Synthese potentieller Cytostatica. V. 4‐Brom‐butyläther von mehrbasischen Aminoäthanolen

SummaryAffinity chromatography of proteins requires a ligand covalently bound to a solid support separated by a spacer of sufficient length. In the specific case of acetylcholinesterase we have reduced the conventional spacer synthesis from five to three steps.For affinity chromatography of cholinergic proteins the ideal ligand would be acetylcholine which, however, could not be used because it is easily hydrolyzed. We synthesized hydrolysis-resistent ligands. Different specific ligands were synthesized for the affinity chromatography of serum esterase.Affinity chromatography has achieved great importance in the last decade for the purification of biologically active proteins [l-31. In this method a ligand bound covalently to a solid support creates an affinity for the desired protein. As proteins generally have large molecular volumes, the ligand must not be too closely bound onto the support. Cuatrecasas [ 11 first mentioned the importance of a 'spacer'. In the case of acetylcholinesterase, from both theoretical and practical experience, the ligand must be bound to a spacer of 45-58 A of length to achieve optimum interaction with the active centre of the enzyme. The definition 'affinity chromatography' has been used differently by several authors. Unspecific elution of the desired protein with increasing ionic strength of buffer solutions after more or less specific adsorption on a support has also been defined as 'affinity chromatography' [4] [5]. We use the term affinity chromatography to mean specific adsorption and subsequent specific desorption chromatography.An adequate support for affinity chromatography is agarose'). Cuatrecasas [ 11 has already described in detail the spacer synthesis on agarose. Generally the following sequence leads to good results. Bromocyano-activation of agarose, coupling with a diamine, elongation with succinic anhydride, another treatment with diamine catalyzed by water-soluble carbodiimide, again elongation with succinic anhydride, and finally, carbodiimide-catalyzed coupling of the ligand.

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Synthesis of specific cholinergic inhibitors for affinity chromatography

Riggio

Hopff

Hofmann

1979

Experientia

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Synthese potentieller Cytostatica. V. 4‐Brom‐butyläther von mehrbasischen Aminoäthanolen

Cited by 4 publications

References 9 publications

ChemInform Abstract: SYNTHESE POTENTIELLER CYTOSTATICA 5. MITT. 4‐BROM‐BUTYLAETHER VON MEHRBASISCHEN AMINOAETHANOLEN

ChemInform Abstract: SYNTHESE POTENTIELLER CYTOSTATICA 5. MITT. 4‐BROM‐BUTYLAETHER VON MEHRBASISCHEN AMINOAETHANOLEN

Specific Ligands for the Affinity Chromatography of Cholinergic Proteins

Synthesis of specific cholinergic inhibitors for affinity chromatography

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