Selective derivatization of N-terminal cysteines using cyclopentenediones

The outcome of the Michael-type reaction between thiols and 2,2-disubstituted cyclopentenediones varies depending on the thiol. Stable compounds with two fused rings were formed upon reaction with 1,2-aminothiols (such as N-terminal cysteines in peptides). Other thiols gave reversibly Michael-type a...

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Detalles Bibliográficos
Autores: Brun Cubero, Omar, Agramunt, Jordi, Raich Armendáriz, Lluís Adrià, Rovira i Virgili, Carme, Pedroso Muller, Enrique, Grandas Sagarra, Anna
Tipo de recurso: artículo
Estado:Versión aceptada para publicación
Fecha de publicación:2016
País:España
Institución:Universidad de Barcelona
Repositorio:Dipòsit Digital de la UB
OAI Identifier:oai:diposit.ub.edu:2445/102811
Acceso en línea:https://hdl.handle.net/2445/102811
Access Level:acceso abierto
Palabra clave:Bioquímica
Reaccions químiques
Cisteïna
Biochemistry
Chemical reactions
Cysteine
Descripción
Sumario:The outcome of the Michael-type reaction between thiols and 2,2-disubstituted cyclopentenediones varies depending on the thiol. Stable compounds with two fused rings were formed upon reaction with 1,2-aminothiols (such as N-terminal cysteines in peptides). Other thiols gave reversibly Michael-type adducts that were in equilibrium with the starting materials. This differential reactivity allows differently placed cysteines to be distinguished and has been exploited to prepare bioconjugates incorporating two or three different moieties.