Thymidine phosphorylase from Escherichia coli: Tight-binding inhibitors as enzyme active-site titrants

Abdul Gbaj; Philip N. Edwards; Philip Reigan; Sally Freeman; Mohammed Jaffar; Kenneth T. Douglas

doi:10.1080/14756360500424010

Thymidine phosphorylase from Escherichia coli: Tight-binding inhibitors as enzyme active-site titrants

Abdul Gbaj, Philip N. Edwards, Philip Reigan, Sally Freeman, Mohammed Jaffar, Kenneth T. Douglas

Research output: Contribution to journal › Article › peer-review

Abstract

Thymidine phosphorylase (EC 2.4.2.4) catalyses the reversible phosphorolysis of pyrimidine 2′-deoxynucleosides, forming 2-deoxyribose-1-phosphate and pyrimidine. 5-Chloro-6-(2-imino-pyrrolidin-1-yl)methyl-uracil hydrochloride (TPI, 1) and its 5-bromo analogue (2), 6-(2-amino-imidazol-1-yl) methyl-5-bromo-uracil (3) and its 5-chloro analogue (4) act as tight-binding stoichiometric inhibitors of recombinant E. coli thymidine phosphorylase, and thus can be used as the first active-site titrants for it using either thymidine or 5-nitro-2′-deoxyuridine as substrate. © 2006 Taylor & Francis.

Original language	English
Pages (from-to)	69-73
Number of pages	4
Journal	Journal of Enzyme Inhibition and Medicinal Chemistry
Volume	21
Issue number	1
DOIs	https://doi.org/10.1080/14756360500424010
Publication status	Published - Feb 2006

Keywords

Angiogenesis
Anticancer drugs
Inhibitors
Stoichiometric inhibition
Thymidine phosphorylase
Transition state inhibitor

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1080/14756360500424010

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title = "Thymidine phosphorylase from Escherichia coli: Tight-binding inhibitors as enzyme active-site titrants",

abstract = "Thymidine phosphorylase (EC 2.4.2.4) catalyses the reversible phosphorolysis of pyrimidine 2′-deoxynucleosides, forming 2-deoxyribose-1-phosphate and pyrimidine. 5-Chloro-6-(2-imino-pyrrolidin-1-yl)methyl-uracil hydrochloride (TPI, 1) and its 5-bromo analogue (2), 6-(2-amino-imidazol-1-yl) methyl-5-bromo-uracil (3) and its 5-chloro analogue (4) act as tight-binding stoichiometric inhibitors of recombinant E. coli thymidine phosphorylase, and thus can be used as the first active-site titrants for it using either thymidine or 5-nitro-2′-deoxyuridine as substrate. {\textcopyright} 2006 Taylor \& Francis.",

keywords = "Angiogenesis, Anticancer drugs, Inhibitors, Stoichiometric inhibition, Thymidine phosphorylase, Transition state inhibitor",

author = "Abdul Gbaj and Edwards, \{Philip N.\} and Philip Reigan and Sally Freeman and Mohammed Jaffar and Douglas, \{Kenneth T.\}",

year = "2006",

month = feb,

doi = "10.1080/14756360500424010",

language = "English",

volume = "21",

pages = "69--73",

journal = "Journal of Enzyme Inhibition and Medicinal Chemistry",

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TY - JOUR

T1 - Thymidine phosphorylase from Escherichia coli: Tight-binding inhibitors as enzyme active-site titrants

AU - Gbaj, Abdul

AU - Edwards, Philip N.

AU - Reigan, Philip

AU - Freeman, Sally

AU - Jaffar, Mohammed

AU - Douglas, Kenneth T.

PY - 2006/2

Y1 - 2006/2

N2 - Thymidine phosphorylase (EC 2.4.2.4) catalyses the reversible phosphorolysis of pyrimidine 2′-deoxynucleosides, forming 2-deoxyribose-1-phosphate and pyrimidine. 5-Chloro-6-(2-imino-pyrrolidin-1-yl)methyl-uracil hydrochloride (TPI, 1) and its 5-bromo analogue (2), 6-(2-amino-imidazol-1-yl) methyl-5-bromo-uracil (3) and its 5-chloro analogue (4) act as tight-binding stoichiometric inhibitors of recombinant E. coli thymidine phosphorylase, and thus can be used as the first active-site titrants for it using either thymidine or 5-nitro-2′-deoxyuridine as substrate. © 2006 Taylor & Francis.

AB - Thymidine phosphorylase (EC 2.4.2.4) catalyses the reversible phosphorolysis of pyrimidine 2′-deoxynucleosides, forming 2-deoxyribose-1-phosphate and pyrimidine. 5-Chloro-6-(2-imino-pyrrolidin-1-yl)methyl-uracil hydrochloride (TPI, 1) and its 5-bromo analogue (2), 6-(2-amino-imidazol-1-yl) methyl-5-bromo-uracil (3) and its 5-chloro analogue (4) act as tight-binding stoichiometric inhibitors of recombinant E. coli thymidine phosphorylase, and thus can be used as the first active-site titrants for it using either thymidine or 5-nitro-2′-deoxyuridine as substrate. © 2006 Taylor & Francis.

KW - Angiogenesis

KW - Anticancer drugs

KW - Inhibitors

KW - Stoichiometric inhibition

KW - Thymidine phosphorylase

KW - Transition state inhibitor

UR - https://www.scopus.com/pages/publications/33646099832

U2 - 10.1080/14756360500424010

DO - 10.1080/14756360500424010

M3 - Article

SN - 1475-6366

VL - 21

SP - 69

EP - 73

JO - Journal of Enzyme Inhibition and Medicinal Chemistry

JF - Journal of Enzyme Inhibition and Medicinal Chemistry

IS - 1

ER -

Thymidine phosphorylase from Escherichia coli: Tight-binding inhibitors as enzyme active-site titrants

Abstract

Keywords

UN SDGs

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