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Literature summary extracted from

  • Chan, H.C.; Feng, X.; Ko, T.P.; Huang, C.H.; Hu, Y.; Zheng, Y.; Bogue, S.; Nakano, C.; Hoshino, T.; Zhang, L.; Lv, P.; Liu, W.; Crick, D.C.; Liang, P.H.; Wang, A.H.; Oldfield, E.; Guo, R.T.
    Structure and inhibition of tuberculosinol synthase and decaprenyl diphosphate synthase from Mycobacterium tuberculosis (2014), J. Am. Chem. Soc., 136, 2892-2896.
    View publication on PubMedView publication on EuropePMC

Application

EC Number Application Comment Organism
2.5.1.86 drug development the enzyme is a target for development of specific inhibitors for anti-infective therapies that block virulence factor formation, the enzyme is a target in treatment of tuberculosis Mycobacterium tuberculosis

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.5.1.86 gene Rv2361c, recombinant expression Mycobacterium tuberculosis

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
2.5.1.86 in complex with BPH-640, hanging drop vapor diffusion method, using Mycobacterium tuberculosis
2.5.1.86 purified recombinant enzyme in complex with inhibitor BPH-640, X-ray diffraction structure determination and analysis at 1.8-1.9 A resolution Mycobacterium tuberculosis
2.5.1.153 native enzyme and complexes with inhibitor BPH-629, and mutants Y51F with TPP, mutant Y51F/Y90F with TPP, to 1.8-2.7 A resolution Mycobacterium tuberculosis

Protein Variants

EC Number Protein Variants Comment Organism
2.5.1.153 D34A compared to wild-type, mutant produces about 1% (13S)-isotuberculosinol and 60% tuberculosinol Mycobacterium tuberculosis
2.5.1.153 R38A compared to wild-type, mutant produces about 5% (13S)-isotuberculosinol and 140% tuberculosinol Mycobacterium tuberculosis
2.5.1.153 Y51F production of both (13S)-isotuberculosinol and tuberculosinol is reduced Mycobacterium tuberculosis
2.5.1.153 Y51F/Y90F no enzymic activity Mycobacterium tuberculosis
2.5.1.153 Y90F compared to wild-type, mutant produces about 1% (13S)-isotuberculosinol and 49% tuberculosinol Mycobacterium tuberculosis

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.5.1.86 BPH-640 a bisphosphonate inhibitor, three-dimensional structure from crystal structure, dimeric DPPS structure with one bound BPH-640 molecule in each monomer, overview. BPH-640 occupies a dimer interface binding site, sandwiched between residues G77, N78, G79, R80, T83, R89, and R127 of monomer A and residues R292 and F293 of monomer B Mycobacterium tuberculosis

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
2.5.1.86 cell wall
-
Mycobacterium tuberculosis 5618
-

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.5.1.86 Mg2+ required Mycobacterium tuberculosis

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.5.1.86 (2Z,6E)-farnesyl diphosphate + 7 isopentenyl diphosphate Mycobacterium tuberculosis
-
7 diphosphate + trans,octacis-decaprenyl diphosphate
-
?
2.5.1.86 (2Z,6E)-farnesyl diphosphate + 7 isopentenyl diphosphate Mycobacterium tuberculosis H37Rv
-
7 diphosphate + trans,octacis-decaprenyl diphosphate
-
?
2.5.1.86 (2Z,6E)-farnesyl diphosphate + isopentenyl diphosphate Mycobacterium tuberculosis
-
diphosphate + trans,octacis-decaprenyl diphosphate
-
?
2.5.1.86 (2Z,6E)-farnesyl diphosphate + isopentenyl diphosphate Mycobacterium tuberculosis H37Rv
-
diphosphate + trans,octacis-decaprenyl diphosphate
-
?

Organism

EC Number Organism UniProt Comment Textmining
2.5.1.86 Mycobacterium tuberculosis P9WFF7
-
-
2.5.1.86 Mycobacterium tuberculosis P9WFF7 gene Rv2361c
-
2.5.1.86 Mycobacterium tuberculosis H37Rv P9WFF7
-
-
2.5.1.153 Mycobacterium tuberculosis P9WJ61 bifunctional tuberculosinol/iso-tuberculosinol synthase, ECs 3.1.7.8 and 3.1.7.9
-
2.5.1.153 Mycobacterium tuberculosis ATCC 25618 P9WJ61 bifunctional tuberculosinol/iso-tuberculosinol synthase, ECs 3.1.7.8 and 3.1.7.9
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.5.1.86 (2Z,6E)-farnesyl diphosphate + 7 isopentenyl diphosphate
-
Mycobacterium tuberculosis 7 diphosphate + trans,octacis-decaprenyl diphosphate
-
?
2.5.1.86 (2Z,6E)-farnesyl diphosphate + 7 isopentenyl diphosphate the enzyme is a cis-prenyl transferase Mycobacterium tuberculosis 7 diphosphate + trans,octacis-decaprenyl diphosphate
-
?
2.5.1.86 (2Z,6E)-farnesyl diphosphate + 7 isopentenyl diphosphate
-
Mycobacterium tuberculosis H37Rv 7 diphosphate + trans,octacis-decaprenyl diphosphate
-
?
2.5.1.86 (2Z,6E)-farnesyl diphosphate + 7 isopentenyl diphosphate the enzyme is a cis-prenyl transferase Mycobacterium tuberculosis H37Rv 7 diphosphate + trans,octacis-decaprenyl diphosphate
-
?
2.5.1.86 (2Z,6E)-farnesyl diphosphate + isopentenyl diphosphate
-
Mycobacterium tuberculosis diphosphate + trans,octacis-decaprenyl diphosphate
-
?
2.5.1.86 (2Z,6E)-farnesyl diphosphate + isopentenyl diphosphate
-
Mycobacterium tuberculosis H37Rv diphosphate + trans,octacis-decaprenyl diphosphate
-
?
2.5.1.153 tuberculosinyl diphosphate + H2O
-
Mycobacterium tuberculosis tuberculosinol + diphosphate reaction of EC 3.1.7.8. Wild-type synthesizes 41% (13S)-isotuberculosinol and 59% tuberculosinol ?
2.5.1.153 tuberculosinyl diphosphate + H2O wild-type synthesizes 41% (13S)-isotuberculosinol and 59% tuberculosinol Mycobacterium tuberculosis tuberculosinol + diphosphate
-
?
2.5.1.153 tuberculosinyl diphosphate + H2O
-
Mycobacterium tuberculosis ATCC 25618 tuberculosinol + diphosphate reaction of EC 3.1.7.8. Wild-type synthesizes 41% (13S)-isotuberculosinol and 59% tuberculosinol ?
2.5.1.153 tuberculosinyl diphosphate + H2O wild-type synthesizes 41% (13S)-isotuberculosinol and 59% tuberculosinol Mycobacterium tuberculosis ATCC 25618 tuberculosinol + diphosphate
-
?
2.5.1.153 tuberculosinyl diphosphate + H2O
-
Mycobacterium tuberculosis (13S)-isotuberculosinol + diphosphate wild-type synthesizes 41% (13S)-isotuberculosinol and 59% tuberculosinol ?
2.5.1.153 tuberculosinyl diphosphate + H2O
-
Mycobacterium tuberculosis (13S)-isotuberculosinol + diphosphate reaction of EC 3.1.7.9. Wild-type synthesizes 41% (13S)-isotuberculosinol and 59% tuberculosinol ?
2.5.1.153 tuberculosinyl diphosphate + H2O
-
Mycobacterium tuberculosis ATCC 25618 (13S)-isotuberculosinol + diphosphate wild-type synthesizes 41% (13S)-isotuberculosinol and 59% tuberculosinol ?
2.5.1.153 tuberculosinyl diphosphate + H2O
-
Mycobacterium tuberculosis ATCC 25618 (13S)-isotuberculosinol + diphosphate reaction of EC 3.1.7.9. Wild-type synthesizes 41% (13S)-isotuberculosinol and 59% tuberculosinol ?

Subunits

EC Number Subunits Comment Organism
2.5.1.86 dimer
-
Mycobacterium tuberculosis

Synonyms

EC Number Synonyms Comment Organism
2.5.1.86 cis-decaprenyl diphosphate synthase
-
Mycobacterium tuberculosis
2.5.1.86 decaprenyl diphosphate synthase
-
Mycobacterium tuberculosis
2.5.1.86 DPPS
-
Mycobacterium tuberculosis
2.5.1.86 Rv2361c
-
Mycobacterium tuberculosis
2.5.1.153 Rv3378c
-
Mycobacterium tuberculosis

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.5.1.86 0.00041
-
pH and temperature not specified in the publication Mycobacterium tuberculosis BPH-640

General Information

EC Number General Information Comment Organism
2.5.1.86 physiological function the enzyme is involved in cell wall biosynthesis Mycobacterium tuberculosis