The cryptophycins as potent payloads for antibody drug conjugates

[Display omitted] 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 refle...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2015-02, Vol.25 (4), p.864-868
Hauptverfasser:	Verma, Vishal A., Pillow, Thomas H., DePalatis, Laura, Li, Guangmin, Phillips, Gail Lewis, Polson, Andrew G., Raab, Helga E., Spencer, Susan, Zheng, Bing
Format:	Artikel
Sprache:	eng
Schlagworte:	Antibody drug conjugate Antineoplastic Agents - therapeutic use Cell Line, Tumor Cryptophycin Depsipeptides - therapeutic use Humans Immunoconjugates - therapeutic use
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Zusammenfassung:	[Display omitted] 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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2014.12.070