Results 31 to 40 of about 39,275 (210)

The cardiovascular safety of incretin-based therapies: a review of the evidence [PDF]

, 2013
Cardiovascular disease (CVD) is a leading cause of morbidity and mortality in people with diabetes and therefore managing cardiovascular (CV) risk is a critical component of diabetes care. As incretin-based therapies are effective recent additions to the
Petrie, J.R.
core   +2 more sources

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

Novel skeletal effects of glucagon-like peptide-1 (GLP-1) receptor agonists [PDF]

, 2017
Type 2 diabetes mellitus (T2DM) leads to bone fragility and predisposes to increased risk of fracture, poor bone healing and other skeletal complications.
Chantal Chenu, Guillaume Mabilleau, Iepsen, Iepsen, Marie Pereira   +4 more
core   +5 more sources

The role of ECL2 in CGRP receptor activation: a combined modelling and experimental approach [PDF]

, 2013
The calcitonin gene-related peptide (CGRP) receptor is a complex of a calcitonin receptor-like receptor (CLR), which is a family B G-protein-coupled receptor (GPCR) and receptor activity modifying protein 1.
Alex C. Conner, Barwell J, Bruck Taddese, Christopher A. Reynolds, Conner AC, David R. Poyner, Debbie L. Hay, Harriet A. Watkins, James Barwell, Kevin J. Smith, Michael. J. Woolley, Urano D, Watkins HA, Z. Gamze Karakullukcu   +13 more
core   +2 more sources

Future Perspectives on GLP-1 Receptor Agonists and GLP-1/glucagon Receptor Co-agonists in the Treatment of NAFLD [PDF]

Frontiers in Endocrinology, 2018
Along the obesity pandemic, the prevalence of non-alcoholic fatty liver disease (NAFLD), often regarded as the hepatic manifestation of the metabolic syndrome, increases worldwide representing now the prevalent liver disease in western countries. No pharmacotherapy is approved for the treatment of NAFLD and, currently, the cornerstone treatment is ...
Marta Seghieri, Marta Seghieri, Alexander S. Christensen, Andreas Andersen, Anna Solini, Filip K. Knop, Filip K. Knop, Filip K. Knop, Tina Vilsbøll, Tina Vilsbøll   +9 more
openaire   +6 more sources

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

The effects of species ortholog and SNP variation on receptors for free fatty acids [PDF]

, 2013
Although it is widely assumed that species orthologs of hormone responsive G protein-coupled receptors will be activated by the same endogenously produced ligand(s), variation in potency, particularly in cases where more than one receptor responds to the
1000 Genomes Project Consortium, Bellahcene, Bergman, Bjursell, Blad, Brian D. Hudson, Briscoe, Brown, Burant, Christiansen, Christiansen, Christiansen, Christiansen, Cummings, Edfalk, Fredriksson, Galindo, Ge, Graeme Milligan, Hamid, Hannah Murdoch, Hirasawa, Hong, Hudson, Hudson, Hudson, Hudson, Humphries, Ichimura, Insel, Itoh, Kaku, Kalis, Kebede, Kebede, Kimura, Lan, Latour, Le Poul, Leonard, Liaw, Lin, Luo, Maslowski, Milligan, Milligan, Moore, Negoro, Ogawa, Oh, Ryan, Sawzdargo, Schmidt, Shimpukade, Sina, Smith, Smith, Steneberg, Stoddart, Stoddart, Strasser, Sum, Tan, Taneera, Tolhurst, Vettor, Watson, Wolever, Xiong, Xiong, Yashiro, Zaibi, Zhou   +72 more
core   +1 more source

G protein-coupled receptors not currently in the spotlight: free fatty acid receptor 2 and GPR35 [PDF]

, 2017
It is widely appreciated that G protein-coupled receptors have been the most successfully exploited class of targets for the development of small molecule medicines. Despite this, to date, less than 15% of the non-olfactory G protein-coupled receptors in
Milligan, Graeme
core   +1 more source

Activation of the GLP-1 receptor by a non-peptidic agonist [PDF]

Nature, 2020
Class B G-protein-coupled receptors are major targets for the treatment of chronic diseases, including diabetes and obesity1. Structures of active receptors reveal peptide agonists engage deep within the receptor core, leading to an outward movement of extracellular loop 3 and the tops of transmembrane helices 6 and 7, an inward movement of ...
Zhao, Peishen, Liang, Yi-Lynn, Belousoff, Matthew J, Deganutti, Giuseppe, Fletcher, Madeleine M, Willard, Francis S, Bell, Michael G, Christe, Michael E, Sloop, Kyle W, Inoue, Asuka, Truong, Tin T, Clydesdale, Lachlan, Furness, Sebastian GB, Christopoulos, Arthur, Wang, Ming-Wei, Miller, Laurence J, Reynolds, Christopher A, Danev, Radostin, Sexton, Patrick M, Wootten, Denise   +19 more
openaire   +4 more sources

Long‐term safety and efficacy of the sodium–glucose cotransporter 2 inhibitor, tofogliflozin, added on glucagon‐like peptide‐1 receptor agonist in Japanese patients with type 2 diabetes mellitus: A 52‐week open‐label, multicenter, post‐marketing clinical study

Journal of Diabetes Investigation, 2019
Aims/Introduction Tofogliflozin is a potent and highly selective sodium–glucose cotransporter 2 inhibitor that is currently used to treat patients with type 2 diabetes mellitus.
Yasuo Terauchi, Hisataka Fujiwara, Yuji Kurihara, Hideki Suganami, Masahiro Tamura, Masayuki Senda, Ryoji Gunji, Kohei Kaku   +7 more
doaj   +1 more source