G蛋白偶联受体(GPCR)

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Cell重磅:华人团队开发新型镇痛药物,效果突出且避免成瘾等副作用
生物世界· 2025-05-20 03:03
Core Viewpoint - The article discusses the development of a new non-addictive pain relief drug, SBI-810, which targets neurotensin receptor-1 (NTSR1) and offers effective pain management without the severe side effects associated with opioid medications [3][10]. Group 1: Pain Management and Opioid Crisis - Pain is the primary reason for seeking medical care, affecting over 600 million people globally, with opioid medications widely used despite addiction risks [2]. - The economic burden and social impact of opioid use disorder have prompted U.S. healthcare agencies to prioritize the development of safer alternatives [2]. Group 2: Research and Development of SBI-810 - SBI-810 is a novel analgesic that provides strong pain relief for both acute and chronic pain, demonstrating more precise action than opioids by selectively activating the β-arrestin2 signaling pathway [3][8]. - The research team has applied for multiple patents related to SBI-810 and plans to initiate human clinical trials soon [3]. Group 3: Mechanism of Action - SBI-810's analgesic effects require NTSR1 and β-arrestin2 but do not involve NTSR2 or β-arrestin1, inhibiting excitatory synaptic transmission in spinal cord nociceptive neurons [8]. - It reduces the expression of Nav1.7 in primary sensory neurons and diminishes the response of C fibers, effectively blocking both peripheral and central sensitization [8][10]. Group 4: Benefits Over Opioids - SBI-810 alleviates common opioid-related side effects such as constipation and tolerance, and it reduces withdrawal symptoms associated with opioid use [8]. - The findings highlight the potential of NTSR1 biased allosteric modulators as a promising non-addictive pain management strategy, addressing both acute and chronic pain [10].
两个月内达成超50亿美元潜在规模交易,诺和诺德疯狂押注新一代减重疗法
Di Yi Cai Jing· 2025-05-14 13:40
Group 1 - Novo Nordisk's market value has decreased by over 50% from its peak a year ago, primarily due to competitive pressures from Eli Lilly's GLP-1 drug, tirzepatide, which has shown superior weight loss efficacy compared to semaglutide [1][3] - Novo Nordisk has made significant investments in weight loss therapies, including a recent collaboration with Septerna to develop oral small molecule drugs for obesity and type 2 diabetes, with a potential deal value of up to $2.2 billion, including a $200 million upfront payment [1][3] - In March, Novo Nordisk entered into a $1 billion licensing agreement with Lexicon Pharmaceuticals for a drug targeting obesity and related metabolic disorders, and also acquired global rights for a three-target agonist weight loss drug from China National Pharmaceutical for up to $2 billion [3] Group 2 - Both Novo Nordisk and Eli Lilly are focusing on next-generation weight loss drugs, including oral formulations, with Novo Nordisk emphasizing its historical innovation in obesity and diabetes treatment [3][4] - The U.S. regulatory agency has accepted Novo Nordisk's application for the oral version of semaglutide, which, if approved, will be the first oral GLP-1 weight loss therapy [4] - Novo Nordisk is also exploring digital health solutions for obesity management, recently partnering with Ping An Health Technology to create a comprehensive service model for obesity management and public health education [4]