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Literature summary 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)

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

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.6.3 8-mercaptoguanine
-
 Staphylococcus aureus
2.7.6.3 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

EC Number Metals/Ions Comment Organism Structure
2.7.6.3 Mg2+ required Staphylococcus aureus

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.6.3 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

EC Number Organism UniProt Comment Textmining
2.7.6.3 Staphylococcus aureus
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.6.3 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

EC Number Synonyms Comment Organism
2.7.6.3 6-hydroxymethyl-7,8-dihydropterin pyrophosphokinase
-
 Staphylococcus aureus
2.7.6.3 HPPK
-
 Staphylococcus aureus

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.6.3 ATP
-
 Staphylococcus aureus

General Information

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