发现首个共价别构 SUMO E1 激活酶抑制剂。
Discovery of a First-In-Class Covalent Allosteric Inhibitor of SUMO E1 Activating Enzyme.
机构信息
Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02215, USA; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA 02115, USA.
Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02215, USA; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA 02115, USA; Department of Systems Biology and Laboratory of Systems Pharmacology, Harvard Medical School, Boston, MA 02115, USA.
出版信息
Cell Chem Biol. 2019 Feb 21;26(2):153-155. doi: 10.1016/j.chembiol.2019.02.006.
SUMOylation is a post-translational modification with important roles in normal physiology and whose dysregulation is associated with human diseases. In this issue of Cell Chemical Biology, Li et al. (2019) describe a covalent, allosteric inhibitor of the SUMO E1 enzyme and demonstrate its anti-tumor activity in preclinical models of colorectal cancer.
SUMOylation 是一种翻译后修饰，在正常生理中具有重要作用，其失调与人类疾病有关。在本期《细胞化学生物学》中，Li 等人（2019 年）描述了一种 SUMO E1 酶的共价别构抑制剂，并在结直肠癌的临床前模型中证明了其抗肿瘤活性。
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