7-Deazaxanthine, a novel prototype inhibitor of thymidine phosphorylase.

7-Deazaxanthine (7DX) was identified as a novel inhibitor of thymidine (dThd) phosphorylase (TPase). It inhibited the TPase reaction in a concentration-dependent manner. At 1 mM, it almost completely prevented the TPase-catalysed hydrolysis of dThd to thymine. The 50% inhibitory concentration (IC50...

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Asıl Yazarlar: Balzarini, J, Gamboa, A, Esnouf, R, Liekens, S, Neyts, J, De Clercq, E, Camarasa, M, Pérez-Pérez, M
Materyal Türü: Journal article
Dil:English
Baskı/Yayın Bilgisi: 1998
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author Balzarini, J
Gamboa, A
Esnouf, R
Liekens, S
Neyts, J
De Clercq, E
Camarasa, M
Pérez-Pérez, M
author_facet Balzarini, J
Gamboa, A
Esnouf, R
Liekens, S
Neyts, J
De Clercq, E
Camarasa, M
Pérez-Pérez, M
author_sort Balzarini, J
collection OXFORD
description 7-Deazaxanthine (7DX) was identified as a novel inhibitor of thymidine (dThd) phosphorylase (TPase). It inhibited the TPase reaction in a concentration-dependent manner. At 1 mM, it almost completely prevented the TPase-catalysed hydrolysis of dThd to thymine. The 50% inhibitory concentration (IC50 of 7DX was 40 microM in the presence of 100 microM of the natural substrate dThd. 7DX is also endowed with a marked inhibitory effect on angiogenesis. It significantly prevents neovascularisation in the chicken chorioallantoic membrane during development. 7DX is the first purine derivative shown to be a potent inhibitor of purified TPase and angiogenesis.
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spelling oxford-uuid:56f4e9ae-edc1-410c-8531-501deaab58d92022-03-26T16:53:47Z7-Deazaxanthine, a novel prototype inhibitor of thymidine phosphorylase.Journal articlehttp://purl.org/coar/resource_type/c_dcae04bcuuid:56f4e9ae-edc1-410c-8531-501deaab58d9EnglishSymplectic Elements at Oxford1998Balzarini, JGamboa, AEsnouf, RLiekens, SNeyts, JDe Clercq, ECamarasa, MPérez-Pérez, M7-Deazaxanthine (7DX) was identified as a novel inhibitor of thymidine (dThd) phosphorylase (TPase). It inhibited the TPase reaction in a concentration-dependent manner. At 1 mM, it almost completely prevented the TPase-catalysed hydrolysis of dThd to thymine. The 50% inhibitory concentration (IC50 of 7DX was 40 microM in the presence of 100 microM of the natural substrate dThd. 7DX is also endowed with a marked inhibitory effect on angiogenesis. It significantly prevents neovascularisation in the chicken chorioallantoic membrane during development. 7DX is the first purine derivative shown to be a potent inhibitor of purified TPase and angiogenesis.
spellingShingle Balzarini, J
Gamboa, A
Esnouf, R
Liekens, S
Neyts, J
De Clercq, E
Camarasa, M
Pérez-Pérez, M
7-Deazaxanthine, a novel prototype inhibitor of thymidine phosphorylase.
title 7-Deazaxanthine, a novel prototype inhibitor of thymidine phosphorylase.
title_full 7-Deazaxanthine, a novel prototype inhibitor of thymidine phosphorylase.
title_fullStr 7-Deazaxanthine, a novel prototype inhibitor of thymidine phosphorylase.
title_full_unstemmed 7-Deazaxanthine, a novel prototype inhibitor of thymidine phosphorylase.
title_short 7-Deazaxanthine, a novel prototype inhibitor of thymidine phosphorylase.
title_sort 7 deazaxanthine a novel prototype inhibitor of thymidine phosphorylase
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