Insulin resistance and neurodegeneration: progress towards the development of new therapeutics for Alzheimer's disease

SM De la Monte - Drugs, 2017 - Springer
Alzheimer's disease (AD) should be regarded as a degenerative metabolic disease caused
by brain insulin resistance and deficiency, and overlapping with the molecular, biochemical …

Glucagon‐like peptide‐1 in diabetes care: Can glycaemic control be achieved without nausea and vomiting?

T Borner, IC Tinsley, RP Doyle… - British journal of …, 2022 - Wiley Online Library
Introduced less than two decades ago, glucagon‐like peptide‐1 receptor agonists rapidly
reshaped the field of Type 2 diabetes mellitus (T2DM) care by providing glycaemic control in …

Design and evaluation of peptide dual-agonists of GLP-1 and NPY2 receptors for glucoregulation and weight loss with mitigated nausea and emesis

BT Milliken, C Elfers, OG Chepurny… - Journal of medicinal …, 2021 - ACS Publications
There is a critical unmet need for therapeutics to treat the epidemic of comorbidities
associated with obesity and type 2 diabetes, ideally devoid of nausea/emesis. This study …

Corrination of a GLP-1 receptor agonist for glycemic control without emesis

T Borner, JL Workinger, IC Tinsley, SM Fortin, LM Stein… - Cell reports, 2020 - cell.com
Summary Glucagon-like peptide-1 receptor (GLP-1R) agonists used to treat type 2 diabetes
mellitus often produce nausea, vomiting, and in some patients, undesired anorexia. Notably …

A second‐generation glucagon‐like peptide‐1 receptor agonist mitigates vomiting and anorexia while retaining glucoregulatory potency in lean diabetic and emetic …

T Borner, ED Shaulson, IC Tinsley… - Diabetes, Obesity …, 2020 - Wiley Online Library
Aim To develop a conjugate of vitamin B12 bound to the glucagon‐like peptide‐1 receptor
(GLP‐1R) agonist exendin‐4 (Ex4) that shows reduced penetrance into the central nervous …

Separation of emetic and anorexic responses of exendin-4, a GLP-1 receptor agonist in Suncus murinus (house musk shrew)

SW Chan, G Lin, DTW Yew, CK Yeung, JA Rudd - Neuropharmacology, 2013 - Elsevier
The use of glucagon-like peptide-1 (7–36) amide (GLP-1) receptor agonists for the treatment
of type 2 diabetes mellitus is commonly associated with nausea and vomiting. Therefore, the …

The differential antiemetic properties of GLP-1 receptor antagonist, exendin (9–39) in Suncus murinus (house musk shrew)

SW Chan, Z Lu, G Lin, DTW Yew, CK Yeung… - Neuropharmacology, 2014 - Elsevier
The use of glucagon-like peptide-1 (7–36) amide (GLP-1) receptor agonists for the treatment
of type 2 diabetes mellitus is commonly associated with nausea and vomiting. Previous …

Differential hypoglycaemic, anorectic, autonomic and emetic effects of the glucagon-like peptide receptor agonist, exendin-4, in the conscious telemetered ferret

Z Lu, N Percie Du Sert, SW Chan, CK Yeung… - Journal of Translational …, 2014 - Springer
Background Rodents are incapable of emesis and consequently the emetic potential of
glucagon-like peptide-1 receptor (GLP-1R) agonists in studies designed to assess a …

Insights into the central pathways involved in the emetic and behavioural responses to exendin-4 in the ferret

Z Lu, CK Yeung, G Lin, DTW Yew, PLR Andrews… - Autonomic …, 2017 - Elsevier
Background GLP-1 receptor agonists are utilised for the treatment of Type-2 diabetes but
can be associated with undesirable effects of nausea and vomiting. Objectives To …

Synthesis, optimization, and biological evaluation of corrinated conjugates of the GLP-1R agonist exendin-4

IC Tinsley, T Borner, MKL Swanson… - Journal of Medicinal …, 2021 - ACS Publications
Corrination is the conjugation of a corrin ring containing molecule, such as vitamin B12
(B12) or B12 biosynthetic precursor dicyanocobinamide (Cbi), to small molecules, peptides …