Membrane proteins account for approximately 20-30% of proteins encoded by the human genome and play central roles in cell signaling, substance transport, and cell recognition. Aberrant expression and dysfunction of membrane proteins are closely associated with a variety of diseases, including cancer, neurological disorders, and metabolic diseases, making them key focuses in drug discovery. Among […]
DIMA’s CXCR4-Nanodisc Empowers New Preprint from David Baker, which is entitled “De novo design of miniprotein agonists and antagonists targeting G protein-coupled receptors”
In recent years, the rapid development of AI-driven drug discovery (AI-based drug discovery) and Cryo-EM (cryo-electron microscopy) has gradually unveiled the mysteries of many previously considered “undruggable” protein targets. Among them, membrane proteins, which are crucial targets for drug development, are now seeing unprecedented breakthroughs under the dual influence of AI and Cryo-EM technologies. However, membrane protein […]
1. About Synthetic Nanodisc The lipid composition of traditional membrane scaffold protein (MSP) nanodiscs often differs from that of natural cell membranes, which can lead to deviations in membrane protein properties compared to their native environment. To address this limitation, DIMA has developed the Synthetic Nanodisc platform. This innovative technology enables the direct preparation of […]
Do you remember the temperature and touch receptor TRPV1 that made American scientists David Julius and Ardem Patapoutian accessible to the Nobel Prize in Physiology or Medicine in 2021? Transient Receptor Potential Vanilloid 1 (TRPV1) has gained significant attention in the field of pain treatment due to its potential as a therapeutic target. However, as […]
On July 16, 2024, Dr. Roger Cone, co-founder of the preclinical biotech company Courage, published a study in The Journal of Clinical Investigation titled “Subthreshold activation of the melanocortin system causes generalized sensitization to anorectic agents in mice.” The research demonstrated the synergistic effect between GLP-1 receptor agonists (GLP1RA) and MC4R agonists, revealing that low […]
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).
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 […]
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 […]
Since Ganymed unveiled the efficacy data of Zolbetuximab (IMAB362), the anti-Claudin18.2 monoclonal antibody, for the treatment of advanced gastric and gastroesophageal junction adenocarcinoma (GC/GEJ) at the 2016 ASCO conference, Claudin18.2 has emerged as a focal point for pharmaceutical companies eager to advance therapeutic options. These companies explore various technological routes, including monoclonal antibodies, bispecific antibodies, […]