266(1):5-8.

40.

Biophysical and genetic analysis of the ligand-binding site of the beta-adrenoceptor.

Tota MR, Candelore MR, Dixon RA, Strader CD.

Trends Pharmacol Sci. 1991 Jan;12(1):4-6. Review. No abstract available.

PMID:
1848734
41.

Mutational analysis of beta-adrenergic receptor glycosylation.

Rands E, Candelore MR, Cheung AH, Hill WS, Strader CD, Dixon RA.

J Biol Chem. 1990 Jun 25;265(18):10759-64.

42.

A single amino acid substitution in the beta-adrenergic receptor promotes partial agonist activity from antagonists.

Strader CD, Candelore MR, Hill WS, Dixon RA, Sigal IS.

J Biol Chem. 1989 Oct 5;264(28):16470-7.

43.

Identification of two serine residues involved in agonist activation of the beta-adrenergic receptor.

Strader CD, Candelore MR, Hill WS, Sigal IS, Dixon RA.

J Biol Chem. 1989 Aug 15;264(23):13572-8.

44.

Genetic analysis of the molecular basis for beta-adrenergic receptor subtype specificity.

Dixon RA, Hill WS, Candelore MR, Rands E, Diehl RE, Marshall MS, Sigal IS, Strader CD.

Proteins. 1989;6(3):267-74.

PMID:
2560192
45.

Conserved aspartic acid residues 79 and 113 of the beta-adrenergic receptor have different roles in receptor function.

Strader CD, Sigal IS, Candelore MR, Rands E, Hill WS, Dixon RA.

J Biol Chem. 1988 Jul 25;263(21):10267-71.

46.

Mutations that uncouple the beta-adrenergic receptor from Gs and increase agonist affinity.

Strader CD, Dixon RA, Cheung AH, Candelore MR, Blake AD, Sigal IS.

J Biol Chem. 1987 Dec 5;262(34):16439-43. Erratum in: J Biol Chem 1988 Feb 25;263(6):3050.

47.

Structural features required for ligand binding to the beta-adrenergic receptor.

Dixon RA, Sigal IS, Candelore MR, Register RB, Scattergood W, Rands E, Strader CD.

EMBO J. 1987 Nov;6(11):3269-75.

48.

Beta-adrenergic receptor subtype is an intrinsic property of the receptor gene product.

Strader CD, Candelore MR, Rands E, Dixon RA.

Mol Pharmacol. 1987 Aug;32(1):179-83.

PMID:
3039335
49.

Identification of residues required for ligand binding to the beta-adrenergic receptor.

Strader CD, Sigal IS, Register RB, Candelore MR, Rands E, Dixon RA.

Proc Natl Acad Sci U S A. 1987 Jul;84(13):4384-8.

50.

The carboxyl terminus of the hamster beta-adrenergic receptor expressed in mouse L cells is not required for receptor sequestration.

Strader CD, Sigal IS, Blake AD, Cheung AH, Register RB, Rands E, Zemcik BA, Candelore MR, Dixon RA.

Cell. 1987 Jun 19;49(6):855-63.

PMID:
3034435

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