Pubblicazioni

Pyridoxal 5'-Phosphate Enzymes as Targets for Therapeutic Agents  (2007)

Autori:
A. Amadasi; M. Bertoldi; R. Contestabile S. Bettati; B. Cellini; M.L. di Salvo; C. Borri-Voltattorni; F. Bossa; A. Mozzarelli
Titolo:
Pyridoxal 5'-Phosphate Enzymes as Targets for Therapeutic Agents
Anno:
2007
Tipologia prodotto:
Articolo in Rivista
Tipologia ANVUR:
Articolo su rivista
Nazioni degli autori:
ITALIA
Lingua:
Inglese
Formato:
A Stampa
Referee:
Nome rivista:
Current Medicinal Chemistry
ISSN Rivista:
0929-8673
N° Volume:
14
Editore:
Bentham Science Publishers
Intervallo pagine:
1291-1324
Parole chiave:
vitamin B6-enzymes, drug design, pyridoxal 5'-phosphate, inhibitors, functional genomics
Breve descrizione dei contenuti:
The vitamin B6-derived pyridoxal 5'-phosphate (PLP) is the cofactor of enzymes catalyzing a large variety of chemical reactions mainly involved in amino acid metabolism. These enzymes have been divided in five families and fold types on the basis of evolutionary relationships and protein structural organization. Almost 1.5% of all genes in prokaryotes code for PLP-dependent enzymes, whereas the percentage is substantially lower in eukaryotes. Although about 4% of enzyme-catalyzed reactions catalogued by the Enzyme Commission are PLP-dependent, only a few enzymes are targets of approved drugs and about twenty are recognised as potential targets for drugs or herbicides. PLP-dependent enzymes for which there are already commercially available drugs are DOPA decarboxylase (involved in the Parkinson disease), GABA aminotransferase (epilepsy), serine hydroxymethyltransferase (tumors and malaria), ornithine decarboxylase (African sleeping sickness and, potentially, tumors), alanine racemase (antibacterial agents), and human cytosolic branched-chain aminotransferase (pathological states associated to the GABA/glutamate equilibrium concentrations). Within each family or metabolic pathway, the enzymes for which drugs have been already approved for clinical use are discussed first, reporting the enzyme structure, the catalytic mechanism, the mechanism of enzyme inactivation or modulation by substrate-like or transition state-like drugs, and on-going research for increasing specificity and decreasing side-effects. Then, PLP-dependent enzymes that have been recently characterized and proposed as drug targets are reported. Finally, the relevance of recent genomic analysis of PLP-dependent enzymes for the selection of drug targets is discussed.
Id prodotto:
37624
Handle IRIS:
11562/308398
depositato il:
29 marzo 2012
ultima modifica:
2 novembre 2016
Citazione bibliografica:
A. Amadasi; M. Bertoldi; R. Contestabile S. Bettati; B. Cellini; M.L. di Salvo; C. Borri-Voltattorni; F. Bossa; A. Mozzarelli, Pyridoxal 5'-Phosphate Enzymes as Targets for Therapeutic Agents «Current Medicinal Chemistry» , vol. 142007pp. 1291-1324

Consulta la scheda completa presente nel repository istituzionale della Ricerca di Ateneo IRIS

Progetti Collegati
Titolo Dipartimento Responsabili
<<indietro

Attività

Strutture