Results 31 to 40 of about 38,022 (310)

Exendin-4 Upregulates Adiponectin Level in Adipocytes via Sirt1/Foxo-1 Signaling Pathway. [PDF]

PLoS ONE, 2017
Glucagon-like peptide-1 (GLP-1) receptor plays an essential role in regulating glucose metabolism. GLP-1 receptor agonists have been widely used for treating diabetes and other insulin resistance-related diseases.
Anping Wang, Ting Li, Ping An, Wenhua Yan, Hua Zheng, Baoan Wang, Yiming Mu   +6 more
doaj   +1 more source

GIPR antagonist antibodies conjugated to GLP-1 peptide are bispecific molecules that decrease weight in obese mice and monkeys

Cell Reports Medicine, 2021
Summary: Glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) regulate glucose and energy homeostasis. Targeting both pathways with GIP receptor (GIPR) antagonist antibody (GIPR-Ab) and GLP-1 receptor (GLP-1R) agonist ...
Shu-Chen Lu, Michelle Chen, Larissa Atangan, Elizabeth A. Killion, Renee Komorowski, Yuan Cheng, Chawita Netirojjanakul, James R. Falsey, Marina Stolina, Denise Dwyer, Clarence Hale, Shanaka Stanislaus, Todd Hager, Veena A. Thomas, John M. Harrold, David J. Lloyd, Murielle M. Véniant   +16 more
doaj   +1 more source

Distinct Regions in the C-Terminus Required for GLP-1R Cell Surface Expression, Activity and Internalisation [PDF]

, 2015
The glucagon-like peptide-1 (GLP-1) receptor (GLP-1R), an important drug target in the treatment of type 2 diabetes, is a G-protein coupled receptor (GPCR) that mediates insulin secretion by GLP-1.
Venkat Kanamarlapudi
core   +1 more source

In Vivo Imaging of Transplanted Islets with ^(64)Cu-DO3A-VS-Cys^(40)-Exendin-4 by Targeting GLP-1 Receptor [PDF]

, 2011
Glucagon-like peptide 1 receptor (GLP-1R) is highly expressed in pancreatic islets, especially on β-cells. Therefore, a properly labeled ligand that binds to GLP-1R could be used for in vivo pancreatic islet imaging.
Bading, James R., Colcher, David, Conti, Peter E., Fraser, Scott E., Ishiyama, Kohei, Kandeel, Fouad, Li, Lin, Li, Zibo, Nair, Indu, Shively, John E., Todorov, Ivan, Wu, Zhanhong   +11 more
core   +2 more sources

Bumps and humps in the success of Tirzepatide as the first GLP1 and GIP receptor agonist

Health Sciences Review, 2022
Glucagon-like peptide 1 (GLP-1) receptor agonists have acquired importance in Type 2 diabetes (T2D) treatment due to their glycemic advantages, cardiorenal effects, and favorable body weight. Despite this, the continuous discovery of higher effectiveness
Rouchan Ali, Sharma Arvind Virendra, Pooja A Chawla   +2 more
doaj   +1 more source

Type 2 Diabetes Mellitus and Glucagon Like Peptide-1 Receptor Signalling [PDF]

, 2013
It has been estimated that approximately 8.4% of the world population currently live with diabetes mellitus and type 2 diabetes is the most common form. Type 2 diabetes increases the risk of complications such as heart attacks, blindness, amputations and
Venkat Kanamarlapudi
core   +1 more source

Tirzepatide is an imbalanced and biased dual GIP and GLP-1 receptor agonist

JCI Insight, 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.
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   +17 more
doaj   +1 more source

BI 456906: Discovery and preclinical pharmacology of a novel GCGR/GLP-1R dual agonist with robust anti-obesity efficacy

Molecular Metabolism, 2022
Objective: Obesity and its associated comorbidities represent a global health challenge with a need for well-tolerated, effective, and mechanistically diverse pharmaceutical interventions.
Tina Zimmermann, Leo Thomas, Tamara Baader-Pagler, Peter Haebel, Eric Simon, Wolfgang Reindl, Besnik Bajrami, Wolfgang Rist, Ingo Uphues, Daniel J. Drucker, Holger Klein, Rakesh Santhanam, Dieter Hamprecht, Heike Neubauer, Robert Augustin   +14 more
doaj   +1 more source

The pharmacology and function of receptors for short-chain fatty acids [PDF]

, 2015
Despite some blockbuster G protein–coupled receptor (GPCR) drugs, only a small fraction (∼15%) of the more than 390 nonodorant GPCRs have been successfully targeted by the pharmaceutical industry.
Bolognini, Daniele, Milligan, Graeme, Moss, Catherine E., Tobin, Andrew B.   +3 more
core   +1 more source

Insulin–glucagon‐like peptide‐1 receptor agonist relay and glucagon‐like peptide‐1 receptor agonist first regimens in individuals with type 2 diabetes: A randomized, open‐label trial study

Journal of Diabetes Investigation, 2022
Aims/Introduction Glucagon‐like peptide‐1 receptor agonists (GLP‐1 RA) might be less effective in patients with severe hyperglycemia, because hyperglycemia downregulated the GLP‐1 receptor in an animal study.
Yumie Takeshita, Yuki Kita, Takeo Tanaka, Hisanori Goto, Yujiro Nakano, Chisato Teramura, Yasufumi Enyama, Toshinari Takamura, the Establishment of Rationale for Antiaging Diabetic Medicine (ERA‐DM) Study Group   +8 more
doaj   +1 more source