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Mari Rios Candelore

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Yusheng Xiong; Suoyu S Xu; Xiaodong Yang; Bei B Zhang; Sajjad A Qureshi; Jackie Shang; James R Tata; Xinchun Tong; Laurie M Tota; Stella H Vincent; Michael J Wright; Mari Rios Candelore; Qing Dallas-Yang; Jian Guo; Guoqiang Jiang; Rui Liang; Peggy E McCann; Corey Miller; Emma R Parmee
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.
James Mu; Eric S Muise; Emma R Parmee; Sajjad A Qureshi; Margaret S Wu; Yusheng Xiong; Xiaodong Yang; Edward J Brady; Mari Rios Candelore; Qing Dallas-Yang; Guoqiang Jiang; Ronald B Langdon; Zhihua Li; Corey Miller; Bei B Zhang
Anti-diabetic efficacy and impact on amino acid metabolism of GRA1, a novel small-molecule glucagon receptor antagonist.
Dong-Ming Shen; Edward J Brady; Mari Rios Candelore; Qing Dallas-Yang; Victor D H Ding; William P Feeney; Guoquiang Jiang; Margaret E McCann; Steve Mock; Sajjad A Qureshi; Richard Saperstein; Xiaolan Shen; Xinchun Tong; Laurie M Tota; Michael J Wright; Xiaodong Yang; Song Zheng; Kevin Chapman; Bei B Zhang; James R Tata; Emma R Parmee
Discovery of novel, potent, selective, and orally active human glucagon receptor antagonists containing a pyrazole core.

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All Publications

2012: Yusheng Xiong; Suoyu S Xu; Xiaodong Yang; Bei B Zhang; Sajjad A Qureshi; Jackie Shang; James R Tata; Xinchun Tong; Laurie M Tota; Stella H Vincent; Michael J Wright; Mari Rios Candelore; Qing Dallas-Yang; Jian Guo; Guoqiang Jiang; Rui Liang; Peggy E McCann; Corey Miller; Emma R Parmee
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.
Journal of medicinal chemistry 2012;55(13):6137-48.
2012: James Mu; Eric S Muise; Emma R Parmee; Sajjad A Qureshi; Margaret S Wu; Yusheng Xiong; Xiaodong Yang; Edward J Brady; Mari Rios Candelore; Qing Dallas-Yang; Guoqiang Jiang; Ronald B Langdon; Zhihua Li; Corey Miller; Bei B Zhang
Anti-diabetic efficacy and impact on amino acid metabolism of GRA1, a novel small-molecule glucagon receptor antagonist.
PloS one 2012;7(11):e49572.
2011: Dong-Ming Shen; Edward J Brady; Mari Rios Candelore; Qing Dallas-Yang; Victor D H Ding; William P Feeney; Guoquiang Jiang; Margaret E McCann; Steve Mock; Sajjad A Qureshi; Richard Saperstein; Xiaolan Shen; Xinchun Tong; Laurie M Tota; Michael J Wright; Xiaodong Yang; Song Zheng; Kevin Chapman; Bei B Zhang; James R Tata; Emma R Parmee
Discovery of novel, potent, selective, and orally active human glucagon receptor antagonists containing a pyrazole core.
Bioorganic & medicinal chemistry letters 2011;21(1):76-81.
2008: Ronald M Kim; Jiang Chang; Ashley R Lins; Edward J Brady; Mari Rios Candelore; Qing Dallas-Yang; Victor D H Ding; Jasminka Dragovic; Susan Iliff; Guoqiang Jiang; Steve Mock; Sajjad Qureshi; Richard Saperstein; Deborah Szalkowski; Constantin Tamvakopoulos; Laurie M Tota; Michael Wright; Xiaodong Yang; James R Tata; Kevin Chapman; Bei B Zhang; Emma R Parmee
Discovery of potent, orally active benzimidazole glucagon receptor antagonists.
Bioorganic & medicinal chemistry letters 2008;18(13):3701-5.
2007: Rui Liang; Lauren Abrardo; Edward J Brady; Mari Rios Candelore; Victor D H Ding; Richard Saperstein; Laurie M Tota; Michael Wright; Steve Mock; Constantin Tamvakopolous; Sharon Tong; Song Zheng; Bei B Zhang; James R Tata; Emma R Parmee
Design and synthesis of conformationally constrained tri-substituted ureas as potent antagonists of the human glucagon receptor.
Bioorganic & medicinal chemistry letters 2007;17(3):587-92.
2007: Xiaodong Yang; Marla L Yates; Mari Rios Candelore; William P Feeney; Donald F Hora; Ron M Kim; Emma R Parmee; Joel P Berger; Bei B Zhang; Sajjad A Qureshi
Cloning and expression of canine glucagon receptor and its use to evaluate glucagon receptor antagonists in vitro and in vivo.
European journal of pharmacology 2007;555(1):8-16.
2006: Sheila M Cohen; Joseph L Duffy; Corin Miller; Brian A Kirk; Mari Rios Candelore; Victor D H Ding; Gregory Kaczorowski; Laurie M Tota; Jeffrey G Werrmann; Michael Wright; Emma R Parmee; James R Tata; Bei B Zhang
Direct observation (NMR) of the efficacy of glucagon receptor antagonists in murine liver expressing the human glucagon receptor.
Bioorganic & medicinal chemistry 2006;14(5):1506-17.
2005: Dong-Ming Shen; Fengqi Zhang; Edward J Brady; Mari Rios Candelore; Qing Dallas-Yang; Victor D H Ding; Jasminka Dragovic; William P Feeney; Guoquiang Jiang; Peggy E McCann; Steve Mock; Sajjad A Qureshi; Richard Saperstein; Xiaolan Shen; Constantin Tamvakopoulos; Xinchun Tong; Laurie M Tota; Michael J Wright; Xiaodong Yang; Song Zheng; Kevin Chapman; Bei B Zhang; James R Tata; Emma R Parmee
Discovery of novel, potent, and orally active spiro-urea human glucagon receptor antagonists.
Bioorganic & medicinal chemistry letters 2005;15(20):4564-9.
2005: Joseph L Duffy; Brian A Kirk; Zenon Konteatis; Elizabeth L Campbell; Rui Liang; Edward J Brady; Mari Rios Candelore; Victor D H Ding; Guoqiang Jiang; Frank Liu; Sajjad A Qureshi; Richard Saperstein; Deborah Szalkowski; Sharon Tong; Laurie M Tota; Dan Xie; Xiaodong Yang; Peter Zafian; Song Zheng; Kevin Chapman; Bei B Zhang; James R Tata
Discovery and investigation of a novel class of thiophene-derived antagonists of the human glucagon receptor.
Bioorganic & medicinal chemistry letters 2005;15(5):1401-5.
2004: Qing Dallas-Yang; Xiaolan Shen; Mathias Z Strowski; Edward J Brady; Richard Saperstein; Raymond E Gibson; Deborah Szalkowski; Sajjad A Qureshi; Mari Rios Candelore; Judy Fenyk-Melody; Emma R Parmee; Bei B Zhang; Guoqiang Jiang
Hepatic glucagon receptor binding and glucose-lowering in vivo by peptidyl and non-peptidyl glucagon receptor antagonists.
European journal of pharmacology 2004;501(1-3):225-34.
2002: Mari Rios Candelore; Michael J Wright; Laurie M Tota; James A Milligan; Gan-Ju Shei; James Bergstrom; Suzanne Mandala
Phytosphingosine 1-phosphate: a high affinity ligand for the S1P(4)/Edg-6 receptor.
Biochemical and biophysical research communications 2002;297(3):600-6.
2001: Gary J Hom; Michael J Forrest; TJ Bach; Edward J Brady; Mari Rios Candelore; Margaret A Cascieri; D J Fletcher; Michael H Fisher; Susan A Iliff; Robert J Mathvink; J Metzger; V Pecore; Richard Saperstein; T Shih; Ann E Weber; Matthew J Wyvratt; P Zafian; D Euan MacIntyre
Beta(3)-adrenoceptor agonist-induced increases in lipolysis, metabolic rate, facial flushing, and reflex tachycardia in anesthetized rhesus monkeys.
The Journal of pharmacology and experimental therapeutics 2001;297(1):299-307.
2001: Linda L Brockunier; Mari Rios Candelore; Margaret A Cascieri; Y Liu; Laurie M Tota; Matthew J Wyvratt; Michael H Fisher; Ann E Weber; Emma R Parmee
Human beta3 adrenergic receptor agonists containing cyanoguanidine and nitroethylenediamine moieties.
Bioorganic & medicinal chemistry letters 2001;11(3):379-82.
2000: Michael J Forrest; Gary J Hom; TJ Bach; Mari Rios Candelore; Margaret A Cascieri; Catherine D Strader; Laurie M Tota; Michael H Fisher; J Szumiloski; Hyun O Ok; Ann E Weber; Matthew J Wyvratt; Pasquale P Vicario; O Marko; L Deng; C Cioffe; B Hegarty-Friscino; E MacIntyre
L-750355, a human beta3-adrenoceptor agonist; in vitro pharmacology and profile of activity in vivo in the rhesus monkey.
European journal of pharmacology 2000;407(1-2):175-81.
2000: Robert J Mathvink; J S Tolman; Dawn Chitty; Mari Rios Candelore; Margaret A Cascieri; Lawrence F Colwell; L Deng; William P Feeney; Michael J Forrest; Gary J Hom; D Euan MacIntyre; Randall R Miller; Ralph A Stearns; Laurie M Tota; Matthew J Wyvratt; Michael H Fisher; Ann E Weber
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.
Journal of medicinal chemistry 2000;43(21):3832-6.
2000: Emma R Parmee; Linda L Brockunier; Jiafang He; Sheo B Singh; Mari Rios Candelore; Margaret A Cascieri; L Deng; Y Liu; Laurie M Tota; Matthew J Wyvratt; Michael H Fisher; Ann E Weber
Tetrahydroisoquinoline derivatives containing a benzenesulfonamide moiety as potent, selective human beta3 adrenergic receptor agonists.
Bioorganic & medicinal chemistry letters 2000;10(20):2283-6.
2000: Linda L Brockunier; Emma R Parmee; Hyun O Ok; Mari Rios Candelore; Margaret A Cascieri; Lawrence F Colwell; L Deng; William P Feeney; Michael J Forrest; Gary J Hom; D Euan MacIntyre; Laurie M Tota; Matthew J Wyvratt; Michael H Fisher; Ann E Weber
Human beta3-adrenergic receptor agonists containing 1,2,3-triazole-substituted benzenesulfonamides.
Bioorganic & medicinal chemistry letters 2000;10(18):2111-4.
2000: Robert J Mathvink; J S Tolman; Dawn Chitty; Mari Rios Candelore; Margaret A Cascieri; Lawrence F Colwell; L Deng; William P Feeney; Michael J Forrest; Gary J Hom; D Euan MacIntyre; Laurie M Tota; Matthew J Wyvratt; Michael H Fisher; Ann E Weber
Potent, selective 3-pyridylethanolamine beta3 adrenergic receptor agonists possessing a thiazole benzenesulfonamide pharmacophore.
Bioorganic & medicinal chemistry letters 2000;10(17):1971-3.
2000: Hyun O Ok; L B Reigle; Mari Rios Candelore; Margaret A Cascieri; Lawrence F Colwell; L Deng; William P Feeney; Michael J Forrest; Gary J Hom; D Euan MacIntyre; Catherine D Strader; Laurie M Tota; P Wang; Matthew J Wyvratt; Michael H Fisher; Ann E Weber
Substituted oxazole benzenesulfonamides as potent human beta3 adrenergic receptor agonists.
Bioorganic & medicinal chemistry letters 2000;10(14):1531-4.
2000: Szalkowski Deborah; D D Feng; Gui-Bai Liang; H Kuo; Xiaoxia Qian; Elizabeth M Naylor; Vincent J Colandrea; Mari Rios Candelore; Margaret A Cascieri; Lawrence F Colwell; Michael J Forrest; Gary J Hom; D Euan MacIntyre; Ralph A Stearns; Catherine D Strader; Matthew J Wyvratt; Michael H Fisher; Ann E Weber
Synthesis and SAR of benzyl and phenoxymethylene oxadiazole benzenesulfonamides as selective beta3 adrenergic receptor agonist antiobesity agents.
Bioorganic & medicinal chemistry letters 2000;10(13):1431-4.
2000: D D Feng; Szalkowski Deborah; Mari Rios Candelore; Margaret A Cascieri; Lawrence F Colwell; L Deng; William P Feeney; Michael J Forrest; Gary J Hom; D Euan MacIntyre; Randall R Miller; Ralph A Stearns; Catherine D Strader; Laurie M Tota; Matthew J Wyvratt; Michael H Fisher; Ann E Weber
Discovery of an orally bioavailable alkyl oxadiazole beta3 adrenergic receptor agonist.
Bioorganic & medicinal chemistry letters 2000;10(13):1427-9.
1999: Mari Rios Candelore; L Deng; Laurie M Tota; Xiao-Ming Guan; A Amend; Y Liu; R Newbold; Margaret A Cascieri; Ann E Weber
Potent and selective human beta(3)-adrenergic receptor antagonists.
The Journal of pharmacology and experimental therapeutics 1999;290(2):649-55.
1999: Robert J Mathvink; A M Barritta; Mari Rios Candelore; Margaret A Cascieri; L Deng; Laurie M Tota; Catherine D Strader; Matthew J Wyvratt; Michael H Fisher; Ann E Weber
Potent, elective human beta3 adrenergic receptor agonists containing a substituted indoline-5-sulfonamide pharmacophore.
Bioorganic & medicinal chemistry letters 1999;9(13):1869-74.
1999: Thomas L Shih; Mari Rios Candelore; Margaret A Cascieri; Shuet-Hing Lee Chiu; Lawrence F Colwell; L Deng; William P Feeney; Michael J Forrest; Gary J Hom; D Euan MacIntyre; Randall R Miller; Ralph A Stearns; Catherine D Strader; Laurie M Tota; Matthew J Wyvratt; Michael H Fisher; Ann E Weber
L-770,644: a potent and selective human beta3 adrenergic receptor agonist with improved oral bioavailability.
Bioorganic & medicinal chemistry letters 1999;9(9):1251-4.
1999: Elizabeth M Naylor; Emma R Parmee; Vincent J Colandrea; L Perkins; Linda L Brockunier; Mari Rios Candelore; Margaret A Cascieri; Lawrence F Colwell; L Deng; William P Feeney; Michael J Forrest; Gary J Hom; D Euan MacIntyre; Catherine D Strader; Laurie M Tota; Pei-ran Wang; Matthew J Wyvratt; Michael H Fisher; Ann E Weber
Human beta3 adrenergic receptor agonists containing imidazolidinone and imidazolone benzenesulfonamides.
Bioorganic & medicinal chemistry letters 1999;9(5):755-8.
1999: Emma R Parmee; Elizabeth M Naylor; L Perkins; Vincent J Colandrea; Hyun O Ok; Mari Rios Candelore; Margaret A Cascieri; L Deng; William P Feeney; Michael J Forrest; Gary J Hom; D Euan MacIntyre; Randall R Miller; Ralph A Stearns; Catherine D Strader; Laurie M Tota; Matthew J Wyvratt; Michael H Fisher; Ann E Weber
Human beta3 adrenergic receptor agonists containing cyclic ureidobenzenesulfonamides.
Bioorganic & medicinal chemistry letters 1999;9(5):749-54.
1998: Linda J Kelly; Pasquale P Vicario; G Marie Thompson; Mari Rios Candelore; Thomas W Doebber; John Ventre; Margaret S Wu; Roger Meurer; Michael J Forrest; M W Conner; Margaret A Cascieri; David E Moller
Peroxisome proliferator-activated receptors gamma and alpha mediate in vivo regulation of uncoupling protein (UCP-1, UCP-2, UCP-3) gene expression.
Endocrinology 1998;139(12):4920-7.
1998: Elizabeth M Naylor; Vincent J Colandrea; Mari Rios Candelore; Margaret A Cascieri; Lawrence F Colwell; L Deng; William P Feeney; Michael J Forrest; Gary J Hom; D Euan MacIntyre; Catherine D Strader; Laurie M Tota; Pei-ran Wang; Matthew J Wyvratt; Michael H Fisher; Ann E Weber
3-Pyridylethanolamines: potent and selective human beta 3 adrenergic receptor agonists.
Bioorganic & medicinal chemistry letters 1998;8(21):3087-92.
1998: Daniel S Fletcher; Mari Rios Candelore; D Grujic; Bradford B Lowell; Silvi Luell; VS Susulic; D Euan MacIntyre
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.
The Journal of pharmacology and experimental therapeutics 1998;287(2):720-4.
1998: Ann E Weber; Hyun O Ok; Raul Alvaro; Mari Rios Candelore; Margaret A Cascieri; Shuet-Hing Lee Chiu; L Deng; Michael J Forrest; Gary J Hom; JE Hutchins; J Kao; D Euan MacIntyre; Robert J Mathvink; Debra McLoughlin; Randall R Miller; R C Newbold; Timothy V Olah; Emma R Parmee; L Perkins; Ralph A Stearns; Catherine D Strader; J Szumiloski; Yui S Tang; Laurie M Tota; Michael H Fisher
3-Pyridyloxypropanolamine agonists of the beta 3 adrenergic receptor with improved pharmacokinetic properties.
Bioorganic & medicinal chemistry letters 1998;8(16):2111-6.
1998: Michael H Fisher; A M Amend; TJ Bach; J M Barker; Edward J Brady; Mari Rios Candelore; D Carroll; Margaret A Cascieri; Shuet-Hing Lee Chiu; L Deng; Michael J Forrest; B Hegarty-Friscino; Xiao-Ming Guan; Gary J Hom; JE Hutchins; Linda J Kelly; Robert J Mathvink; Joseph M Metzger; Randall R Miller; Hyun O Ok; Emma R Parmee; Richard Saperstein; Catherine D Strader; Ralph A Stearns; D Euan MacIntyre
A selective human beta3 adrenergic receptor agonist increases metabolic rate in rhesus monkeys.
The Journal of clinical investigation 1998;101(11):2387-93.
1998: Emma R Parmee; Hyun O Ok; Mari Rios Candelore; Laurie M Tota; L Deng; Catherine D Strader; Matthew J Wyvratt; Michael H Fisher; Ann E Weber
Discovery of L-755,507: a subnanomolar human beta 3 adrenergic receptor agonist.
Bioorganic & medicinal chemistry letters 1998;8(9):1107-12.
1998: Ann E Weber; Robert J Mathvink; L Perkins; JE Hutchins; Mari Rios Candelore; Laurie M Tota; Catherine D Strader; Matthew J Wyvratt; Michael H Fisher
Potent, selective benzenesulfonamide agonists of the human beta 3 adrenergic receptor.
Bioorganic & medicinal chemistry letters 1998;8(9):1101-6.
1998: Pasquale P Vicario; Mari Rios Candelore; Marie-Therese Schaeffer; L Kelly; G Marie Thompson; Edward J Brady; Richard Saperstein; D Euan MacIntyre; Laurie M Tota; Margaret A Cascieri
Desensitization of beta3-adrenergic receptor-stimulated adenylyl cyclase activity and lipolysis in rats.
Life sciences 1998;62(7):627-38.
1997: Catherine D Strader; D Euan MacIntyre; Mari Rios Candelore; Eric M Parker
Molecular approaches to the discovery of new treatments for obesity.
Current opinion in chemical biology 1997;1(2):204-9.
1996: Mari Rios Candelore; L Deng; Laurie M Tota; Linda J Kelly; Margaret A Cascieri; Catherine D Strader
Pharmacological characterization of a recently described human beta 3-adrenergic receptor mutant.
Endocrinology 1996;137(6):2638-41.
1995: O Marko; Margaret A Cascieri; N Ayad; Catherine D Strader; Mari Rios Candelore
Isolation of a preadipocyte cell line from rat bone marrow and differentiation to adipocytes.
Endocrinology 1995;136(10):4582-8.
1991: Michael R Tota; Mari Rios Candelore; R A Dixon; Catherine D Strader
Biophysical and genetic analysis of the ligand-binding site of the beta-adrenoceptor.
Trends in pharmacological sciences 1991;12(1):4-6.
1990: Elaine Rands; Mari Rios Candelore; A H Cheung; W S Hill; Catherine D Strader; R A Dixon
Mutational analysis of beta-adrenergic receptor glycosylation.
The Journal of biological chemistry 1990;265(18):10759-64.
1989: Catherine D Strader; Mari Rios Candelore; W S Hill; R A Dixon; I S Sigal
A single amino acid substitution in the beta-adrenergic receptor promotes partial agonist activity from antagonists.
The Journal of biological chemistry 1989;264(28):16470-7.
1989: Catherine D Strader; Mari Rios Candelore; W S Hill; I S Sigal; R A Dixon
Identification of two serine residues involved in agonist activation of the beta-adrenergic receptor.
The Journal of biological chemistry 1989;264(23):13572-8.
1989: R A Dixon; W S Hill; Mari Rios Candelore; Elaine Rands; R E Diehl; M S Marshall; I S Sigal; Catherine D Strader
Genetic analysis of the molecular basis for beta-adrenergic receptor subtype specificity.
Proteins 1989;6(3):267-74.
1988: Catherine D Strader; I S Sigal; Mari Rios Candelore; Elaine Rands; W S Hill; R A Dixon
Conserved aspartic acid residues 79 and 113 of the beta-adrenergic receptor have different roles in receptor function.
The Journal of biological chemistry 1988;263(21):10267-71.
1987: Catherine D Strader; R A Dixon; A H Cheung; Mari Rios Candelore; A D Blake; I S Sigal
Mutations that uncouple the beta-adrenergic receptor from Gs and increase agonist affinity.
The Journal of biological chemistry 1987;262(34):16439-43.
1987: R A Dixon; I S Sigal; Mari Rios Candelore; R B Register; W Scattergood; Elaine Rands; Catherine D Strader
Structural features required for ligand binding to the beta-adrenergic receptor.
The EMBO journal 1987;6(11):3269-75.
1987: C D Strader; Mari Rios Candelore; Elaine Rands; R A Dixon
Beta-adrenergic receptor subtype is an intrinsic property of the receptor gene product.
Molecular pharmacology 1987;32(1):179-83.
1987: Catherine D Strader; I S Sigal; R B Register; Mari Rios Candelore; Elaine Rands; R A Dixon
Identification of residues required for ligand binding to the beta-adrenergic receptor.
Proceedings of the National Academy of Sciences of the United States of America 1987;84(13):4384-8.
1987: Catherine D Strader; I S Sigal; A D Blake; A H Cheung; R B Register; Elaine Rands; B A Zemcik; Mari Rios Candelore; R A Dixon
The carboxyl terminus of the hamster beta-adrenergic receptor expressed in mouse L cells is not required for receptor sequestration.
Cell 1987;49(6):855-63.
1987: R A Dixon; I S Sigal; Elaine Rands; R B Register; Mari Rios Candelore; A D Blake; Catherine D Strader
Ligand binding to the beta-adrenergic receptor involves its rhodopsin-like core.
Nature 1987;326(6108):73-7.