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Chemoselective Installation of Amine Bonds on Proteins through Aza-Michael Ligation.通过氮杂迈克尔加成反应在蛋白质上选择性地安装胺键。
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2
Brentuximab vedotin for advanced Hodgkin's lymphoma.本妥昔单抗用于治疗晚期霍奇金淋巴瘤。
Lancet Oncol. 2017 Dec;18(12):1566-1568. doi: 10.1016/S1470-2045(17)30845-8. Epub 2017 Nov 10.
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Inotuzumab ozogamicin for the treatment of acute lymphoblastic leukemia.奥英妥珠单抗用于治疗急性淋巴细胞白血病。
Expert Opin Biol Ther. 2017 Dec;17(12):1557-1564. doi: 10.1080/14712598.2017.1387244. Epub 2017 Nov 1.
4
Cathepsin B Is Dispensable for Cellular Processing of Cathepsin B-Cleavable Antibody-Drug Conjugates.组织蛋白酶 B 对于可被组织蛋白酶 B 切割的抗体药物偶联物的细胞内加工是可有可无的。
Cancer Res. 2017 Dec 15;77(24):7027-7037. doi: 10.1158/0008-5472.CAN-17-2391. Epub 2017 Oct 18.
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Gemtuzumab ozogamicin for acute myeloid leukemia.吉妥珠单抗奥佐米星治疗急性髓细胞白血病。
Blood. 2017 Nov 30;130(22):2373-2376. doi: 10.1182/blood-2017-09-797712. Epub 2017 Oct 11.
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Five-year results of brentuximab vedotin in patients with relapsed or refractory systemic anaplastic large cell lymphoma.本妥昔单抗治疗复发或难治性系统性间变性大细胞淋巴瘤患者的5年结果
Blood. 2017 Dec 21;130(25):2709-2717. doi: 10.1182/blood-2017-05-780049. Epub 2017 Oct 3.
7
A non-internalizing antibody-drug conjugate based on an anthracycline payload displays potent therapeutic activity in vivo.基于蒽环类药物有效载荷的非内化抗体药物偶联物在体内显示出强大的治疗活性。
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Inotuzumab Ozogamicin: First Global Approval.依妥珠单抗奥滨尤妥珠单抗：全球首次获批
Drugs. 2017 Sep;77(14):1603-1610. doi: 10.1007/s40265-017-0802-5.
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Protease-Cleavable Linkers Modulate the Anticancer Activity of Noninternalizing Antibody-Drug Conjugates.蛋白酶可裂解连接子调节非内化抗体-药物偶联物的抗癌活性。
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Targeted α-Therapy of Metastatic Castration-Resistant Prostate Cancer with Ac-PSMA-617: Dosimetry Estimate and Empiric Dose Finding.转移性去势抵抗性前列腺癌的靶向 α 治疗：Ac-PSMA-617 的剂量估算和经验剂量探索。
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化学定义的抗体-小分子药物偶联物在体内肿瘤靶向应用中的比较分析。

Chemically Defined Antibody- and Small Molecule-Drug Conjugates for in Vivo Tumor Targeting Applications: A Comparative Analysis.

机构信息

Department of Chemistry and Applied Biosciences, Swiss Federal Institute of Technology (ETH Zürich) , Vladimir-Prelog-Weg 4, CH-8093 Zurich, Switzerland.

出版信息

J Am Chem Soc. 2018 Feb 7;140(5):1617-1621. doi: 10.1021/jacs.7b13361. Epub 2018 Jan 27.

DOI:10.1021/jacs.7b13361
PMID:29342352
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5844464/
Abstract

We present the first direct comparative evaluation of an antibody-drug conjugate and of a small molecule-drug conjugate for cancer therapy, using chemically defined products which bind with high-affinity to carbonic anhydrase IX, a marker of tumor hypoxia and of renal cell carcinoma.

摘要

我们首次对抗体药物偶联物和小分子药物偶联物进行了直接比较评估，这两种偶联物均采用化学定义的产品，它们与碳酸酐酶 IX （肿瘤缺氧和肾细胞癌的标志物）高亲和力结合。