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KRAS抑制剂的发展历程

2024-01-08
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路过二十多年的坚持,生物遗传学家们在采取类型梭形细胞肺部肿瘤肺部肿瘤的KRAS基因突变的方面以及认定了多向新况:After decades of efforts, scientists have made progress into targeting KRAS mutations in several malignancies.在196八年, Ha-Ras 和 Ki-Ras终结录病毒码变为什么是基因被出现,这句话使用的全人类RAS族氏HRAS和KRAS于1982年被出现.In 1967, Ha-Ras and Ki-Ras retroviral transforming genes were discovered.Their human counterparts,Ha-Ras and Ki-Ras ,were discovered in 1982.KRAS 与肺腺癌的的关联于198多年被第一次 简述,哪些年KRAS 基因变异在肺腺癌中早已经有各项进步。基因变异的KRAS被继续性激话,并引起继续的河流下游信息减弱和肺部肿瘤引发。The relationship between KRAS and lung cancer was described in 1984,KRAS mutation in lung cancer has progressed.Mutant KRAS is constitutively activated and leads to persistent downstream signalling and oncogenesis.在201两年多跟着对KRAS动物学的知晓显现和中药设汁新技术的更新换代,科学合理家们在GDP紧密相结合的突然变化型KRAS G12C 淀粉酶中找到了半胱氨酸中药紧密相结合袋。In 2013 improved understanding of KRAS biology and newer drug designing technologies led to crucial discovery of a cysteins drug binding pocket in GDP-bound mutant KRAS G12C  protein.在2023年,生物专家们取得胜利开发技术出传导变化性型KRAS G12C 的共价可抑药物治疗药品。2023年五月,Sotorasib领取FDA审批权,用作的治疗KRAS G12C变化性的NSCLC,这才是第1 个将建的KRAS G12C可抑药物治疗药品,当下仍有更高药物治疗将要研发管理中。In 2021,covalent inhibitors that block mutant KRAS G12C were successfully developed.In May 2021 the US FDA granted accelerated approval to Sotorasib(1st KRAS G12C inhibitor),for the treatment of adults with advanced NSCLC with KRAS G12C mutation.Sotorasib was the first KRAS G12C inhibitor to be approved,with several more in the pipeline。
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