Zobrazeno 1 - 10
of 45
pro vyhledávání: '"Mari R. Candelore"'
Autor:
Stella H. Vincent, Corey Miller, Shiyao Sherrie Xu, Xiaodong Yang, Guoqiang Jiang, Guo Jian, Yusheng Xiong, Peggy E. McCann, Michael Wright, Jackie Shang, Bei B. Zhang, Mari R. Candelore, Qing Dallas-Yang, Sajjad A. Qureshi, Xinchun Tong, James R. Tata, Rui Liang, Emma R. Parmee, Laurie Tota
Publikováno v:
Journal of Medicinal Chemistry. 55:6137-6148
A potent, selective glucagon receptor antagonist 9m, N-[(4-{(1S)-1-[3-(3,5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine, was discovered by optimization of a previously identified lead. Compound 9m is
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5e9d307d9eb6cb46e7e1b8f9a96e2cec
https://doi.org/10.1021/jm300579z
https://doi.org/10.1021/jm300579z
Autor:
Richard Saperstein, Christopher Joseph Sinz, Victor D.-H. Ding, Zhen Lin, Ronald M. Kim, Jackie Shang, Bei Zhang, Michael Wright, Qing Dallas-Yang, Laurie Tota, Stella H. Vincent, Guoqiang Jiang, Gino Salituro, Bittner Amy R, Emma R. Parmee, Deborah Szalkowski, Shiyao Xu, James R. Tata, Mari R. Candelore, Sajjad A. Qureshi, Xiaodong Yang, Ed Brady
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:7124-7130
A novel class of N-aryl-2-acylindole human glucagon receptor (hGCGR) antagonists is reported. These compounds demonstrate good pharmacokinetic profiles in multiple preclinical species. One compound from this series, indole 33, is orally active in a t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::263e9e3d3e1ff6e13c1f10e3da912555
https://doi.org/10.1016/j.bmcl.2011.09.105
https://doi.org/10.1016/j.bmcl.2011.09.105
Autor:
Steve Mock, Guoquiang Jiang, Song Zheng, James R. Tata, Dong-Ming Shen, Kevin T. Chapman, Xiaodong Yang, Sajjad A. Qureshi, Xiaolan Shen, Edward J. Brady, Bei B. Zhang, Margaret E. McCann, Xinchun Tong, Emma R. Parmee, Mari R. Candelore, Laurie Tota, William P. Feeney, Victor D.-H. Ding, Michael Wright, Richard Saperstein, Qing Dallas-Yang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:76-81
A novel class of 1,3,5-pyrazoles has been discovered as potent human glucagon receptor antagonists. Notably, compound 26 is orally bioavailable in several preclinical species and shows selectivity towards cardiac ion channels, other family B receptor
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::598a01439adc406e046e5ad6d160d2f0
https://doi.org/10.1016/j.bmcl.2010.11.074
https://doi.org/10.1016/j.bmcl.2010.11.074
Autor:
Constantin Tamvakopolous, Rui Liang, Emma R. Parmee, Lauren Abrardo, Song Zheng, Bei B. Zhang, Sharon Tong, James R. Tata, Steve Mock, Michael Wright, Mari R. Candelore, Victor D.-H. Ding, Edward J. Brady, Richard Saperstein, Laurie Tota
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:587-592
A series of conformationally constrained tri-substituted ureas were synthesized, and their potential as glucagon receptor antagonists was evaluated. This effort resulted in the identification of compound 4a, which had a binding IC50 of 4.0 nM and was
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1fa30cbe651c82bd44e412b97a827a15
https://doi.org/10.1016/j.bmcl.2006.11.014
https://doi.org/10.1016/j.bmcl.2006.11.014
Autor:
Sajjad A. Qureshi, Don Hora, Joel P. Berger, Ron M. Kim, Emma R. Parmee, William P. Feeney, Marla L. Yates, Xiaodong Yang, Bei B. Zhang, Mari R. Candelore
Publikováno v:
European Journal of Pharmacology. 555:8-16
Glucose homeostasis is maintained by the combined actions of insulin and glucagon. Hyperglucagonemia and/or elevation of glucagon/insulin ratio have been reported in diabetic patients and in animal models of diabetes. Therefore, antagonizing glucagon
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c827ada2b479ba9155801ca83ce303db
https://doi.org/10.1016/j.ejphar.2006.10.033
https://doi.org/10.1016/j.ejphar.2006.10.033
Autor:
Victor D.-H. Ding, Gregory J. Kaczorowski, Michael Wright, Sheila M. Cohen, Emma R. Parmee, Jeffrey G. Werrmann, Corin O. Miller, Brian A. Kirk, Laurie Tota, Mari R. Candelore, Bei B. Zhang, Joseph L. Duffy, James R. Tata
Publikováno v:
Bioorganic & Medicinal Chemistry. 14:1506-1517
The demonstration of pharmacodynamic efficacy of novel chemical entities represents a formidable challenge in the early exploration of synthetic lead classes. Here, we demonstrate a technique to validate the biological efficacy of novel antagonists o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7ad8dd0dd3883a9ac8c23c3df50963e1
https://doi.org/10.1016/j.bmc.2005.10.008
https://doi.org/10.1016/j.bmc.2005.10.008
Autor:
Rui Liang, Lauri M. Tota, Kevin T. Chapman, Joseph L. Duffy, Xiaodong Yang, Frank Xiaoqing Liu, Guoqiang Jiang, Edward J. Brady, Brian A. Kirk, Song Zheng, Zenon Konteatis, James R. Tata, Mari R. Candelore, Deborah Szalkowski, Sharon Tong, Bei B. Zhang, Victor D.-H. Ding, Elizabeth Louise Campbell, Richard Saperstein, Sajjad A. Qureshi, Dan Xie, Peter Zafian
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:1401-1405
A novel class of antagonists of the human glucagon receptor (hGCGR) has been discovered. Systematic modification of the lead compound identified substituents that were essential for activity and those that were amenable to further optimization. This
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::02875fe32941a428c96a4c4eb4d22e48
https://doi.org/10.1016/j.bmcl.2005.01.003
https://doi.org/10.1016/j.bmcl.2005.01.003
Autor:
Kevin T. Chapman, Corin O. Miller, Guoqiang Jiang, Victor D.-H. Ding, Joseph L. Duffy, Ed Brady, Sheila M. Cohen, Xiaodong Yang, Richard Saperstein, Mari R. Candelore, Sajjad A. Qureshi, Zhihua Li, James R. Tata, Dan Xie, Laurie Tota, Alka Bansal, David E. Moller, Bei B. Zhang
Publikováno v:
Diabetes. 53:3267-3273
Glucagon maintains glucose homeostasis during the fasting state by promoting hepatic gluconeogenesis and glycogenolysis. Hyperglucagonemia and/or an elevated glucagon-to-insulin ratio have been reported in diabetic patients and animals. Antagonizing
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4f2904b3cc0b8f7628ee293dc5b39057
https://doi.org/10.2337/diabetes.53.12.3267
https://doi.org/10.2337/diabetes.53.12.3267
Autor:
Laurie Tota, Suzanne M. Mandala, Gan-Ju Shei, Michael Wright, James D. Bergstrom, Mari R. Candelore, James A. Milligan
Publikováno v:
Biochemical and Biophysical Research Communications. 297:600-606
It has been reported recently that the phosphorylated form of the immunomodulator FTY720 activates sphingosine 1-phosphate G protein-coupled receptors [1] , [2] . Therefore, understanding the biology of this new class of receptors will be important i
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b88fcd7e895e1aafe7914cb607b0c5c3
https://doi.org/10.1016/s0006-291x(02)02237-4
https://doi.org/10.1016/s0006-291x(02)02237-4
Autor:
Linda Brockunier, Ann E. Weber, Suresh B. Singh, Michael H. Fisher, Mari R. Candelore, Yong Liu, Liping Deng, Laurie Tota, Margaret A. Cascieri, Jiafang He, Emma R. Parmee, Matthew J. Wyvratt
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 10:2283-2286
Tetrahydroisoquinoline derivatives containing a 4-(hexylureido)benzenesulfonamide were examined as human beta3 adrenergic receptor (AR) agonists. Notably, 4,4-biphenyl derivative 9 was a 6 nM full agonist of the beta3 AR. Naphthyloxy compound 18 (bet
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::119757ed837facb02b3edd1a23f52f0c
https://doi.org/10.1016/s0960-894x(00)00459-5
https://doi.org/10.1016/s0960-894x(00)00459-5