Zobrazeno 1 - 10
of 1 585
pro vyhledávání: '"E. Malmstrom"'
Autor:
James eMoon, Brian eGodman, Max ePetzold, Samantha eAlvarez-Madrazo, Kathleen eBennett, Iain eBishop, Anna eBucsics, Ulrik eHesse, Andrew eMartin, Steven eSimoens, Corinne eZara, Rickard E Malmstrom
Publikováno v:
Frontiers in Pharmacology, Vol 5 (2014)
Introduction: There is an urgent need for health authorities across Europe to fully realise potential savings from increased use of generics to sustain their healthcare systems. A variety of strategies were used across Europe following the availabili
Externí odkaz:
https://doaj.org/article/e7e750d15b714811ba798b4b87e29e8b
Autor:
Mary Jane Cullen, Qian Xiang, Jeffrey A. Robl, Philip M. Sher, Brian J. Murphy, Keith J. Miller, Timothy M. Harper, Andrew Alt, Emily Luk, Sarah E. Malmstrom, Dean A. Wacker, Ginger Wu, Kimberly A. Foster, John M. Fevig, Joseph Carpenter, Robert L. Bertekap, Mary F. Grubb, Ying Wang, Karen A. Rossi, Gang Wu, Christian L. Morales, Jianxin Feng, Xiang Yang Ye, Anthony V. Azzara, Matthias Broekema
Publikováno v:
Journal of Medicinal Chemistry. 60:6166-6190
Agonism of the 5-HT2C receptor represents one of the most well-studied and clinically proven mechanisms for pharmacological weight reduction. Selectivity over the closely related 5-HT2A and 5-HT2B receptors is critical as their activation has been sh
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::9ab408370d6568ec38a8faeab8daced5
https://doi.org/10.1021/acs.jmedchem.7b00385
https://doi.org/10.1021/acs.jmedchem.7b00385
Autor:
Jean-François Lavallée, Yanou Yang, Carol A. Watson, Karen S. Hartl, Victor R. Guarino, Mark Gagnon, Timothy W. Harper, E. Scott Priestley, Jing Yang, Anne Marinier, Ruediger Edward H, Alain Martel, Dietmar A. Seiffert, Michel Bouvier, Ruth R. Wexler, Jacques Banville, Todd J. Friends, Roger Remillard, Michael M. Miller, Pancras C. Wong, Shana L. Posy, Ge Zhang, David G. Harden, Jonathan L. Josephs, Jon J. Hangeland, Harold R. O'Grady, R. Michael Lawrence, Sarah E. Malmstrom, Nick J. Allegretto, François Tremblay
Publikováno v:
Journal of medicinal chemistry. 62(16)
In an effort to identify novel antithrombotics, we have investigated protease-activated receptor 4 (PAR4) antagonism by developing and evaluating a tool compound, UDM-001651, in a monkey thrombosis model. Beginning with a high-throughput screening hi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cf314765253f0852affa327de9bc38c5
https://pubmed.ncbi.nlm.nih.gov/31246024
https://pubmed.ncbi.nlm.nih.gov/31246024
Autor:
Joseph, Carpenter, Ying, Wang, Gang, Wu, Jianxin, Feng, Xiang-Yang, Ye, Christian L, Morales, Matthias, Broekema, Karen A, Rossi, Keith J, Miller, Brian J, Murphy, Ginger, Wu, Sarah E, Malmstrom, Anthony V, Azzara, Philip M, Sher, John M, Fevig, Andrew, Alt, Robert L, Bertekap, Mary Jane, Cullen, Timothy M, Harper, Kimberly, Foster, Emily, Luk, Qian, Xiang, Mary F, Grubb, Jeffrey A, Robl, Dean A, Wacker
Publikováno v:
Journal of medicinal chemistry. 60(14)
Agonism of the 5-HT
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::b4aad16c8dfe5c23e1f667fa571a60d5
https://pubmed.ncbi.nlm.nih.gov/28635286
https://pubmed.ncbi.nlm.nih.gov/28635286
Autor:
Gerry Everlof, Chen-Pin Hung, Bradley A. Zinker, Ginger Wu, Steven C. Griffen, Stephanie Boehm, Hong Cai, Larisa Sereda, Li Xin, Matthias Broekema, Linda LaMarre, Sarah E. Malmstrom, Randolph P. Ponticiello, Cuixia Chu, Anjaneya Chimalakonda, Jeffrey A. Robl, Chiuwa Emily Luk, Michelle Lee, Steven O’Connor, Rachel Zebo, Keith J. Miller, Ying Wang, Richard L. Wong, John Krupinski, Zhenqiu Hong, Lisa Zhang, Jacob Zalaznick, Songping Han, Chunyu K. Wu, Yi-Xin Li, Karen A. Rossi, Dean A. Wacker
Publikováno v:
Journal of Medicinal Chemistry. 57:7499-7508
G-protein-coupled receptor 119 (GPR119) is expressed predominantly in pancreatic β-cells and in enteroendocrine cells in the gastrointestinal tract. GPR119 agonists have been shown to stimulate glucose-dependent insulin release by direct action in t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::debf907f70f44a75ff3d13d93c084a7d
https://doi.org/10.1021/jm501175v
https://doi.org/10.1021/jm501175v
Autor:
Keith J. Miller, Kenneth W. Rohrbach, Jianxin Feng, Mary Ann Pelleymounter, Sarah E. Malmstrom, Jinping Gan, Ge Zhang, Ginger Wu, Thao Ung, Chen-Pin Hung, William J. Keim, Karen A. Rossi, Jeffrey A. Robl, Qinling Qu, John M. Fevig, Mary Jane Cullen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:330-335
A series of 2,3,3a,4-tetrahydro-1H-pyrrolo[3,4-c]isoquinolin-5(9bH)-ones is described, several examples of which exhibit potent 5-HT(2C) agonism with excellent selectivity over the closely related 5-HT(2A) and 5-HT(2B) receptors. Compounds such as 38
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2079c57086a886d54141aa8d75f1c8e7
https://doi.org/10.1016/j.bmcl.2012.10.091
https://doi.org/10.1016/j.bmcl.2012.10.091
Autor:
Li Xin, Ming Lei, Claudio Mapelli, Tasir Shamsul Haque, Ge Zhang, John Krupinski, Sarah E. Malmstrom, Ving G. Lee, Douglas James Riexinger, Songping Han, William R. Ewing, Cooper Christopher B
Publikováno v:
Peptides. 31:950-955
We report the identification of potent agonists of the Glucagon-Like Peptide-1 Receptor (GLP-1R). These compounds are short, 11 amino acid peptides containing several unnatural amino acids, including (in particular) analogs of homohomophenylalanine (
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::22ba8ccad0d57dfbb86122717aef54d4
https://doi.org/10.1016/j.peptides.2010.01.008
https://doi.org/10.1016/j.peptides.2010.01.008
Autor:
Evan B. Janovitz, Mary Ann Pelleymounter, Mary F. Malley, Eva Zuvich, Jeffrey G. Varnes, Xueying Cao, Chen-Pin Hung, Karen A. Rossi, Mary Jane Cullen, Thao Ung, William J. Keim, Sarah E. Malmstrom, Michael Thomas, Keith J. Miller, Ginger Wu, Kenneth W. Rohrbach, Ge Zhang, Rangaraj Narayanan, Qinling Qu, Lois D. Lehman-McKeeman, Jeffrey A. Robl, James Devenny, Dean A. Wacker
Publikováno v:
Journal of Medicinal Chemistry. 50:1365-1379
Robust pharmaceutical treatment of obesity has been limited by the undesirable side-effect profile of currently marketed therapies. This paper describes the synthesis and optimization of a new class of pyrazinoisoindolone-containing, selective 5-HT2C
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::af9455a4be4dd87363342b50ad98d204
https://doi.org/10.1021/jm0612968
https://doi.org/10.1021/jm0612968
Autor:
Atsu Apedo, Xiang-Yang Ye, Christian L. Morales, John Krupinski, Mojgan Abousleiman, Dean A. Wacker, Karen A. Rossi, Keith J. Miller, Sarah E. Malmstrom, Ying Wang, Jeffrey A. Robl, Larisa Sereda
Publikováno v:
Bioorganicmedicinal chemistry letters. 24(11)
Through appropriate medicinal chemistry design tactics and computer-assisted conformational modeling, the initial lead A was evolved into a series of dihydrobenzofuran derivatives 3 as potent GPR119 agonists. This Letter describes the optimization of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e908958eea3a92e6e2fef557925c8511
https://pubmed.ncbi.nlm.nih.gov/24755425
https://pubmed.ncbi.nlm.nih.gov/24755425
Autor:
Jeffrey A. Robl, Mary Jane Cullen, Guohua Zhao, Mary Ann Pelleymounter, Ginger Wu, Thao Ung, Keith J. Miller, Chet Kwon, Xueying Cao, Chen-Pin Hung, Kenneth W. Rohrbach, Philip D. Stein, Sarah E. Malmstrom, Jinping Gan, Qinling Qu, William J. Keim, Karen A. Rossi, James Devenny, Ge Zhang, Sharon N. Bisaha
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(13)
The 5-HT2C receptor has been implicated as a critical regulator of appetite. Small molecule activation of the 5-HT2C receptor has been shown to affect food intake and regulate body weight gain in rodent models and more recently in human clinical tria
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b37d0ab47b2f6505a7e24bd04d9c9731
https://pubmed.ncbi.nlm.nih.gov/23683593
https://pubmed.ncbi.nlm.nih.gov/23683593