An Exceptionally Potent Inhibitor of Human CD73

Bowman Christine E.; da Silva Rafael G.; Pham Amber; Young Stephen W.

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An Exceptionally Potent Inhibitor of Human CD73

机译：人类CD73的异常有效的抑制剂

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We recently reported the initiation of a Phase I clinical trial with AB680, a potent human CD73 inhibitor, being developed for the treatment of solid tumors (NCT03677973). We undertook a detailed kinetic analysis of the interaction between human CD73 and AB680 to determine the mode of inhibition. We found AB680 to be a reversible, slow-onset competitive inhibitor of human CD73 with a K-i of 5 pM. Clinical candidates of this potency are uncommon and deserve special consideration during lead optimization.

机译：我们最近报道了与AB680的临床试验开始，这是一种用于治疗实体肿瘤的效力人CD73抑制剂（NCT03677973）。我们对人CD73和AB680之间的相互作用进行了详细的动力学分析，以确定抑制模式。我们发现AB680是一种可逆的，慢性发病的人类CD73的竞争性抑制剂，k-i pm为5 pm。这种效力的临床候选者罕见并在铅优化期间应得特别考虑。

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《Biochemistry》 |2019年第31期|共4页
作者
Bowman Christine E.; da Silva Rafael G.; Pham Amber; Young Stephen W.;
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Arcus Biosci Inc Dept Quantitat Biol 3928 Point Eden Way Hayward CA 94545 USA;

Univ St Andrews Biomed Sci Res Complex Sch Biol St Andrews KY16 9ST Fife Scotland;

Arcus Biosci Inc Dept Quantitat Biol 3928 Point Eden Way Hayward CA 94545 USA;

Arcus Biosci Inc Dept Quantitat Biol 3928 Point Eden Way Hayward CA 94545 USA;

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正文语种 eng
中图分类生物化学;
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1. An Exceptionally Potent Inhibitor of Human CD73 [J] . Bowman Christine E., da Silva Rafael G., Pham Amber, Biochemistry . 2019,第31期

机译：人类CD73的异常有效的抑制剂
2. Anti-human CD73 monoclonal antibody inhibits metastasis formation in human breast cancer by inducing clustering and internalization of CD73 expressed on the surface of cancer cells [J] . TerpM.G., OlesenK.A., ArnspangE.C., The Journal of Immunology: Official Journal of the American Association of Immunologists . 2013,第8期

机译：抗人CD73单克隆抗体通过诱导癌细胞表面表达的CD73的聚集和内在化来抑制人乳腺癌的转移形成
3. AB680, a potent and selective CD73 small molecule inhibitor, reverses the AMP/adenosine-mediated impairment of immune effector cell activation by immune checkpoint inhibitors [J] . Schindler U., Becker A., Lawson K., European journal of cancer: official journal for European Organization for Research and Treatment of Cancer (EORTC) [and] European Association for Cancer Research (EACR) . 2018,第期

机译：AB680，一种有效和选择性的CD73小分子抑制剂，逆转AMP /腺苷介导的免疫效应细胞活化的损伤通过免疫检查点抑制剂
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机译：第一部分：串联Diels-Alder中的1,3,4-恶二唑，1,3-偶极环加成反应：长春花生物碱基序的快速合成。第二部分：脂肪酸酰胺水解酶的超强抑制剂
6. Exceptionally Potent and Broadly Cross-Reactive Bispecific Multivalent HIV-1 Inhibitors Based on Single Human CD4 and Antibody Domains [O] . Weizao Chen, Yang Feng, Ponraj Prabakaran, 2014

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7. An Exceptionally Potent Inhibitor of Human CD73 [O] . -1

机译：人类CD73的异常有效的抑制剂

An Exceptionally Potent Inhibitor of Human CD73

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