GIPR/GLP-1R dual agonist therapies for diabetes and weight loss—chemistry, physiology, and clinical applications
The incretin system is an essential metabolic axis that regulates postprandial metabolism.
The two incretin peptides that enable this effect are the glucose-dependent insulinotropic …
The two incretin peptides that enable this effect are the glucose-dependent insulinotropic …
Incretin hormones and type 2 diabetes
abstract Incretin hormones (glucose-dependent insulinotropic polypeptide [GIP] and
glucagon-like peptide-1 [GLP-1]) play a role in the pathophysiology of type 2 diabetes. Along …
glucagon-like peptide-1 [GLP-1]) play a role in the pathophysiology of type 2 diabetes. Along …
Structural insights into multiplexed pharmacological actions of tirzepatide and peptide 20 at the GIP, GLP-1 or glucagon receptors
Glucose homeostasis, regulated by glucose-dependent insulinotropic polypeptide (GIP),
glucagon-like peptide-1 (GLP-1) and glucagon (GCG) is critical to human health. Several …
glucagon-like peptide-1 (GLP-1) and glucagon (GCG) is critical to human health. Several …
Recent advances in incretin-based pharmacotherapies for the treatment of obesity and diabetes
The incretin hormone glucagon-like peptide-1 (GLP-1) has received enormous attention
during the past three decades as a therapeutic target for the treatment of obesity and type 2 …
during the past three decades as a therapeutic target for the treatment of obesity and type 2 …
[HTML][HTML] GLP-1 and GIP receptor signaling in beta cells–a review of receptor interactions and co-stimulation
Glucagon-like peptide 1 receptor (GLP-1R) and glucose-dependent insulinotropic
polypeptide receptor (GIPR) are two class B1 G protein-coupled receptors, which are …
polypeptide receptor (GIPR) are two class B1 G protein-coupled receptors, which are …
Brain uptake pharmacokinetics of albiglutide, dulaglutide, tirzepatide, and DA5-CH in the search for new treatments of Alzheimer's and Parkinson's diseases
EM Rhea, A Babin, P Thomas, M Omer, R Weaver… - Tissue …, 2024 - Taylor & Francis
Background A number of peptide incretin receptor agonists (IRAs) show promise as
therapeutics for Alzheimer's disease (AD) and Parkinson's disease (PD). Transport across …
therapeutics for Alzheimer's disease (AD) and Parkinson's disease (PD). Transport across …
Tirzepatide: A systematic update
I Forzano, F Varzideh, R Avvisato… - International Journal of …, 2022 - mdpi.com
Tirzepatide is a new molecule capable of controlling glucose blood levels by combining the
dual agonism of Glucose-Dependent Insulinotropic Polypeptide (GIP) and Glucagon-Like …
dual agonism of Glucose-Dependent Insulinotropic Polypeptide (GIP) and Glucagon-Like …
Designing a dual GLP-1R/GIPR agonist from tirzepatide: comparing residues between tirzepatide, GLP-1, and GIP
L Wang - Drug design, development and therapy, 2023 - Taylor & Francis
Improving type 2 diabetes using incretin analogues is becoming increasingly plausible.
Currently, tirzepatide is the most promising listed incretin analogue. Here, I briefly explain …
Currently, tirzepatide is the most promising listed incretin analogue. Here, I briefly explain …
Obesity pharmacotherapy: incretin action in the central nervous system
The prevalence of obesity is rising, creating an urgent need for efficacious therapies. Recent
clinical trials show that tirzepatide, a dual agonist of receptors for the incretin hormones …
clinical trials show that tirzepatide, a dual agonist of receptors for the incretin hormones …
Engineered mini-G proteins block the internalization of cognate GPCRs and disrupt downstream intracellular signaling
Y Manchanda, L ElEid, AI Oqua, Z Ramchunder… - Science …, 2024 - science.org
Mini-G proteins are engineered, thermostable variants of Gα subunits designed to stabilize
G protein–coupled receptors (GPCRs) in their active conformations. Because of their small …
G protein–coupled receptors (GPCRs) in their active conformations. Because of their small …