Peptidomimetics containing a vinyl ketone warhead as falcipain-2 inhibitors

Publikationstyp:
Zeitschriftenaufsatz
Metadaten:
Autoren
  • Roberta Ettari
  • Maria Zappala
  • Nicola Micale
  • Giovanni Grazioso
  • Salvatore Giofre
  • Tanja Schirmeister
  • Silvana Grasso
Autoren-URL
https://www.webofscience.com/api/gateway?GWVersion=2&SrcApp=fis-test-1&SrcAuth=WosAPI&KeyUT=WOS:000291118600013&DestLinkType=FullRecord&DestApp=WOS_CPL
DOI
10.1016/j.ejmech.2011.02.058
eISSN
1768-3254
Externe Identifier
  • Clarivate Analytics Document Solution ID: 770WG
  • PubMed Identifier: 21420760
ISSN
0223-5234
Ausgabe der Veröffentlichung
6
Zeitschrift
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Schlüsselwörter
  • Peptidomimetics
  • Falcipain-2 inhibitors
  • Cysteine proteases
  • Docking studies
Paginierung
2058 - 2065
Datum der Veröffentlichung
2011
Status
Published
Titel
Peptidomimetics containing a vinyl ketone warhead as falcipain-2 inhibitors
Sub types
  • Article
Ausgabe der Zeitschrift
46

Datenquelle: Web of Science (Lite)

Andere Metadatenquellen:
Autoren
  • Roberta Ettari
  • Maria Zappalà
  • Nicola Micale
  • Giovanni Grazioso
  • Salvatore Giofrè
  • Tanja Schirmeister
  • Silvana Grasso
DOI
10.1016/j.ejmech.2011.02.058
ISSN
0223-5234
Ausgabe der Veröffentlichung
6
Zeitschrift
European Journal of Medicinal Chemistry
Sprache
en
Paginierung
2058 - 2065
Datum der Veröffentlichung
2011
Status
Published
Herausgeber
Elsevier BV
Herausgeber URL
http://dx.doi.org/10.1016/j.ejmech.2011.02.058
Datum der Datenerfassung
2018
Titel
Peptidomimetics containing a vinyl ketone warhead as falcipain-2 inhibitors
Ausgabe der Zeitschrift
46

Datenquelle: Crossref

Abstract
The design, chemical synthesis, and enzymatic activity evaluation of a set of falcipain-2 inhibitors are reported. These compounds contain a proven peptidomimetic recognition motif based on a benzo[1,4]diazepin-2-one (1,4-BDZ) framework built on a dipeptide sequence, and a Michael acceptor terminal moiety capable of deactivating the cysteine protease active site. Our goal is to modify the P(3) site of this motif in order to identify the structural requirements for the interaction with the target.
Addresses
  • Dipartimento Farmaco-Chimico, University of Messina, Viale Annunziata, 98168 Messina, Italy. rettari@pharma.unime.it
Autoren
  • Roberta Ettari
  • Maria Zappalà
  • Nicola Micale
  • Giovanni Grazioso
  • Salvatore Giofrè
  • Tanja Schirmeister
  • Silvana Grasso
DOI
10.1016/j.ejmech.2011.02.058
eISSN
1768-3254
Externe Identifier
  • PubMed Identifier: 21420760
Funding acknowledgements
  • German Research Society:
Open access
false
ISSN
0223-5234
Ausgabe der Veröffentlichung
6
Zeitschrift
European journal of medicinal chemistry
Schlüsselwörter
  • Humans
  • Benzodiazepinones
  • Cysteine Endopeptidases
  • Cysteine Proteinase Inhibitors
  • Enzyme Activation
  • Molecular Structure
  • Structure-Activity Relationship
  • Drug Design
  • Stereoisomerism
  • Models, Molecular
  • Peptidomimetics
Sprache
eng
Medium
Print-Electronic
Online publication date
2011
Paginierung
2058 - 2065
Datum der Veröffentlichung
2011
Status
Published
Datum der Datenerfassung
2011
Titel
Peptidomimetics containing a vinyl ketone warhead as falcipain-2 inhibitors.
Sub types
  • Research Support, Non-U.S. Gov't
  • Journal Article
Ausgabe der Zeitschrift
46

Datenquelle: Europe PubMed Central

Abstract
The design, chemical synthesis, and enzymatic activity evaluation of a set of falcipain-2 inhibitors are reported. These compounds contain a proven peptidomimetic recognition motif based on a benzo[1,4]diazepin-2-one (1,4-BDZ) framework built on a dipeptide sequence, and a Michael acceptor terminal moiety capable of deactivating the cysteine protease active site. Our goal is to modify the P(3) site of this motif in order to identify the structural requirements for the interaction with the target.
Date of acceptance
2011
Autoren
  • Roberta Ettari
  • Maria Zappalà
  • Nicola Micale
  • Giovanni Grazioso
  • Salvatore Giofrè
  • Tanja Schirmeister
  • Silvana Grasso
Autoren-URL
https://www.ncbi.nlm.nih.gov/pubmed/21420760
DOI
10.1016/j.ejmech.2011.02.058
eISSN
1768-3254
Ausgabe der Veröffentlichung
6
Zeitschrift
Eur J Med Chem
Schlüsselwörter
  • Benzodiazepinones
  • Cysteine Endopeptidases
  • Cysteine Proteinase Inhibitors
  • Drug Design
  • Enzyme Activation
  • Humans
  • Models, Molecular
  • Molecular Structure
  • Peptidomimetics
  • Stereoisomerism
  • Structure-Activity Relationship
Sprache
eng
Country
France
Paginierung
2058 - 2065
PII
S0223-5234(11)00186-3
Datum der Veröffentlichung
2011
Status
Published
Datum, an dem der Datensatz öffentlich gemacht wurde
2011
Titel
Peptidomimetics containing a vinyl ketone warhead as falcipain-2 inhibitors.
Sub types
  • Journal Article
  • Research Support, Non-U.S. Gov't
Ausgabe der Zeitschrift
46

Datenquelle: PubMed

Beziehungen:
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