Review
Endocrinology & Metabolism
David C. D. Hope, Matthew L. Vincent, Tricia M. M. Tan
Summary: Obesity and Type 2 diabetes are global health challenges, with potential treatment options such as co-agonists showing promise in improving efficacy and reducing adverse effects. Further research is needed to guide the safe, effective, and personalized use of GLP-1/glucagon co-agonists in targeting weight loss and metabolic disease in the future.
FRONTIERS IN ENDOCRINOLOGY
(2021)
Article
Endocrinology & Metabolism
Neil Tanday, Andrew English, Ryan A. Lafferty, Peter R. Flatt, Nigel Irwin
Summary: The combined activation of GLP-1 and CCK1 receptors through [Lys(12)Pal]Ex-4/CCK showed enhanced beneficial effects on pancreatic beta-cells, leading to improved insulin secretion and glucose homeostasis in vitro and in mice models. This hybrid peptide therapy also resulted in reductions in energy intake and body weight, as well as improvements in glucose tolerance, insulin responsiveness, and pancreatic islet morphology, highlighting its potential for treating obesity-related diabetes.
FRONTIERS IN ENDOCRINOLOGY
(2021)
Article
Pharmacology & Pharmacy
Anna Thorso Larsen, Morten A. Karsdal, Kim Henriksen
Summary: Long-acting dual amylin and calcitonin receptor agonists (DACRAs) have potential as treatments for obesity. Switching or combining treatment with KBP-336 and semaglutide improves weight loss and glucose tolerance in obese rats.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2023)
Review
Cardiac & Cardiovascular Systems
Erin D. Michos, Francisco Lopez-Jimenez, Martha Gulati
Summary: Obesity remains a major public health problem in the United States, with almost half of adults affected. Weight loss is now recommended as a key strategy for the primary prevention of cardiovascular disease (CVD) in overweight or obese patients. Recent studies have shown the efficacy of some pharmacologic therapies for chronic weight management, which may encourage healthcare professionals to recognize obesity as a treatable chronic disease. This review article focuses on the benefits and challenges of lifestyle changes, bariatric surgery, and pharmacologic interventions in the treatment of obesity, particularly glucagon-like peptide-1 receptor agonist medications for managing obesity and reducing CVD risk.
JOURNAL OF THE AMERICAN HEART ASSOCIATION
(2023)
Review
Endocrinology & Metabolism
Isabella Zaffina, Maria Chiara Pelle, Giuseppe Armentaro, Federica Giofre, Velia Cassano, Angela Sciacqua, Franco Arturi
Summary: Obesity is a growing problem worldwide, especially in industrialized countries. Current drugs for treating obesity have limited efficacy, thus new anti-obesity treatments are needed. Tirzepatide, a drug that coactivates the GIP receptor and GLP-1 receptor, has been developed to improve glycemic control and reduce body weight. It offers more effective treatment of diabetes and obesity with fewer side effects compared to selective GLP-1 receptor agonists.
FRONTIERS IN ENDOCRINOLOGY
(2023)
Article
Neurosciences
Laura N. Deden, Jan Booij, Joanes Grandjean, Judith R. Homberg, Eric J. Hazebroek, Martin Gotthardt, Marti Boss
Summary: Stimulation of GLP-1 receptors increases insulin release and induces satiety. GLP-1 receptor agonists may have potential benefits for Parkinson's and Alzheimer's diseases, but Ga-68-NODAGA-exendin-4 PET cannot be used to analyze GLP-1 receptors in the brain of obese subjects.
Article
Chemistry, Medicinal
Ariana M. Chao, Jena Shaw Tronieri, Anastassia Amaro, Thomas A. Wadden
Summary: Losing 5-10% or more of initial body weight can improve obesity-related comorbidities, but achieving and maintaining this weight loss level is challenging. The novel anti-obesity medication semaglutide, when used as an adjunct to a reduced-calorie diet and physical activity, helps patients achieve average weight losses of 9.6-17.4% of initial body weight at week 68 and improves cardiometabolic and psychosocial indices. Factors to consider for the selection and use of this medication include efficacy, safety, contraindications, adverse effects, comorbidity management, drug interactions, insurance coverage and cost, and patient preferences.
DRUG DESIGN DEVELOPMENT AND THERAPY
(2022)
Review
Endocrinology & Metabolism
Nitya Kumar, David A. D'Alessio
Summary: Recent clinical trials have shown that GLP-1 receptor agonists are effective and well-tolerated agents for weight loss. Originally developed for glucose control in type 2 diabetes, research over the past 30 years has demonstrated that GLP-1 receptor agonists also reduce food intake by acting in the central nervous system.
JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM
(2022)
Article
Medicine, Research & Experimental
Shimpei Iikuni, Ichiro Kamei, Takaki Ohara, Hiroyuki Watanabe, Masahiro Ono
Summary: A GLP-1R imaging probe [In-111]In-E4DA1 has been developed, which can detect the location of insulinomas in vivo and has reduced renal accumulation.
MOLECULAR PHARMACEUTICS
(2022)
Review
Cardiac & Cardiovascular Systems
Muhammad Shariq Usman, Melanie Davies, Michael E. Hall, Subodh Verma, Stefan D. Anker, Julio Rosenstock, Javed Butler
Summary: This study investigates the cardiovascular effects of weight-loss interventions and provides practical guidance for cardiologists in developing and implementing treatment plans.
EUROPEAN HEART JOURNAL
(2023)
Article
Medicine, Research & Experimental
Shimpei Iikuni, Takaki Ohara, Hiroyuki Watanabe, Masahiro Ono
Summary: In this study, 111In-labeled exendin-4 derivatives with specific albumin binder (ALB) moieties were designed and synthesized for noninvasive detection of insulinomas. Through in vitro and in vivo experiments, it was determined that these derivatives exhibited good affinity and tumor accumulation, while showing lower renal accumulation. These results provide important guidance for the design of novel radioligands targeting GLP-1R.
MOLECULAR PHARMACEUTICS
(2022)
Article
Medicine, General & Internal
Dandan Mao, Huanyi Cao, Mai Shi, Chi Chiu Wang, Joseph Kwong, Joshua Jing Xi Li, Yong Hou, Xing Ming, Heung Man Lee, Xiao Yu Tian, Chun Kwok Wong, Elaine Chow, Alice Pik Shan Kong, Vivian Wai Yan Lui, Paul Kay Sheung Chan, Juliana Chung Ngor Chan
Summary: Our study revealed that the expression of PSMA2 and GLP-1R was increased and positively correlated in T2D-related cervical cancer specimens, suggesting hyperglycemia might promote cancer growth by increasing PSMA2 expression, which could be attenuated by Exendin-4.
Article
Endocrinology & Metabolism
Mikhail N. Kosiborod, Meena Bhatta, Melanie Davies, John E. Deanfield, W. Timothy Garvey, Usman Khalid, Robert Kushner, Domenica M. Rubino, Niels Zeuthen, Subodh Verma
Summary: This study evaluated the effects of once-weekly subcutaneous semaglutide 2.4 mg on cardiometabolic risk factors in people with overweight/obesity without diabetes. The results showed that semaglutide can improve waist circumference, blood pressure, blood glucose, and lipid levels, and reduce the use of antihypertensive and lipid-lowering medications. However, these benefits were not maintained after treatment discontinuation.
DIABETES OBESITY & METABOLISM
(2023)
Review
Biology
Fatma Haddad, Ghadeer Dokmak, Maryam Bader, Rafik Karaman
Summary: Obesity is a complex metabolic condition that can be detrimental to health and result in mortality. There are various methods to manage obesity, such as lifestyle changes, medications, and bariatric surgery. Liraglutide and semaglutide are FDA-approved anti-obesity drugs used in the treatment of type 2 diabetes mellitus (T2DM). Through analysis of clinical studies, it has been found that some antihyperglycemic medications can aid in weight loss, with GLP-1 agonists showing the most promise.
Article
Neurosciences
Zhiyi Xie, Budbazar Enkhjargal, Matei Nathanael, Lingyun Wu, Qiquan Zhu, Tongyu Zhang, Jiping Tang, John H. Zhang
Summary: The study suggests that Ex-4 may protect BBB integrity after SAH in rats through GLP-1R/AMPK-dependent NF-kappa B/MMP-9 inhibition.
FRONTIERS IN MOLECULAR NEUROSCIENCE
(2021)
Article
Physiology
Zhi Yi Ong, Amber L. Alhadeff, Harvey J. Grill
AMERICAN JOURNAL OF PHYSIOLOGY-REGULATORY INTEGRATIVE AND COMPARATIVE PHYSIOLOGY
(2015)
Review
Biochemistry & Molecular Biology
Jessica Rose Gugusheff, Zhi Yi Ong, Beverly Sara Muhlhausler
Article
Biochemistry & Molecular Biology
M. A. Vithayathil, J. R. Gugusheff, R. A. Gibson, Z. Y. Ong, B. S. Muhlhausler
PROSTAGLANDINS LEUKOTRIENES AND ESSENTIAL FATTY ACIDS
(2016)
Article
Endocrinology & Metabolism
Zhi Yi Ong, Diana M. Bongiorno, Mary Ann Hernando, Harvey J. Grill
Article
Neurosciences
Zhi Yi Ong, Jing-Jing Liu, Zhiping P. Pang, Harvey J. Grill
NEUROPSYCHOPHARMACOLOGY
(2017)
Article
Nutrition & Dietetics
M. A. Vithayathil, J. R. Gugusheff, Z. Y. Ong, S. C. Langley-Evans, R. A. Gibson, B. S. Muhlhausler
NUTRITION & METABOLISM
(2018)
Article
Psychology, Biological
J. R. Gugusheff, Z. Y. Ong, B. S. Mullhausler
PHYSIOLOGY & BEHAVIOR
(2014)
Editorial Material
Neurosciences
Zhi Yi Ong
JOURNAL OF PHYSIOLOGY-LONDON
(2019)
Article
Neurosciences
Amber L. Alhadeff, Sineadh M. Conway, Zhi Yi Ong, Hallie S. Wald, Mitchell F. Roitman, Harvey J. Grill
Review
Neurosciences
Zhi Yi Ong, Gavan P. McNally
Article
Substance Abuse
Tiarani N. Dixon, Gavan P. McNally, Zhi Yi Ong
ALCOHOLISM-CLINICAL AND EXPERIMENTAL RESEARCH
(2020)
Article
Physiology
Hallie S. Wald, Ananya Chandra, Anita Kalluri, Zhi Yi Ong, Matthew R. Hayes, Harvey J. Grill
AMERICAN JOURNAL OF PHYSIOLOGY-REGULATORY INTEGRATIVE AND COMPARATIVE PHYSIOLOGY
(2020)
Review
Biochemistry & Molecular Biology
Ruth Naomi, Hasnah Bahari, Zhi Yi Ong, Yong Yoke Keong, Hashim Embong, Retnagowri Rajandram, Soo Huat Teoh, Fezah Othman, Rosnani Hasham, Khoo Boon Yin, Priyatharisni Kaniappan, Muhammad Dain Yazid, Zainul Amiruddin Zakaria
Summary: This article provides an overview of the medicinal chemistry and pharmacology of Andrographis paniculata and its active compounds in terms of anti-cancer activity, primary mechanism of action, and cellular targets, particularly in the lipid-dependent cancer pathway.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Neurosciences
Stephanie Murphy, Metika Collis Glynn, Tiarani N. Dixon, Harvey J. Grill, Gavan P. McNally, Zhi Yi Ong
Summary: The NTS A2 neurons play a significant role in controlling food intake, suppressing consumption without affecting food approach, anxiety-like behaviors, or locomotor activity. Their projections to the PVH, rather than the BNST, mediate this control.
NEUROPSYCHOPHARMACOLOGY
(2023)