Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 1.5.1.33 extracted from

  • McLuskey, K.; Gibellini, F.; Carvalho, P.; Avery, M.A.; Hunter, W.N.
    Inhibition of Leishmania major pteridine reductase by 2,4,6-triaminoquinazoline: structure of the NADPH ternary complex (2004), Acta Crystallogr. Sect. D, 60, 1780-1785.
    View publication on PubMed

Application

Application Comment Organism
medicine enzyme is a target for development of improved therapies for infection by trypanosomatid parasites Leishmania major

Crystallization (Commentary)

Crystallization (Comment) Organism
enzyme in ternary complex with NADPH and inhibitor 2,4,6-triaminoquinazoline in protein solution containing 10 mg/ml protein, 20 mM sodium acetate, pH 5.3, 1 mM NADPH, 1 mM 2,4,6-triaminoquinazoline, 20 mM DTT, and 1% DMSO, hanging drop vapour diffusion method, against equal volume of 0.002 ml of reservoir solution containing 11-14% PEG 5000, 100 mM sodium acetate, pH 5.5, and 40-140 mM calcium acetate, 20°C, thin grew clumps of thin fragile rods, cryopreservation in a solution of 0% reservoir solution and 30% glycerol, X-ray diffraction structure determination and analysis at 2.6 A resolution, molecular replacement Leishmania major

Inhibitors

Inhibitors Comment Organism Structure
2,4,6-triaminoquinazoline i.e. TAQ, mimics the pterin head group of methotrexate, binds to the active site, binding structure and inhibition mechanism Leishmania major
methotrexate antifolate drug Leishmania major
additional information structure-based inhibitor development Leishmania major

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
25700
-
4 * 25700, crystal structure Leishmania major

Organism

Organism UniProt Comment Textmining
Leishmania major Q01782
-
-

Subunits

Subunits Comment Organism
tetramer 4 * 25700, crystal structure Leishmania major

Cofactor

Cofactor Comment Organism Structure
NADPH dependent on Leishmania major