Zobrazeno 1 - 10
of 36
pro vyhledávání: '"Aaron D. Showalter"'
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-
Autor:
Hitoshi Yoshino, Takahiro Kawai, Dan Feng, Shunsuke Nagao, Francis S. Willard, Kyle W. Sloop, Tong Sun Kobilka, Aaron D. Showalter, Yoshiki Kawabe, David B. Wainscott, Brian A. Droz, Matthew P. Coghlan, Brian K. Kobilka, Masanori Fukazawa, Yoshiyuki Suzuki, Bingfa Sun
Publikováno v:
Proceedings of the National Academy of Sciences of the United States of America
Significance Glucagon-like peptide-1 receptor agonists have become established as a leading class of diabetes medications. However, these peptide-based drugs are administered by subcutaneous injection or, in one case, by a complex oral dosing regimen
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:
Lucy S Jun, Aaron D Showalter, Nosher Ali, Feihan Dai, Wenzhen Ma, Tamer Coskun, James V Ficorilli, Michael B Wheeler, M Dodson Michael, Kyle W Sloop
Publikováno v:
PLoS ONE, Vol 10, Iss 7, p e0132875 (2015)
Externí odkaz:
https://doaj.org/article/db5f11437f6b44edb5250bb08977bc68
Autor:
David B. Wainscott, Francis S. Willard, Fariba Norouziyan Cooper, James Ficorilli, Kyle W. Sloop, Jorge Alsina-Fernandez, William C. Roell, Tamer Coskun, Over Cabrera, Shweta Urva, Aaron D. Showalter, Libbey S. O’Farrell, Xiaoping Ruan, Hongchang Qu, Julie S. Moyers, Ajit Regmi, Lili Guo
Publikováno v:
Diabetes. 70
The ever-growing prevalence of obesity and its associated comorbidities (T2D, NASH/NAFLD) is driving the need to discover new therapies for improving metabolic health. Recently, multi-receptor agonists have offered promise for meeting this need. Here
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
Autor:
Graham M West, Francis S Willard, Kyle W Sloop, Aaron D Showalter, Bruce D Pascal, Patrick R Griffin
Publikováno v:
PLoS ONE, Vol 9, Iss 9, p e105683 (2014)
Activation of the glucagon-like peptide-1 receptor (GLP-1R) in pancreatic β-cells potentiates insulin production and is a current therapeutic target for the treatment of type 2 diabetes mellitus (T2DM). Like other class B G protein-coupled receptors
Externí odkaz:
https://doaj.org/article/041fff9bc52e4843b0f9ce5af37eab12
Autor:
Lucy S Jun, Aaron D Showalter, Nosher Ali, Feihan Dai, Wenzhen Ma, Tamer Coskun, James V Ficorilli, Michael B Wheeler, M Dodson Michael, Kyle W Sloop
Publikováno v:
PLoS ONE, Vol 9, Iss 4, p e93746 (2014)
Class B G protein-coupled receptors (GPCRs) are important regulators of endocrine physiology, and peptide-based therapeutics targeting some of these receptors have proven effective at treating disorders such as hypercalcemia, osteoporosis, and type 2
Externí odkaz:
https://doaj.org/article/578e71df589f4d7ab60826be5886a3bc