http://www.cnr.it/ontology/cnr/individuo/prodotto/ID17470

Peptidyl fluoro-ketones as proteolytic enzyme inhibitors (Articolo in rivista)

Type

Label

Peptidyl fluoro-ketones as proteolytic enzyme inhibitors (Articolo in rivista) (literal)

Anno

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Alternative label

Sani M., Sinisi R., Viani F. (2006)
Peptidyl fluoro-ketones as proteolytic enzyme inhibitors
in Current topics in medicinal chemistry (Print); Bentham science publishers, Sharjah (Emirati Arabi Uniti)
(literal)

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Pagina inizio

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http://sfx.biblio.polimi.it:3210/sfx_local?sid=Elsevier:Scopus&_service_type=getFullTxt&issn=15680266&isbn=&volume=6&issue=14&spage=1545&epage=1566&pages=1545-1566&artnum=&date=2006&id=doi:10.2174%2f156802606777951064&title=Current+Topics+in+Medicinal+Chemistry&atitle=Peptidyl+fluoro-ketones+as+proteolytic+enzyme+inhibitors&aufirst=M.&auinit=M.&auinit1=M&aulast=Sani (literal)

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Note

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Dipartimento di Chimica, Materiali ed Ingegneria Chimica \"G. Natta\" del Politecnico di Milano and C.N.R. - Istituto di Chimica del Riconoscimento Molecolare, Sezione \"A.Quilico\", via Mancinelli 7, I-20131 Milano, Italy (literal)

Titolo

Abstract

Proteolytic enzymes are involved in many important physiological processes. Because of the critical roles played by these enzymes, aberrations in regulation of their activities can lead to pathological conditions. For this reason, finding inhibitors selective for a proteolytic enzyme that is contributing to a medical problem can be an effective therapeutic strategy. The introduction of fluorine in the backbone of proteolytic enzyme substrates can lead to active and selective inhibitors belonging to the peptidyl fluorinated ketone family. Fluorine not only can influence the mechanism of substrate/enzyme recognition events but also can modify the in vivo profile of the substrate. Although prediction of the total effects of fluorine on the pharmacokinetic parameters can be difficult, the pharmaceutical interest in the synthesis and biological evaluation of peptidyl fluorinated ketones highlights the potential of this family of molecules as therapeutically useful inhibitors (literal)

Editore