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

Yanwen Chen

ISBN 10: 3639255682 / ISBN 13: 9783639255683

Published by VDM Verlag Dr. Müller, 2010

About this Item

nach der Bestellung gedruckt Neuware - Printed after ordering - 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.

Seller Inventory # 9783639255683

Bibliographic Details

• Title: 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
• Publisher: VDM Verlag Dr. Müller
• Publication Date: 2010
• Language: English
• ISBN 10: 3639255682
• ISBN 13: 9783639255683
• Binding: Taschenbuch
• Condition: Neu
• Dimensions: 220W x 176H x 33D millimeters 220 millimeters width by 176 millimeters height by 33 millimeters depth
• Weight: 338 grams

About this title

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.