Non-nucleoside inhibitors of human adenosine kinase: synthesis, molecular modeling, and biological studies. (Articolo in rivista)

Type

• Prodotto della ricerca (Classe)
• Articolo in rivista (Classe)

Label

• Non-nucleoside inhibitors of human adenosine kinase: synthesis, molecular modeling, and biological studies. (Articolo in rivista) (literal)

Anno

• 2011-01-01T00:00:00+01:00 (literal)

Alternative label

• Butini S, Gemma S, Brindisi M, Borrelli G, Lossani A, Ponte AM, Torti A, Maga G, Marinelli L, La Pietra V, Fiorini I, Lamponi S, Campiani G, Zisterer DM, Nathwani SM, Sartini S, La Motta C, Da Settimo F, Novellino E, Focher F. (2011)
  Non-nucleoside inhibitors of human adenosine kinase: synthesis, molecular modeling, and biological studies.
  in Journal of medicinal chemistry
  (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori

• Butini S, Gemma S, Brindisi M, Borrelli G, Lossani A, Ponte AM, Torti A, Maga G, Marinelli L, La Pietra V, Fiorini I, Lamponi S, Campiani G, Zisterer DM, Nathwani SM, Sartini S, La Motta C, Da Settimo F, Novellino E, Focher F. (literal)

Pagina inizio

• 1401 (literal)

Pagina fine

• 1420 (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume

• 54 (literal)

Rivista

• Journal of medicinal chemistry (Rivista)

Note

• ISI Web of Science (WOS) (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni

• European Research Centre for Drug Discovery and Development (NatSynDrugs), Universit?a di Siena, 53100 Siena, Italy Dipartimento Farmaco Chimico Tecnologico, Via Aldo Moro, Universit?a di Siena, 53100 Siena, Italy Istituto di Genetica Molecolare, CNR, Via Abbiategrasso 207, 27100 Pavia, Italy School of Biochemistry and Immunology, Trinity College, Dublin 2, Ireland Dipartimento di Scienze Farmaceutiche, Universit?a di Pisa, Via Bonanno, 6, 56126 Pisa, Italy Dipartimento di Chimica Farmaceutica e Tossicologica, Universit?a di Napoli Federico II, Via D. Montesano 49, 80131 Napoli, Italy (literal)

Titolo

• Non-nucleoside inhibitors of human adenosine kinase: synthesis, molecular modeling, and biological studies. (literal)

Abstract

• Adenosine kinase (AK) catalyzes the phosphorylation of adenosine (Ado) to AMP by means of a kinetic mechanism in which the two substrates Ado and ATP bind the enzyme in a binary and/or ternary complex, with distinct protein conformations. Most of the described inhibitors have Ado-like structural motifs and are nonselective, and some of them (e.g., the tubercidine-like ligands) are characterized by a toxic profile. We have cloned and expressed human AK (hAK) and searched for novel non-substrate-like inhibitors. Our efforts to widen the structural diversity of AK inhibitors led to the identification of novel non-nucleoside, noncompetitive allosteric modulators characterized by a unique molecular scaffold. Among the pyrrolobenzoxa(thia)zepinones (4a-qq) developed, 4a was identified as a non-nucleoside prototype hAK inhibitor. 4a has proapoptotic efficacy, slight inhibition of short-term RNA synthesis, and cytostatic activity on tumor cell lines while showing low cytotoxicity and no significant adverse effects on short-term DNA synthesis in cells. (literal)

Prodotto di

• Institute of molecular genetics (IGM) (Istituto)
• Sviluppo e meccanismo d'azione di analoghi nucleotidici e nucleosidici come composti antiproliferativi e antivirali : nuovi composti e nuovi bersagli per la terapia (ME.P04.004.001) (Modulo)

Autore CNR

• GIOVANNI MAGA (Unità di personale interno)
• FEDERICO FOCHER (Unità di personale interno)

Incoming links:

Prodotto

• Institute of molecular genetics (IGM) (Istituto)
• Sviluppo e meccanismo d'azione di analoghi nucleotidici e nucleosidici come composti antiproliferativi e antivirali : nuovi composti e nuovi bersagli per la terapia (ME.P04.004.001) (Modulo)

Autore CNR di

• GIOVANNI MAGA (Unità di personale interno)
• FEDERICO FOCHER (Unità di personale interno)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#rivistaDi

• Journal of medicinal chemistry (Rivista)