Zobrazeno 1 - 10
of 37
pro vyhledávání: '"Ana B. Bueno"'
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-
Autor:
Bingfa Sun, Francis S. Willard, Dan Feng, Jorge Alsina-Fernandez, Qi Chen, Michal Vieth, Joseph D. Ho, Aaron D. Showalter, Cynthia Stutsman, Liyun Ding, Todd M. Suter, James D. Dunbar, John W. Carpenter, Faiz Ahmad Mohammed, Eitaro Aihara, Robert A. Brown, Ana B. Bueno, Paul J. Emmerson, Julie S. Moyers, Tong Sun Kobilka, Matthew P. Coghlan, Brian K. Kobilka, Kyle W. Sloop
Publikováno v:
Proceedings of the National Academy of Sciences of the United States of America. 119(13)
Significance Tirzepatide is a dual agonist of the glucose-dependent insulinotropic polypeptide receptor (GIPR) and the glucagon-like peptide-1 receptor (GLP-1R), which are incretin receptors that regulate carbohydrate metabolism. This investigational
Autor:
Betty Chau, Joseph D. Ho, Francisco J Agejas, Francis S. Willard, Ana B. Bueno, Tong Sun Kobilka, Brian K. Kobilka, Isabel Rojo, James Ficorilli, Bingfa Sun, Aaron D. Showalter, Qi Chen, Cynthia Stutsman, Dan Feng, Kyle W. Sloop, Michal Vieth, Alma Jiménez, David B. Wainscott, Graham R Cumming
Publikováno v:
Nature Chemical Biology. 16:1105-1110
Drugs that promote the association of protein complexes are an emerging therapeutic strategy. We report discovery of a G protein-coupled receptor (GPCR) ligand that stabilizes an active state conformation by cooperatively binding both the receptor an
Autor:
Ana B, Bueno, Bingfa, Sun, Francis S, Willard, Dan, Feng, Joseph D, Ho, David B, Wainscott, Aaron D, Showalter, Michal, Vieth, Qi, Chen, Cynthia, Stutsman, Betty, Chau, James, Ficorilli, Francisco J, Agejas, Graham R, Cumming, Alma, Jiménez, Isabel, Rojo, Tong Sun, Kobilka, Brian K, Kobilka, Kyle W, Sloop
Publikováno v:
Nature chemical biology. 16(10)
Drugs that promote the association of protein complexes are an emerging therapeutic strategy. We report discovery of a G protein-coupled receptor (GPCR) ligand that stabilizes an active state conformation by cooperatively binding both the receptor an
Autor:
José Francisco Soriano, Javier Agejas, Rosario Gonzalez, Ramón Rodríguez, Timothy B. Durham, Howard Barff Broughton, Juan F. Espinosa, Paloma Vidal, Ana B. Bueno, Robert Dean Dally, Hsiu-Chiung Yang, Alicia Marcos, David E. Timm, Gema Sanz, James R. McCarthy, Patric James Hahn
Publikováno v:
Journal of Medicinal Chemistry. 60:9807-9820
NMR conformational analysis of a hydroxyethylamine peptide isostere developed as an aspartic protease inhibitor shows that it is a flexible architecture. Cyclization to form pyrrolidines, piperidines, or morpholines results in a preorganization of th
Autor:
Amy L. Cox, Eyas Raddad, Timothy M. Jones, Charles Reidy, Michaël Genin, John R. Stille, Chahrzad Montrose-Rafizadeh, Wayne P. Bocchinfuso, Laura F. Michael, Ellen A. Cannady, Manninen Peter Rudolph, M. Dodson Michael, Javier Agejas Francisco, Ana B. Bueno
Publikováno v:
Journal of Medicinal Chemistry. 58:9768-9772
The farnesoid X receptor (FXR) is a member of the "metabolic" subfamily of nuclear receptors. Several FXR agonists have been reported in the literature to have profound effects on plasma lipids in animal models. To discover novel and effective therap
Publikováno v:
Diabetes. 67(2)
Therapeutic engineering of glucagon-like peptide 1 (GLP-1) has enabled development of new medicines to treat type 2 diabetes. These injectable analogs achieve robust glycemic control by increasing concentrations of “GLP-1 equivalents” (∼50 pmol
Autor:
Carlos Montero, Lorna Hayhurst, Leslie Walton, Stephen N. Mitchell, Rosemarie Tomlinson, Louise Wallace, Graham Henry Timms, Jeremy Gilmore, Jeremy Findlay, Jane Cooper, John R. Boot, Richard J. Broadmore, Alicia Marcos, Ana B. Bueno
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:3344-3348
SAR around a known molecule with dual 5-HT(1D) antagonist and 5-HT(transporter) inhibitory activity has led to the discovery of molecules with improved dual activity and reduced cross-reactivity toward other aminergic receptors (5-HT(1B), alpha(1), a
Autor:
Robert E. Stratford, Ivan Collado, Maria Angeles Martinez-Grau, and Rebecca A. Wright, Joseph P. Tizzano, Anne H. Dantzig, Darryle D. Schoepp, M. Herin, Luisa M. Martín, Carmen M. Dominguez, Linda B. Tabas, Michael P. Clay, D. Scott Coffey, John T. Catlow, Carlos Montero, Alfonso de Dios, Ana B. Bueno, James A. Monn, Haiyan Jiang, Terry D. Lindstrom, Jose Alfredo Martin, Concepción Pedregal
Publikováno v:
Journal of Medicinal Chemistry. 48:5305-5320
(+)-2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (1), also known as LY354740, is a highly potent and selective agonist for group II metabotropic glutamate receptors (mGlu receptors 2 and 3) tested in clinical trials. It has been shown to block a
Autor:
Jon A. Erickson, Lianshen Zhang, Marian Mosior, Jose Alfredo Martin, Mccarthy James R, Sheila P. Little, Xiyun Chai, Jingdan Hu, Wayne David Kohn, Shu-Hui Chen, John P. Mayer, Ana B. Bueno, Patrick C. May, Mcclure Don B, Leonard N. Boggs, Hsiu-Chiung Yang, Wu-Kuang Yeh, Patricia Gonzalez-DeWhitt
Publikováno v:
Journal of Neurochemistry. 91:1249-1259
β-amyloid peptides (Aβ) are produced by a sequential cleavage of amyloid precursor protein (APP) by β- and γ-secretases. The lack of Aβ production in beta-APP cleaving enzyme (BACE1)–/– mice suggests that BACE1 is the principal β-secretase