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Literature summary for 1.1.1.205 extracted from

  • Singh, V.; Donini, S.; Pacitto, A.; Sala, C.; Hartkoorn, R.; Dhar, N.; Keri, G.; Ascher, D.; Mondesert, G.; Vocat, A.; Lupien, A.; Sommer, R.; Vermet, H.; Lagrange, S.; Buechler, J.; Warner, D.; McKinney, J.; Pato, J.; Cole, S.; Blundell, T.; Rizzi, M.
    The inosine monophosphate dehydrogenase, GuaB2, is a vulnerable new bactericidal drug target for tuberculosis (2017), ACS Infect. Dis., 3, 5-17 .
    View publication on PubMedView publication on EuropePMC
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Crystallization (Commentary)

Crystallization (Comment) Organism
hanging drop vapor diffusion method, using 100 mM sodium acetate, pH 5.5, 200 mM calcium chloride, and 8-14% (v/v) isopropanol Mycobacterium tuberculosis

Protein Variants

Protein Variants Comment Organism
Y487C the mutant is not inhibited by VCC234718 Mycobacterium tuberculosis

Inhibitors

Inhibitors Comment Organism Structure
cyclohexyl[4-(isoquinoline-5-sulfonyl)piperazin-1-yl]methanone uncompetitive inhibition with respect to IMP and NAD+ Mycobacterium tuberculosis
VCC234718 uncompetitive inhibition with respect to IMP and NAD+ Mycobacterium tuberculosis

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
IMP + NAD+ + H2O Mycobacterium tuberculosis
-
 XMP + NADH + H+
-
 ?
IMP + NAD+ + H2O Mycobacterium tuberculosis H37Rv
-
 XMP + NADH + H+
-
 ?

Organism

Organism UniProt Comment Textmining
Mycobacterium tuberculosis
-
-
-
Mycobacterium tuberculosis H37Rv
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Mycobacterium tuberculosis

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
IMP + NAD+ + H2O
-
 Mycobacterium tuberculosis XMP + NADH + H+
-
 ?
IMP + NAD+ + H2O
-
 Mycobacterium tuberculosis H37Rv XMP + NADH + H+
-
 ?

Synonyms

Synonyms Comment Organism
guaB2
-
 Mycobacterium tuberculosis
IMPDH
-
 Mycobacterium tuberculosis
inosine monophosphate dehydrogenase
-
 Mycobacterium tuberculosis

Cofactor

Cofactor Comment Organism Structure
NAD+
-
 Mycobacterium tuberculosis

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0001
-
 cyclohexyl[4-(isoquinoline-5-sulfonyl)piperazin-1-yl]methanone pH and temperature not specified in the publication Mycobacterium tuberculosis
0.0001
-
 VCC234718 pH and temperature not specified in the publication Mycobacterium tuberculosis

General Information

General Information Comment Organism
malfunction enzyme depletion is bactericidal in vitro and ex vivo Mycobacterium tuberculosis
physiological function the enzyme is essential for Mycobacterium tuberculosis to establish an infection in mice Mycobacterium tuberculosis