沉寂4年终爆发,STING再次高光!诺华8.35亿美金收购IFM临床前STING拮抗剂

文摘   科技   2024-03-13 22:53   北京  

BOSTONMarch 13, 2024 /PRNewswire/ -- IFM Therapeutics (IFM), a privately held biopharmaceutical company focused on developing therapies that modulate novel targets in the innate immune system, announced today that Novartis has exercised its option to acquire all of the outstanding capital stock of IFM Due, a subsidiary company of IFM. Launched in February 2019, with a focus on developing small molecules that inhibit the cGAS-STING pathway, the company entered into an option and collaboration agreement with Novartis in September, 2019 whereby Novartis made fixed payments sufficient to fully finance IFM Due's research and development costs for the cGAS-STING program in exchange for the option to acquire the IFM Due subsidiary (link). Under the terms of the option exercise, IFM received $90 million in upfront payment and will be eligible for up to $745 million in milestone payments, adding up to $835 million in total consideration.

本人持续关注STING
本人与合作者早在2013年开始研究STING激动剂,仅筛选不到50个分子得到uM级激动剂,并通过分析文献数据,2015首次再发现G10是STING直接激动剂(外界多数认为是非直接激动剂,参考被误杀的首个人STING小分子激动剂)。
2015年和合作者首次筛到STING拮抗剂(仅筛选不到50个化合物),与2018年Nature 报道的H-151 有共同分子骨架,与IFM第一代STING拮抗剂有共同分子骨架(而IFM 于2020年公开

红圈是本人与合作者筛选的STING拮抗剂与IFM拮抗剂相同分子骨架

红圈是本人与合作者筛选的STING拮抗剂与IFM拮抗剂相同分子骨架

IFM靠这个第一代分子,赢得诺华合作

本人还研究过IFM第一代STING拮抗剂应该是脱靶了

靶向性验证,难度非常大,对于STING这种adaptor Protein...
本人与合作者,曾得到过高活性STING dependent inhibitor

基于对STING系统性研究,对激活机理认知达到一定深度。。。预判了STING激动剂的命运!参考GSK放弃了备受瞩目的STING激动剂!网红STING激动机制存疑,国内追随者真能follow上吗?
如今,诺华&IFM,给了STING靶标新生!
开发STING拮抗剂,推荐企业与北京大学蒋争凡教授合作、来鲁华教授合作!

药物发现进展杂评
靶向蛋白非活性位点的药物设计有巨大的待开发空间;Allostery,PROTAC,Covalent binding,PPI 等将undruggable 变为可能。本账号将分享一些前沿药物发现方法、前沿靶点的动态与洞见。