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Literature summary for 2.7.6.3 extracted from

  • Dennis, M.L.; Chhabra, S.; Wang, Z.C.; Debono, A.; Dolezal, O.; Newman, J.; Pitcher, N.P.; Rahmani, R.; Cleary, B.; Barlow, N.; Hattarki, M.; Graham, B.; Peat, T.S.; Baell, J.B.; Swarbrick, J.D.
    Structure-based design and development of functionalized mercaptoguanine derivatives as inhibitors of the folate biosynthesis pathway enzyme 6-hydroxymethyl-7,8-dihydropterin pyrophosphokinase from Staphylococcus aureus (2014), J. Med. Chem., 57, 9612-9626.
    View publication on PubMed

Crystallization (Commentary)

Crystallization (Comment) Organism
X-ray diffraction crystal structure analysis of both the SaHPPK/inhibitor/cofactor analogue ternary and the SaHPPK/cofactor analogue binary complexes Staphylococcus aureus

Inhibitors

Inhibitors Comment Organism Structure
8-mercaptoguanine
-
Staphylococcus aureus
additional information structure-based design and development of functionalized mercaptoguanine derivatives as inhibitors of the folate biosynthesis pathway enzyme 6-hydroxymethyl-7,8-dihydropterin diphosphokinase from Staphylococcus aureus, binding of an S8-functionalized derivative of 8-mercaptoguanine, overview. Synthesis and binding analysis of a set of analogues including a compound displaying over 20fold higher affinity for SaHPPK than 8-mercaptoguanine. A number of the compounds exhibit low micromolar affinity for dihydropteroate synthase (DHPS, EC 2.5.1.15), the adjacent, downstream enzyme to HPPK, and may thus represent bienzyme inhibitors Staphylococcus aureus

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ required Staphylococcus aureus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + 2-amino-4-hydroxy-6-hydroxymethyl-7,8-dihydropteridine Staphylococcus aureus
-
AMP + (2-amino-4-hydroxy-7,8-dihydropteridin-6-yl)methyl diphosphate
-
?

Organism

Organism UniProt Comment Textmining
Staphylococcus aureus
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + 2-amino-4-hydroxy-6-hydroxymethyl-7,8-dihydropteridine
-
Staphylococcus aureus AMP + (2-amino-4-hydroxy-7,8-dihydropteridin-6-yl)methyl diphosphate
-
?

Synonyms

Synonyms Comment Organism
6-hydroxymethyl-7,8-dihydropterin pyrophosphokinase
-
Staphylococcus aureus
HPPK
-
Staphylococcus aureus

Cofactor

Cofactor Comment Organism Structure
ATP
-
Staphylococcus aureus

General Information

General Information Comment Organism
metabolism the enzyme is involved in the folate biosynthesis pathway catalyzing the diphosphoryl transfer from ATP to 6-hydroxymethyl-7,8-dihydropterin Staphylococcus aureus