Concepedia

Convergent synthesis of hydrophilic monomethyl dolastatin 10 based drug linkers for antibody–drug conjugation

Kanwen Yang, Bo Chen, Diego A. Gianolio, James E. Stefano, Michelle Busch, Charlene Manning, Kim Alving, Richard C. Gregory, William Brondyk, Robert J. Miller,

Organic & Biomolecular Chemistry · 2019 · 16 citations · 23 references

DOI

Concepts

Abstract

A cytotoxic reagent-free fragment coupling methodology was developed to produce hydrophilic drug linkers to prepare aggregation free antibody–drug conjugates.

References

23

Reducing hydrophobicity of homogeneous antibody-drug conjugates improves pharmacokinetics and therapeutic index

Robert P. Lyon, Tim D. Bovee, Svetlana O. Doronina et al. · Nature Biotechnology · 2015 · 523 citations

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Cleavage of N-Carbobenzoxy Groups by dry Hydrogen Bromide and Hydrogen Chloride

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Dolastatin 10, a powerful cytostatic peptide derived from a marine animal

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Synthesis and Evaluation of Hydrophilic Linkers for Antibody–Maytansinoid Conjugates

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Design and Synthesis of Tesirine, a Clinical Antibody–Drug Conjugate Pyrrolobenzodiazepine Dimer Payload

Arnaud Tiberghien, Jean-Noel Levy, Luke A. Masterson et al. · ACS Medicinal Chemistry Letters · 2016 · 167 citations

, , +17