KRAS抑製劑的發展曆程

經過多年的努力，科學家們在針對幾種惡性腫瘤的KRAS突變方麵已經取得了多向進展:

After decades of efforts, scientists have made progress into targeting KRAS mutations in several malignancies.

在1967年, Ha-Ras 和 Ki-Ras逆轉錄病毒轉化基因被發現，它們對應的人類RAS家族HRAS和KRAS於1982年被發現.

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 與肺癌的關係於1984年被首次描述，這些年KRAS 突變在肺癌中已經有多項進展。突變的KRAS被持續性激活，並導致持續的下遊信號傳導和腫瘤發生。

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2013年隨著對KRAS生物學的了解加深和藥物設計技術的更新，科學家們在GDP結合的突變型KRAS G12C 蛋白中發現了半胱氨酸藥物結合袋。

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2021年，科學家們成功開發出阻斷突變型KRAS G12C 的共價抑製劑。2021年5月，Sotorasib獲得FDA批準，用於治療KRAS G12C突變的NSCLC，這是第一個獲批的KRAS G12C抑製劑，目前還有更多藥物正在研發中。

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。

KRAS新藥研發平台

什麽是KRAS?

KRAS的信號通路

hjc黄金城助力信諾維抗腫瘤1類新藥XNW14010（小分子KRAS G12C蛋白共價結合抑製劑）獲批臨床