锁定一个臭名昭著的难以捉摸的癌症靶点：通过共价小分子直接抑制 MYC。
Nailing Down a Notoriously Elusive Cancer Target: Direct Inhibition of MYC by a Covalent Small Molecule.
机构信息
David H. Koch Institute for Integrative Cancer Research, Massachusetts Institute of Technology, Cambridge, MA 02142, USA.
David H. Koch Institute for Integrative Cancer Research, Massachusetts Institute of Technology, Cambridge, MA 02142, USA.
出版信息
Cell Chem Biol. 2021 Jan 21;28(1):1-3. doi: 10.1016/j.chembiol.2020.12.014.
Abstract
Direct inhibition of the transcription factor MYC is widely recognized as one of the thorniest challenges in cancer drug discovery. In this issue of Cell Chemical Biology, Boike et al. (2020) discover a covalent MYC inhibitor that selectively targets a single cysteine residue in an unstructured region of the protein.
摘要
直接抑制转录因子 MYC 被广泛认为是癌症药物发现中最棘手的挑战之一。在本期《细胞化学生物学》中，Boike 等人（2020 年）发现了一种共价 MYC 抑制剂，它选择性地靶向蛋白质无规则区域中的单个半胱氨酸残基。
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