52898-20-1Relevant academic research and scientific papers
Cancer-targeting antibody-drug conjugates: Site-specific conjugation of doxorubicin to anti-EGFR 528 Fab′ through a polyethylene glycol linker
Hong, Lisa P. T.,Scoble, Judith A.,Doughty, Larissa,Coia, Gregory,Williams, Charlotte C.
, p. 779 - 789 (2011)
Antibodydrug conjugates have been prepared to examine the effect that attaching small-molecule drugs to an antibody fragment has on antibody activity. The anticancer drug doxorubicin was covalently attached through a polyethylene glycol linker to a cancer-targeting, anti-epidermal growth factor receptor antibody fragment (Fab′). The reactivity of maleimide was compared with a substituted maleimide derivative (citraconimide) in conjugation reactions with cysteine residues on a Fab′. Introduction of polyethylene glycol increased aqueous solubility of the cytotoxic drug, which led to an improvement in overall yield of the conjugation reaction with the antibody fragment. Antibodydrug conjugates prepared retained activity of the parent antibody, as determined by antigen binding experiments measured by surface plasmon resonance.
Synthesis of 4-maleimidobutyric acid and related maleimides
De Figueiredo, Renata Marcia,Oczipka, Philipp,Froehlich, Roland,Christmann, Mathias
, p. 1316 - 1318 (2008)
Maleimidoalkanoic acids and their activated derivatives, such as their N-hydroxysuccinimide esters, are important, though expensive, linkers for the conjugation of biomolecules. During our synthesis of UCS1025A, we have developed a chromatography-free preparation of 4-maleimidobutyric acid on a one-mole scale. Georg Thieme Verlag Stuttgart.
