Method for conjugating to polyamino compounds employing haloacyl

Chemistry: molecular biology and microbiology – Enzyme – proenzyme; compositions thereof; process for... – Stablizing an enzyme by forming a mixture – an adduct or a...

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435177, 435 7, 260112R, 424 12, 260112B, 2601125R, 2601127, C12N 996

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active

042207223

ABSTRACT:
Methods and compositions are provided for conjugating a wide variety of compounds, particularly polyfunctional compounds, having a mercapto group, either naturally present or synthetically introduced, to a polyamino compound, particularly a polypeptide (including proteins). The method employs a haloalkylcarbonyl compound, which is conjugated to one or more of the amino groups under mild acylating conditions. This is followed by combining the acylated polyamino compound with a mercapto containing compound, whereby the halogen is displaced by the sulfur of the mercapto group to form a stable thioether linkage. The resulting conjugates, depending on the compounds involved, can find uses in immunoassays, as hapten-antigen conjugates for the production of antibodies, and as ligand analog enzyme conjugates for use as reagents in controlling the distribution of substitution of a mercapto compound to a polyamino compound.

REFERENCES:
patent: 4067774 (1978-01-01), Rubenstein
patent: 4100268 (1978-07-01), Scherr
patent: 4144131 (1979-03-01), Richardson

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