Thiol-containing crosslinking agent with enhanced steric hindrance

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Abstract
Ricin A chain immunotoxins disulfide cross-linked with conventional, sterically unhindered reagents have unsatisfactorily short circulating life times in vivo. (Acetylthio)succinic anhydride, a thiolating reagent with partial steric hindrance of the sulfur atom, does not remedy this situation. Sulfosuccinimidyl N-[3-(acetylthio)-3-methylbutyryl]-beta- alaninate, a new cross-linker in which the carbon alpha to the sulfur is doubly methylated, creates disulfide bonds 2 orders of magnitude more resistant to reduction than unhindered disulfides. Nevertheless, this deactivated thiolating agent rapidly and reliably cross-links ricin A chain and antibodies to create immunotoxins with in vitro cytotoxicities comparable to those of 2-iminothiolane-coupled conjugates.

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