INSIDE THE PLASMA AMINE OXIDASE: PRELIMINARY DRUG DISCOVERY STUDY OF PLASMA AMINE OXIDASE: STRUCTURAL BASIS OF SUBSTRATE AND INHIBITORY ACTIVITY OF BOVINE PLASMA AMINE OXIDASE - Couverture souple

Chen, Yanwen

 
9783639255683: INSIDE THE PLASMA AMINE OXIDASE: PRELIMINARY DRUG DISCOVERY STUDY OF PLASMA AMINE OXIDASE: STRUCTURAL BASIS OF SUBSTRATE AND INHIBITORY ACTIVITY OF BOVINE PLASMA AMINE OXIDASE
Couverture souple
ISBN 10 : 3639255682 ISBN 13 : 9783639255683
Editeur : VDM Verlag, 2010

Synopsis

The copper-containing amine oxidases, like bovine plasma amine oxidase (BPAO), carry out a transaminative oxidation of primary amines to aldehydes via use of an active site Tyr-derived 2,4,5-trihydroxyphenylalanine quinone (TPQ) cofactor. Propargylamine is a potent inactivator of BPAO (IC50 = 3 µM), possibly through active-site modification by the a,ß-unsaturated aldehyde turnover product, but the simple structure is expected to confer low selectivity. On the basis of the finding by previous students that certain extended conjugation analogs such as 1,6-diamino-2,4- hexadiyne and 3-cyanopropargylamine preserve strong inactivation potency, other extended conjugation analogs of propargylamine were evaluated. In particular, 1-amino-2,4-hexadiynes with a 6-OH rather than 6-NH2 group were found to be potent inhibitors.

Les informations fournies dans la section « Synopsis » peuvent faire référence à une autre édition de ce titre.

Présentation de l'éditeur

The copper-containing amine oxidases, like bovine plasma amine oxidase (BPAO), carry out a transaminative oxidation of primary amines to aldehydes via use of an active site Tyr-derived 2,4,5-trihydroxyphenylalanine quinone (TPQ) cofactor. Propargylamine is a potent inactivator of BPAO (IC50 = 3 µM), possibly through active-site modification by the a,ß-unsaturated aldehyde turnover product, but the simple structure is expected to confer low selectivity. On the basis of the finding by previous students that certain extended conjugation analogs such as 1,6-diamino-2,4- hexadiyne and 3-cyanopropargylamine preserve strong inactivation potency, other extended conjugation analogs of propargylamine were evaluated. In particular, 1-amino-2,4-hexadiynes with a 6-OH rather than 6-NH2 group were found to be potent inhibitors.

Les informations fournies dans la section « A propos du livre » peuvent faire référence à une autre édition de ce titre.

Éditeur
VDM Verlag
Date d'édition
2010
Langue
anglais
ISBN 10 
3639255682
ISBN 13 
9783639255683
Reliure
Broché
Nombre de pages
216
Coordonnées du fabricant
non disponible
Personne responsable
non disponible