The cytosolic isoform XIII is a recently discovered member of the human carbonic anhydrase (hCA, EC 4.2.1.1) family. It is selectively expressed among other tissues in the reproductive organs, where it may control pH and ion balance regulation, ensuring thus proper fertilization conditions. The authors report here the X-ray crystallographic structure of this isozyme in the unbound state and in complex with a classical sulfonamide inhibitor, namely acetazolamide. A detailed comparison of the obtained structural data with those already reported for other CA isozymes provides novel insights into the catalytic properties of the members of this protein family. On the basis of the inhibitory properties of acetazolamide against various cytosolic/transmembrane isoforms and the structural differences detected within the active site of the various CA isoforms, further prospects for the design of isozyme-specific CA inhibitors are here proposed.

Crystal structure of human carbonic anhydrase XIII and its complex with the inhibitor acetazolamide / Di Fiore, A; Monti, Sm; Hilvo, M; Parkkila, S; Romano, V; Scaloni, A; Pedone, Carlo; Scozzafava, A; Supuran, Ct; De Simone, G.. - In: PROTEINS. - ISSN 0887-3585. - STAMPA. - 74:1(2009), pp. 164-175.

Crystal structure of human carbonic anhydrase XIII and its complex with the inhibitor acetazolamide.

PEDONE, CARLO;
2009

Abstract

The cytosolic isoform XIII is a recently discovered member of the human carbonic anhydrase (hCA, EC 4.2.1.1) family. It is selectively expressed among other tissues in the reproductive organs, where it may control pH and ion balance regulation, ensuring thus proper fertilization conditions. The authors report here the X-ray crystallographic structure of this isozyme in the unbound state and in complex with a classical sulfonamide inhibitor, namely acetazolamide. A detailed comparison of the obtained structural data with those already reported for other CA isozymes provides novel insights into the catalytic properties of the members of this protein family. On the basis of the inhibitory properties of acetazolamide against various cytosolic/transmembrane isoforms and the structural differences detected within the active site of the various CA isoforms, further prospects for the design of isozyme-specific CA inhibitors are here proposed.
2009
Crystal structure of human carbonic anhydrase XIII and its complex with the inhibitor acetazolamide / Di Fiore, A; Monti, Sm; Hilvo, M; Parkkila, S; Romano, V; Scaloni, A; Pedone, Carlo; Scozzafava, A; Supuran, Ct; De Simone, G.. - In: PROTEINS. - ISSN 0887-3585. - STAMPA. - 74:1(2009), pp. 164-175.
File in questo prodotto:
Non ci sono file associati a questo prodotto.

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11588/348329
Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus ND
  • ???jsp.display-item.citation.isi??? ND
social impact