Article
Pharmacology & Pharmacy
Maria Buur Nordskov Gabe, Laerke Smidt Gasbjerg, Sarina Gadgaard, Peter Lindquist, Jens Juul Holst, Mette Marie Rosenkilde
Summary: This study investigates the regulatory role of the GLP-2 system in the gut and bones by studying the effects of N-terminal truncations of human GLP-2 peptides on GLP-2 receptor activity and selectivity. The results show that the N-terminus of GLP-2 is crucial for GLP-2 receptor activity and selectivity. These findings provide a foundation for the development of tool compounds for further characterization of the GLP-2 system.
BRITISH JOURNAL OF PHARMACOLOGY
(2022)
Review
Endocrinology & Metabolism
Christophe E. M. De Block, Eveline Dirinck, Ann Verhaegen, Luc F. Van Gaal
Summary: Glucagon-like peptide-1 receptor agonists and dual GLP-1/glucose-dependent insulinotropic peptide RA tirzepatide have expanded the population of individuals reaching HbA1c and weight targets, showing potential therapeutic benefits. However, further research is needed to determine whether this will lead to improved cardiovascular outcomes and impact treatment guidelines.
DIABETES OBESITY & METABOLISM
(2022)
Article
Multidisciplinary Sciences
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
Summary: Tirzepatide is a dual incretin receptor agonist that improves glucose control and body weight regulation in type 2 diabetes mellitus. Mechanistic pharmacology studies combined with cryogenic electron microscopy have provided insights into the structural basis and interactions of Tirzepatide with GIPR and GLP-1R.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2022)
Review
Chemistry, Multidisciplinary
Yan Chen, Ying-na Xu, Chen-yu Ye, Wen-bo Feng, Qing-tong Zhou, De-hua Yang, Ming-wei Wang
Summary: NASH, a severe form of NAFLD, is characterized by liver steatosis, inflammation, hepatocellular injury, and fibrosis. Obesity and T2DM are major risk factors, with GLP-1R being a successful drug target for their treatment. GLP-1 mimetics have been proposed as potential therapeutic agents for NASH.
ACTA PHARMACOLOGICA SINICA
(2022)
Review
Pharmacology & Pharmacy
Fuxun Yang, Fan Zeng, Xiaoxiu Luo, Yu Lei, Jiajia Li, Sen Lu, Xiaobo Huang, Yunping Lan, Rongan Liu
Summary: GLP-1 receptor agonists can not only regulate blood glucose levels but also improve organ function, regulate immunity, and control inflammation in patients with sepsis. They have potential therapeutic benefits for sepsis patients with stress hyperglycemia.
FRONTIERS IN PHARMACOLOGY
(2021)
Review
Psychiatry
Daniel H. Cooper, Ranuk Ramachandra, Felicia Ceban, Joshua D. Di Vincenzo, Taeho Greg Rhee, Rodrigo B. Mansur, Kayla M. Teopiz, Hartej Gill, Roger Ho, Bing Cao, Leanna M. W. Lui, Muhammad Youshay Jawad, Juliet Arsenault, Gia Han Le, Diluk Ramachandra, Ziji Guo, Roger S. McIntyre
Summary: This study aimed to investigate whether GLP-1 receptor agonists can be used prophylactically to lower the risk of incident depression in patients with diabetes mellitus (DM). The results showed mixed findings regarding the effect of GLP-1 receptor agonists on lowering the risk of incident depression. Further research is needed to better understand the potential neuroprotective effects of GLP-1 receptor agonists on depression in patients with DM.
JOURNAL OF PSYCHIATRIC RESEARCH
(2023)
Article
Biochemistry & Molecular Biology
Hisayuki Katsuyama, Mariko Hakoshima, Shohei Umeyama, Sakura Iida, Hiroki Adachi, Hidekatsu Yanai
Summary: This study aimed to examine the real-world efficacy of GLP-1RA dulaglutide on metabolic parameters in Japanese patients with T2DM. The 12-month dulaglutide treatment reduced body weight by 1.7 kg and hemoglobin A1c by 1.1%. Significant improvements were also observed in serum HDL-C, TG, and non-HDL-C.
Review
Cell Biology
Karina A. Pena
Summary: The canonical model for GPCR activation assumes that activation occurs only at the cell surface and is turned off by receptor internalization. However, recent research has shown that some internalized GPCRs can continue to signal from endosomes, which has physiological implications.
AMERICAN JOURNAL OF PHYSIOLOGY-CELL PHYSIOLOGY
(2022)
Review
Biochemistry & Molecular Biology
Hwi Seung Kim, Chang Hee Jung
Summary: GLP-1 is a hormone secreted by the gastrointestinal tract that can stimulate insulin secretion, reduce hunger, and promote weight loss. Oral semaglutide, the first ingestible GLP-1RA, has shown efficacy in glycemic management, weight loss, and cardiovascular safety, making it a novel treatment option for patients with type 2 diabetes and/or obesity.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Endocrinology & Metabolism
Keiu Heinla, Eero Vasar, Ingrid Reppo, Tuuli Sedman, Vallo Volke
Summary: The study investigates the effect of GLP-1RAs on growth hormone (GH) secretion. Two separate clinical trials were conducted to examine the impact of short-acting and long-acting GLP-1RAs on GH levels. The findings suggest that GLP-1RAs may increase GH secretion, indicating a potential novel mechanism for regulating GH.
Article
Biochemistry & Molecular Biology
Jiaman Teng, Yuting Liu, Zhuanglin Shen, Weizhong Lv, Yantao Chen
Summary: This study investigated the interaction modes of GLP-1 with different polymer units through molecular simulations, revealing that different types of polymer units have varying effects on the stability and pharmacokinetic properties of GLP-1.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2021)
Article
Oncology
Nan Zhang, Peng Sun, Yuanyuan Xu, Haiyan Li, Huatao Liu, Ling Wang, Yue Cao, Kewen Zhou, Tinghuai Wang
Summary: GPER1, predicted to be a novel oestrogen receptor, negatively modulates the ER alpha signalling pathway by promoting its ubiquitin-proteasome-dependent degradation, inhibiting breast cancer cell proliferation and migration.
Article
Endocrinology & Metabolism
Rasmus Stenlid, Sara Y. Cerenius, Quan Wen, Banu Kucukemre Aydin, Hannes Manell, Azazul Chowdhury, Hjalti Kristinsson, Iris Ciba, Erik S. Gjessing, Katharina Moerwald, Julian Gomahr, Verena Heu, Daniel Weghuber, Anders Forslund, Peter Bergsten
Summary: Weekly injections of 2 mg exenatide extended release maintain endogenous total GLP-1 levels and lower circulating DPP-4 levels. This provides supportive evidence for the use of exenatide in the treatment of pediatric obesity.
FRONTIERS IN ENDOCRINOLOGY
(2023)
Article
Developmental Biology
Xin-Le Kang, Yan-Xue Li, Yan-Li Li, Jin-Xing Wang, Xiao-Fan Zhao
Summary: Animal steroid hormones can initiate signaling through G protein-coupled receptors. A newly discovered ecdysone-responsive GPCR, ErGPCR-3, plays a crucial role in the lepidopteran insect Helicoverpa armigera. Under 20E induction, ErGPCR-3 forms a homotetramer to facilitate 20E entry into cells, transmitting the 20E signal and promoting metamorphosis.
Article
Microbiology
Heetae Lee, Jinho An, Jiyeon Kim, Dohyun Choi, Youngcheon Song, Chong-Kil Lee, Hyunseok Kong, Sang Bum Kim, Kyungjae Kim
Summary: Knowledge of the impact of gut microbiota on human health has increased, and modulation of the bacterial community is now considered a therapeutic target for various diseases. This study found that Butyricimonas virosa has probiotic properties associated with improvement in obesity and related metabolic disorders. The administration of live or heat-killed B. virosa improved body weight, glucose levels, insulin resistance, and liver steatosis in obese mice.
FRONTIERS IN MICROBIOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Carla Gomez Santiago, Emanuele Paci, Dan Donnelly
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2018)
Article
Biochemistry & Molecular Biology
Amit Kumar, Mohanraj Gopalswamy, Clare Wishart, Mathias Henze, Lennart Eschen-Lippold, Dan Donnelly, Jochen Balbach
ACS CHEMICAL BIOLOGY
(2014)
Article
Biochemistry & Molecular Biology
Philip S. Miller, James Barwell, David R. Poyner, Mark J. Wigglesworth, Stephen L. Garland, Dan Donnelly
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2010)
Article
Pharmacology & Pharmacy
R. J. Mann, N. E. Nasr, J. K. Sinfield, E. Paci, D. Donnelly
BRITISH JOURNAL OF PHARMACOLOGY
(2010)
Review
Pharmacology & Pharmacy
Dan Donnelly
BRITISH JOURNAL OF PHARMACOLOGY
(2012)
Article
Endocrinology & Metabolism
R. E. Weaver, D. Donnelly, M. Wabitsch, P. J. Grant, A. J. Balmforth
INTERNATIONAL JOURNAL OF OBESITY
(2008)
Article
Biochemistry & Molecular Biology
Kathryn L. Chapman, Gemma K. Kinsella, Alan Cox, Dan Donnelly, John B. C. Findlay
JOURNAL OF MOLECULAR BIOLOGY
(2010)
Article
Biochemical Research Methods
S. Ravichandran, N. Singh, D. Donnelly, M. Migliore, P. Johnson, C. Fishwick, B. T. Luke, B. Martin, S. Maudsley, S. D. Fugmann, R. Moaddel
JOURNAL OF MOLECULAR GRAPHICS & MODELLING
(2014)
Article
Biochemistry & Molecular Biology
James Barwell, Philip S. Miller, Dan Donnelly, David R. Poyner
Article
Biochemistry & Molecular Biology
Rosalind J. Mann, Suleiman Al-Sabah, Rake Lopez de Maturana, John K. Sinfield, Dan Donnelly
Article
Biochemistry & Molecular Biology
Richard E. Weaver, Mark J. Wigglesworth, Dan Donnelly
Article
Multidisciplinary Sciences
Suleiman Al-Sabah, Munya Al-Fulaij, Ghina Shaaban, Hanadi A. Ahmed, Rosalind J. Mann, Dan Donnelly, Moritz Buenemann, Cornelius Krasel
Article
Pharmacology & Pharmacy
Richard E. Weaver, Juan C. Mobarec, Mark J. Wigglesworth, Christopher A. Reynolds, Dan Donnelly
BIOCHEMICAL PHARMACOLOGY
(2017)
Review
Pharmacology & Pharmacy
Chris de Graaf, Dan Donnelly, Denise Wootten, Jesper Lau, Patrick M. Sexton, Laurence J. Miller, Jung-Mo Ahn, Jiayu Liao, Madeleine M. Fletcher, Dehua Yang, Alastair J. H. Brown, Caihong Zhou, Jiejie Deng, Ming-Wei Wang
PHARMACOLOGICAL REVIEWS
(2016)