Zobrazeno 1 - 10
of 18
pro vyhledávání: '"Guemalli R. Cardona"'
Autor:
Francis S. Willard, Jonathan D. Douros, Maria B.N. Gabe, Aaron D. Showalter, David B. Wainscott, Todd M. Suter, Megan E. Capozzi, Wijnand J.C. van der Velden, Cynthia Stutsman, Guemalli R. Cardona, Shweta Urva, Paul J. Emmerson, Jens J. Holst, David A. D’Alessio, Matthew P. Coghlan, Mette M. Rosenkilde, Jonathan E. Campbell, Kyle W. Sloop
Publikováno v:
JCI Insight, Vol 5, Iss 17 (2020)
Tirzepatide (LY3298176) is a dual GIP and GLP-1 receptor agonist under development for the treatment of type 2 diabetes mellitus (T2DM), obesity, and nonalcoholic steatohepatitis. Early phase trials in T2DM indicate that tirzepatide improves clinical
Externí odkaz:
https://doaj.org/article/03002ae150b14972b6d0c404574ecbbd
Autor:
Daniel A. Briere, David B. Wainscott, José Miguel Minguez, Cynthia Stutsman, Qi Chen, Ana B. Bueno, Alma Jiménez, Kyle W. Sloop, Ana I. Mateo, Guemalli R. Cardona, Wenzhen Ma, Aaron D. Showalter, Graham R Cumming, Ana M. Castaño, Francis S. Willard, Richard W. Zink, Javier Agejas, Nathan Yumibe, Christopher M Corkins
Publikováno v:
Journal of Medicinal Chemistry. 64:3439-3448
The identification of LSN3318839, a positive allosteric modulator of the glucagon-like peptide-1 receptor (GLP-1R), is described. LSN3318839 increases the potency and efficacy of the weak metabolite GLP-1(9-36)NH2 to become a full agonist at the GLP-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5f48ac2debed19ca46755aefd201e2e9
https://doi.org/10.1021/acs.jmedchem.1c00029
https://doi.org/10.1021/acs.jmedchem.1c00029
Autor:
Jorge Alsina-Fernandez, Francis S. Willard, Cynthia Stutsman, Kyle W. Sloop, Matthew P. Coghlan, Guemalli R. Cardona, Tamer Coskun, Aaron D. Showalter, Libbey S. O’Farrell, Over Cabrera, David B. Wainscott
Publikováno v:
Diabetes. 70
GIP receptor (GIPR) agonism enhances the reduction of food intake and weight loss induced by GLP-1 receptor (GLP-1R) agonism. Recently, GLP-1R agonists have been described that exhibit biased agonism as determined using cells engineered to facilitate
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::2d2735991689c2b26169e2d79c07ae66
https://doi.org/10.2337/db21-639-p
https://doi.org/10.2337/db21-639-p
Autor:
Steven D. Kahl, Kelly L. Wilbur, Warshawsky Alan M, Jayana Pankaj Lineswala, Siddaramaiah Cr, Pranab Maiti, Sweetana Stephanie Ann, Diseroad Benjamin Alan, Lisa A. Adams, Yanyun Chen, Richard W. Zink, Anne Reifel Miller, Grace L. Neathery, Anjana Patel Lewis, Over Cabrera, Alison N. Campbell, Guemalli R. Cardona, Nathan Yumibe, Keyue Chen, Keith A. Otto, Cecilia Bouaichi, Xiaosu Ma, Chafiq Hamdouchi, Amy C. DeBaillie, Chahrzad Montrose-Rafizadeh
Publikováno v:
Journal of medicinal chemistry. 61(3)
As a part of our program to identify potent GPR40 agonists capable of being dosed orally once daily in humans, we incorporated fused heterocycles into our recently disclosed spiropiperidine and tetrahydroquinoline acid derivatives 1, 2, and 3 with th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ba33126a14f55ea8f6b1d4d12011e1a1
https://pubmed.ncbi.nlm.nih.gov/29236497
https://pubmed.ncbi.nlm.nih.gov/29236497
Autor:
Anne Reifel Miller, Marialuisa C. Marcelo, Qi Chen, Ruth Belin, Pranab Maiti, Joseph V. Haas, Jared L. Piper, Ellen A. Cannady, Steven D. Kahl, Anjana Patel Lewis, Guemalli R. Cardona, Jason T. Johnson, D. Scott Coffey, Dawn A. Brooks, James Ficorilli, Xiaosu Ma, Sweetana Stephanie Ann, Chafiq Hamdouchi, Yanyun Chen, Edward J. Pratt, Keyue Chen, Richard W. Zink, Kelly L. Wilbur, Keith A. Otto, Mark A. Deeg, Nathan Yumibe, Jayana Pankaj Lineswala, Thomas E Eessalu, Chahrzad Montrose-Rafizadeh
Publikováno v:
Journal of medicinal chemistry. 59(24)
The G protein-coupled receptor 40 (GPR40) also known as free fatty acid receptor 1 (FFAR1) is highly expressed in pancreatic, islet β-cells and responds to endogenous fatty acids, resulting in amplification of insulin secretion only in the presence
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5e874164fca96fc6edd42ba967fc574b
https://pubmed.ncbi.nlm.nih.gov/27749056
https://pubmed.ncbi.nlm.nih.gov/27749056
Autor:
Stramm Lawrence E, Constance King, Debra L. Konkol, Thomas P. Burris, Chahrzad Montrose-Rafizadeh, Burkholder Timothy P, Harold E. Osborne, Brian Eugene Cunningham, Charles Reidy, Peter Ambrose Lander, Joshua Ryan Clayton, Robert M. Amos, Guemalli R. Cardona, Matthew L. Brown, Michael E. Christe, Michael James Genin, Robert Anthony Doti, Richard W. Zink, Gregory L. Durst
Publikováno v:
Bioorganicmedicinal chemistry letters. 25(7)
The design, synthesis, and structure activity relationships for a novel series of indoles as potent, selective, thyroid hormone receptor β (TRβ) agonists is described. Compounds with >50× binding selectivity for TRβ over TRα were generated and e
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::951a2935a45ecc576b4b6f4da15095f9
https://pubmed.ncbi.nlm.nih.gov/25752984
https://pubmed.ncbi.nlm.nih.gov/25752984
Autor:
Lewis E. Braverman, Peter H. K. Eng, William W. Chin, Michael C. Previti, Guemalli R. Cardona
Publikováno v:
European Journal of Endocrinology. :139-144
OBJECTIVE: The acute decrease in iodide organification in the thyroid in response to excess iodide is termed the acute Wolff-Chaikoff effect and normal organification resumes in spite of continued high plasma iodide concentrations (escape from the ac
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::22b595f9455ff2dc6bd42b12a14306ef
https://doi.org/10.1530/eje.0.1440139
https://doi.org/10.1530/eje.0.1440139
Publikováno v:
Proceedings of the National Academy of Sciences. 97:6212-6217
Nuclear hormone receptors activate gene transcription through ligand-dependent association with coactivators. Specific LXXLL sequence motifs present in these cofactors are sufficient to mediate these ligand-induced interactions. A thyroid hormone rec
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5212a0c5495d11d2925446f943a68dd7
https://doi.org/10.1073/pnas.97.11.6212
https://doi.org/10.1073/pnas.97.11.6212
Autor:
Moo-Il Kang, Lewis E. Braverman, John M. Quail, Guemalli R. Cardona, Daniel T. Baran, Moira Milne, William W. Chin
Publikováno v:
Journal of Cellular Biochemistry. 74:684-693
Thyroid hormones influence both bone formation and bone resorption. Clinical data and animal studies provide evidence of skeletal site heterogeneity (hip vs. spine) of bone responses to thyroid hormones. In vitro studies also demonstrate direct effec
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::28bcb9073fe6c17016fd51c3815d0f58
https://doi.org/10.1002/(sici)1097-4644(19990915)74:4<684::aid-jcb17>3.0.co
https://doi.org/10.1002/(sici)1097-4644(19990915)74:4<684::aid-jcb17>3.0.co
Autor:
Nancy Carrasco, Peter H. K. Eng, Michael C. Previti, Guemalli R. Cardona, Lewis E. Braverman, Sharon Alex, William W. Chin, Shih-Lieh Fang
Publikováno v:
Endocrinology. 140:3404-3410
In 1948, Wolff and Chaikoff reported that organic binding of iodide in the thyroid was decreased when plasma iodide levels were elevated (acute Wolff-Chaikoff effect), and that adaptation or escape from the acute effect occurred in approximately 2 da
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::90a75e0861db3e0fc0cb400b63bec3c9
https://doi.org/10.1210/endo.140.8.6893
https://doi.org/10.1210/endo.140.8.6893