scholarly journals Synthesis and Evaluation of 6-Aza-2′-deoxyuridine Monophosphate Analogs as Inhibitors of Thymidylate Synthases, and as Substrates or Inhibitors of Thymidine Monophosphate Kinase in Mycobacterium tuberculosis

2012 ◽  
Vol 9 (3) ◽  
pp. 536-556 ◽  
Author(s):  
Martin Kögler ◽  
Roger Busson ◽  
Steven De Jonghe ◽  
Jef Rozenski ◽  
Kristien Van Belle ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Thymidylate Synthases ◽  
Thymidine Monophosphate

Thymidine (monophosphate) analogues as Mycobacterium tuberculosis thymidylate kinase inhibitors

2002 ◽  
Author(s):  
Philippe Van Rompaey ◽  
Vanheusden Veerle ◽  
Sylvie Pochet ◽  
Hélene Munier-Lehmann ◽  
Matheus Froeyen ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Kinase Inhibitors ◽  
Thymidylate Kinase ◽  
Thymidine Monophosphate

scholarly journals Synthesis and inhibitory activity of thymidine analogues targeting Mycobacterium tuberculosis thymidine monophosphate kinase

2011 ◽  
Vol 19 (24) ◽  
pp. 7603-7611 ◽  
Author(s):  
Sara Van Poecke ◽  
Hélène Munier-Lehmann ◽  
Olivier Helynck ◽  
Matheus Froeyen ◽  
Serge Van Calenbergh
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Inhibitory Activity ◽  
Thymidine Monophosphate

scholarly journals Kinetics and Ligand-Binding Preferences of Mycobacterium tuberculosis Thymidylate Synthases, ThyA and ThyX

PLoS ONE ◽  
2008 ◽  
Vol 3 (5) ◽  
pp. e2237 ◽  
Author(s):  
Joshua H. Hunter ◽  
Ramesh Gujjar ◽  
Cullen K. T. Pang ◽  
Pradipsinh K. Rathod
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Ligand Binding ◽  
Thymidylate Synthases

ChemInform Abstract: A New Family of Inhibitors of Mycobacterium tuberculosis Thymidine Monophosphate Kinase.

ChemInform ◽  
2008 ◽  
Vol 39 (12) ◽  
Author(s):  
C. Gasse ◽  
V. Huteau ◽  
D. Douguet ◽  
H. Munier-Lehmann ◽  
S. Pochet
Keyword(s):  
Mycobacterium Tuberculosis ◽  
New Family ◽  
Thymidine Monophosphate

Quantitative structure–activity relationships and design of thymine-like inhibitors of thymidine monophosphate kinase of Mycobacterium tuberculosis with favourable pharmacokinetic profiles

RSC Advances ◽  
2014 ◽  
Vol 4 (99) ◽  
pp. 55853-55866 ◽  
Author(s):  
M. Keita ◽  
A. Kumar ◽  
B. Dali ◽  
E. Megnassan ◽  
M. I. Siddiqi ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Molecular Design ◽  
Quantitative Structure ◽  
Structure Activity Relationships ◽  
Pharmacokinetic Profiles ◽  
Structure Activity ◽  
Thymidine Monophosphate ◽  
Quantitative Structure Activity Relationships

We have designed new potent inhibitors of thymidine monophosphate kinase of Mycobacterium tuberculosis (TMPKmt) using structure-based molecular design.

scholarly journals Crystal structure of the flavin-dependent thymidylate synthase Thy1 from Thermus thermophilus with an extra C-terminal domain

2019 ◽  
Vol 75 (6) ◽  
pp. 450-454
Author(s):  
Aoba Ogawa ◽  
Gen-ichi Sampei ◽  
Gota Kawai
Keyword(s):  
Crystal Structure ◽  
Characteristic Feature ◽  
Thymidylate Synthase ◽  
Thermus Thermophilus ◽  
Catalytic Reactions ◽  
Database Analysis ◽  
Terminal Domain ◽  
Thymidylate Synthases ◽  
Phosphate Ions ◽  
Thymidine Monophosphate

The thymidylate synthases ThyA and Thy1 are enzymes that catalyse the formation of thymidine monophosphate from 2′-deoxyuridine monophosphate. Thy1 (or ThyX) requires flavin for catalytic reactions, while ThyA does not. In the present study, the crystal structure of the flavin-dependent thymidylate synthase Thy1 from Thermus thermophilus HB8 (TtThy1, TTHA1096) was determined in complex with FAD and phosphate at 2.5 Å resolution. TtThy1 is a tetrameric molecule like other Thy1 proteins, to which four FAD molecules are bound. In the crystal of TtThy1, two phosphate ions were bound to each dUMP-binding site. The characteristic feature of TtThy1 is the existence of an extra C-terminal domain (CTD) consisting of three α-helices and a β-strand. The function of the CTD is unknown and database analysis showed that this CTD is only shared by part of the Deinococcus–Thermus phylum.

Design of Mycobacterium tuberculosis Thymidine Monophosphate Kinase Inhibitors

ChemInform ◽  
2004 ◽  
Vol 35 (4) ◽  
Author(s):  
H. Munier-Lehmann ◽  
S. Pochet ◽  
L. Dugue ◽  
O. Dutruel ◽  
G. Labesse ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Kinase Inhibitors ◽  
Thymidine Monophosphate
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