The cryptophycins as potent payloads for antibody drug conjugates

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:25

Article

Verma, Vishal A.¹  Pillow, Thomas H.¹  DePalatis, Laura¹  Li, Guangmin¹  Phillips, Gail Lewis¹  Polson, Andrew G.¹  Raab, Helga E.¹  Spencer, Susan¹  Zheng, Bing¹ 

[1] Genentech Inc, San Francisco, CA 94080 USA

关键词: Antibody drug conjugate;    Cryptophycin;   

DOI  :  10.1016/j.bmcl.2014.12.070

来源: Elsevier

【 摘 要 】

The cryptophycins are a potent class of cytotoxic agents that were evaluated as antibody drug conjugate (ADC) payloads. Free cryptophycin analog 1 displayed cell activity an order of magnitude more potent than approved ADC payloads MMAE and DM1. This potency increase was also reflected in the activity of the cryptophycin ADCs, attached via a either cleavable or non-cleavable linker. (C) 2015 Elsevier Ltd. All rights reserved.

【 授权许可】

Free