Topics Archives: GPCR

The glucagon receptor (GCGR):A Key Target in Glucose Metabolism

On June 25, 2024, at the 2024 American Diabetes Association (ADA) Scientific Sessions, Suzhou Innovent Biologics and Eli Lilly announced the results of a Phase 3 clinical trialfor the GLP-1R x GCGR dual agonist, Mazdutide. This marks the first Phase 3 clinical trial (GLORY-1) in overweight or obese adults in China。The study’s primary results and exploratory endpoints of liver fat content were disclosed, showing that Mazdutide acts as a dual agonist for both GLP-1R and GCGR. It reduces body weight by suppressing appetite and delaying gastric emptying through GLP-1R activation, while enhancing weight loss efficacy by increasing energy expenditure via GCGR activation. Notably, Mazdutide uniquely promotes fatty acid oxidation and lipolysis in the liver through GCGR activation, thereby improving liver fat metabolism. As GCGR plays a crucial role in glucose metabolism, it has become a hot target in the development of diabetes and weight loss drugs.Let’s delve into the role of  the Glucagon Receptor (GCGR).

Blog ,, 2024-08-29
the structure of GPL1R

GLP1R Target: Not Just for Blood Sugar Control and Weight Loss, but a Potential Breakthrough for Anti-Nausea in Weight Loss Medications

Currently, the most popular GLP1-based monotherapy, Semaglutide, controls blood sugar by promoting insulin secretion and induces a lasting sense of fullness to reduce appetite. However, this drug can cause side effects such as nausea and vomiting, which can affect patient adherence to the treatment. On July 10, 2024, Kuei-Pin Huang and colleagues published a paper…

Blog ,, 2024-08-19
The structure of GIPR

GIP Receptor (GIPR): A Novel Target for Glycemic Control and Weight Loss

On February 27, 2024, Viking Therapeutics announced the results of their Phase IIa clinical study for VK2735, a dual GLP-1R/GIPR agonist for obesity. The results showed a maximum weight loss of 13.1% after 13 weeks of treatment. Following this news, Viking’s stock surged by 121%. The company has received written feedback from the FDA and…

Blog ,, 2024-08-08
20-HETE Receptor (GPR75) Signaling in Endothelial Cells

GPR75 – An Emerging Target for Weight Loss Drugs

When it comes to weight loss medications, one cannot overlook the remarkable success of Semaglutide (GLP-1 weight loss drug), which has propelled the Danish biopharmaceutical company, Novo Nordisk, to new heights. According to Novo Nordisk’s financial report for 2023, Semaglutide sales reached $21.2 billion in 2023. On March 7th, Novo Nordisk’s stock price surged by…

Blog ,, 2024-04-01
mRNA expression of GPRC5D in malignant cell lines

GPRC5D, a promising therapeutic target for multiple myeloma

In 2023…… On May 12th, LaNova announced that AstraZeneca will receive an exclusive global license for LM-305’s research, development, and commercialization. LM-305 is a new pre-clinical stage antibody-drug conjugate (ADC) targeting GPRC5D. LaNova Medicines will receive an immediate payment of $55 million and $545 million in additional development and commercial milestone payments. On May 19th, the clinical trial application for OriCAR-017…

Blog ,, 2023-07-14