A click-ready pH-triggered phosphoramidate-based linker for controlled release of monomethyl auristatin E.

Olatunji, Feyisola P; Herman, Jacob W; Kesic, Brittany N; Olabode, Damilola; Berkman, Clifford E

Olatunji, Feyisola P; Herman, Jacob W; Kesic, Brittany N; Olabode, Damilola; Berkman, Clifford E.

Afiliación

Olatunji FP; Washington State University, Department of Chemistry, PO Box 644630, Pullman, WA 99164-4630, United States.
Herman JW; Washington State University, Department of Chemistry, PO Box 644630, Pullman, WA 99164-4630, United States.
Kesic BN; Washington State University, Department of Chemistry, PO Box 644630, Pullman, WA 99164-4630, United States.
Olabode D; Washington State University, Department of Mathematics and Statistics, PO Box 643113, Pullman, WA 99164-3113, United States.
Berkman CE; Washington State University, Department of Chemistry, PO Box 644630, Pullman, WA 99164-4630, United States.

Tetrahedron Lett ; 61(41)2020 Oct 08.

Article en En | MEDLINE | ID: mdl-33191958

ABSTRACT

ABSTRACT

In this work, we developed a novel "click"-ready pH-cleavable phosphoramidate linker for controlled-release of monomethyl auristantin E (MMAE) in antibody- and small molecule-drug conjugates application. This water-soluble linker was found to have tremendous stability at physiological pHs while rapidly releasing its payload at acidic pH. The linker can also be tailored to release payloads of diverse functional groups, broadening its applications.

Palabras clave

Cleavable linker; MMAE; Monomethyl auristatin E; Payload click-ready; Phosphoramidate

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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Idioma: En Revista: Tetrahedron Lett Año: 2020 Tipo del documento: Article País de afiliación: Estados Unidos

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