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Literature summary extracted from

  • Dinesh, N.; Pallerla, D.S.R.; Kaur, P.K.; Babu, N.K.; Singh, S.
    Exploring Leishmania donovani 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMGR) as a potential drug target by biochemical, biophysical and inhibition studies (2014), Microb. Pathog., 66, 14-23.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.1.1.34 gene HMGR, DNA and amino acid sequence determination and analysis, sequence comparisons, recombinant expression of His-tagged enzyme in Escherichia coli strain BL21(DE3) Leishmania donovani

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.34 atorvastatin inhibits the cell growth as well as the activity of recombinant enzyme, 315.5 nM are enough to cause 50% recombinant LdHMGR enzyme inhibition, 93.2% inhibition at 0.001 mM Leishmania donovani
1.1.1.34 additional information exogenous supplementation of ergosterol in case of atorvastatin and resveratrol treated cells causes complete reversal of growth inhibition whereas simvastatin is ergosterol refractory Leishmania donovani
1.1.1.34 resveratrol inhibits the cell growth as well as the activity of recombinant enzyme. Resveratrol shows antitrypanosomal activity with an IC50 value of 0.00013 mM and moderate antipromastigote activity against Leishmania major with IC50 value: 0.153 mM Leishmania donovani
1.1.1.34 simvastatin inhibits the cell growth as well as the activity of recombinant enzyme, 63% inhibition at 0.1 mM Leishmania donovani

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.1.1.34 additional information
-
 additional information kinetic analysis Leishmania donovani
1.1.1.34 0.0357
-
 (R,S)-3-hydroxy-3-methylglutaryl-CoA pH 7.2, 37°C Leishmania donovani
1.1.1.34 0.07
-
 NADPH pH 7.2, 37°C Leishmania donovani

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
1.1.1.34 45000
-
-
 Leishmania donovani

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.1.1.34 (R)-mevalonate + CoA + 2 NADP+ Leishmania donovani
-
 (S)-3-hydroxy-3-methylglutaryl-CoA + 2 NADPH + 2 H+
-
 r
1.1.1.34 (R)-mevalonate + CoA + 2 NADP+ Leishmania donovani MHOM/80/IN/Dd8
-
 (S)-3-hydroxy-3-methylglutaryl-CoA + 2 NADPH + 2 H+
-
 r

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.34 Leishmania donovani I7CKJ5
-
-
1.1.1.34 Leishmania donovani MHOM/80/IN/Dd8 I7CKJ5
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
1.1.1.34 recombinant His-tagged enzyme from Escherichia coli strain BL21(DE3) by nickel affinity chromatography Leishmania donovani

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.1.1.34 cell culture
-
 Leishmania donovani
-
1.1.1.34 promastigote
-
 Leishmania donovani
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.34 (R)-mevalonate + CoA + 2 NADP+
-
 Leishmania donovani (S)-3-hydroxy-3-methylglutaryl-CoA + 2 NADPH + 2 H+
-
 r
1.1.1.34 (R)-mevalonate + CoA + 2 NADP+
-
 Leishmania donovani MHOM/80/IN/Dd8 (S)-3-hydroxy-3-methylglutaryl-CoA + 2 NADPH + 2 H+
-
 r
1.1.1.34 (R,S)-3-hydroxy-3-methylglutaryl-CoA + 2 NADPH + 2 H+
-
 Leishmania donovani (R)-mevalonate + CoA + 2 NADP+
-
 r
1.1.1.34 (R,S)-3-hydroxy-3-methylglutaryl-CoA + 2 NADPH + 2 H+
-
 Leishmania donovani MHOM/80/IN/Dd8 (R)-mevalonate + CoA + 2 NADP+
-
 r

Subunits

EC Number Subunits Comment Organism
1.1.1.34 ? x * 45000, sequence calculation Leishmania donovani
1.1.1.34 More the secondary structure of LdHMGR confirms the presence of 25.7% alpha helicity Leishmania donovani

Synonyms

EC Number Synonyms Comment Organism
1.1.1.34 3-hydroxy-3-methylglutaryl coenzyme A reductase
-
 Leishmania donovani
1.1.1.34 HMG-CoA reductase
-
 Leishmania donovani
1.1.1.34 HMGR
-
 Leishmania donovani

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
1.1.1.34 37
-
-
 Leishmania donovani

Temperature Range [°C]

EC Number Temperature Minimum [°C] Temperature Maximum [°C] Comment Organism
1.1.1.34 15 55 19% of maximal activity at 15°C and 29% at 55°C Leishmania donovani

Temperature Stability [°C]

EC Number Temperature Stability Minimum [°C] Temperature Stability Maximum [°C] Comment Organism
1.1.1.34 90
-
 the enzyme retains 60% helical structure Leishmania donovani

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
1.1.1.34 7.2
-
-
 Leishmania donovani

pH Range

EC Number pH Minimum pH Maximum Comment Organism
1.1.1.34 5.5 10 19% of maximal activity at pH 5.5 and 29% at pH 10.0 Leishmania donovani

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.1.34 NADP+
-
 Leishmania donovani
1.1.1.34 NADPH dependent on Leishmania donovani

pI Value

EC Number Organism Comment pI Value Maximum pI Value
1.1.1.34 Leishmania donovani sequence calculation
-
 7.4

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.1.1.34 0.0194
-
 pH 7.2, 37°C Leishmania donovani atorvastatin
1.1.1.34 0.0732
-
 pH 7.2, 37°C Leishmania donovani simvastatin

General Information

EC Number General Information Comment Organism
1.1.1.34 metabolism rate limiting enzyme of the ergosterol biosynthetic pathway Leishmania donovani