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PDBsum entry 2it4

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Lyase PDB id
2it4
Jmol
Contents
Protein chains
256 a.a.
Ligands
PPF
Metals
_ZN ×2
Waters ×344

References listed in PDB file
Key reference
Title Phosph(on)ate as a zinc-Binding group in metalloenzyme inhibitors: X-Ray crystal structure of the antiviral drug foscarnet complexed to human carbonic anhydrase i.
Authors C.Temperini, A.Innocenti, A.Guerri, A.Scozzafava, S.Rusconi, C.T.Supuran.
Ref. Bioorg Med Chem Lett, 2007, 17, 2210-2215. [DOI no: 10.1016/j.bmcl.2007.01.113]
PubMed id 17314045
Abstract
Foscarnet (phosphonoformate trisodium salt), an antiviral used for the treatment of HIV and herpes virus infections, also acts as an activator or inhibitor of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1). Interaction of the drug with 11 CA isozymes has been investigated kinetically, and the X-ray structure of its adduct with isoform I (hCA I-foscarnet complex) has been resolved. The first CA inhibitor possessing a phosphonate zinc-binding group is thus evidenced, together with the factors governing recognition of such small molecules by a metalloenzyme active site. Foscarnet is also a clear-cut example of modulator of an enzyme activity which can act either as an activator or inhibitor of a CA isozyme.
PROCHECK
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