来自杂志 Expert opinion on therapeutic patents 的文献。
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李翛然
(2024-06-28 14:45):
#paper: doi.org/10.1080/13543776.2024.2369630 Inhibition of GTPase KRASG12D: a review of patent literature 最近发了篇paper 专利回顾的。我们做了个国产替代, 药物上市太墨迹了,就用ai设计了一个荧光探针试剂盒,以后所有想做KRAS,以及KRAS的多突变药物的,直接买这个试剂盒可以测试药物活性,很方便,对标产品1.6万一盒,我们才6000. 国际上就我们2家。 欢迎大家采购。 核心原理不难,就是把一个对标的有效抑制剂,尾部挂上荧光探针,用AI把linker设计出来,再加一些好合成的条件。 今年这个AI也要发一个paper ,大家别急,带条件生成的ai,也是国际上第一个。另外预告一下,今年我们会用光量子计算机,设计蛋白质~~
IF:5.400Q1
Expert opinion on therapeutic patents,
2024-Aug.
DOI: 10.1080/13543776.2024.2369630
PMID: 38884569
Abstract:
INTRODUCTION: KRAS is a critical oncogenic protein intricately involved in tumor progression, and the difficulty in targeting KRAS has led it to be classified as an 'undruggable target.' Among the …
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INTRODUCTION: KRAS is a critical oncogenic protein intricately involved in tumor progression, and the difficulty in targeting KRAS has led it to be classified as an 'undruggable target.' Among the various KRAS mutations, KRASG12D is highly prevalent and represents a promising therapeutic target, yet there are currently no approved inhibitors for it.AREA COVERED: This review summarizes numerous patents and literature featuring inhibitors or degraders of KRASG12D through searching relevant information in PubMed, SciFinder and Web of Science databases from 2021 to February 2024, providing an overview of the research progress on inhibiting KRASG12D in terms of design strategies, chemical structures, biological activities, and clinical advancements.EXPERT OPINION: Since the approval of AMG510 (Sotorasib), there has been an increasing focus on the inhibition of KRASG12D, leading to numerous reports of related inhibitors and degraders. Among them, MRTX1133, as the first KRASG12D inhibitor to enter clinical trials, has demonstrated excellent tumor suppression in various KRASG12D-bearing human tumor xenograft models. It is important to note, however, that understanding the mechanisms of acquired resistance caused by KRAS inhibition and developing additional combination therapies is crucial. Moreover, seeking covalent inhibition of KRASG12D also holds significant potential.
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