New Tetromycin Derivatives with Anti-Trypanosomal and Protease Inhibitory Activities
- Publikationstyp:
- Zeitschriftenaufsatz
- Metadaten:
-
- Autoren
- Sheila M Pimentel-Elardo
- Verena Buback
- Tobias AM Gulder
- Tim S Bugni
- Jason Reppart
- Gerhard Bringmann
- Chris M Ireland
- Tanja Schirmeister
- Ute Hentschel
- Autoren-URL
- https://www.webofscience.com/api/gateway?GWVersion=2&SrcApp=fis-test-1&SrcAuth=WosAPI&KeyUT=WOS:000298928300001&DestLinkType=FullRecord&DestApp=WOS_CPL
- DOI
- 10.3390/md9101682
- eISSN
- 1660-3397
- Externe Identifier
- Clarivate Analytics Document Solution ID: 874AV
- PubMed Identifier: 22072992
- Ausgabe der Veröffentlichung
- 10
- Zeitschrift
- MARINE DRUGS
- Schlüsselwörter
- tetromycin
- anti-trypanosomal
- protease inhibition
- Streptomyces axinellae
- marine sponge
- Paginierung
- 1682 - 1697
- Datum der Veröffentlichung
- 2011
- Status
- Published
- Titel
- New Tetromycin Derivatives with Anti-Trypanosomal and Protease Inhibitory Activities
- Sub types
- Article
- Ausgabe der Zeitschrift
- 9
Datenquelle: Web of Science (Lite)
- Andere Metadatenquellen:
-
- Autoren
- Sheila M Pimentel-Elardo
- Verena Buback
- Tobias AM Gulder
- Tim S Bugni
- Jason Reppart
- Gerhard Bringmann
- Chris M Ireland
- Tanja Schirmeister
- Ute Hentschel
- DOI
- 10.3390/md9101682
- eISSN
- 1660-3397
- Ausgabe der Veröffentlichung
- 10
- Zeitschrift
- Marine Drugs
- Sprache
- en
- Online publication date
- 2011
- Paginierung
- 1682 - 1697
- Status
- Published online
- Herausgeber
- MDPI AG
- Herausgeber URL
- http://dx.doi.org/10.3390/md9101682
- Datum der Datenerfassung
- 2018
- Titel
- New Tetromycin Derivatives with Anti-Trypanosomal and Protease Inhibitory Activities
- Ausgabe der Zeitschrift
- 9
Datenquelle: Crossref
- Abstract
- Four new tetromycin derivatives, tetromycins 1-4 and a previously known one, tetromycin B (5) were isolated from Streptomyces axinellae Pol001(T) cultivated from the Mediterranean sponge Axinella polypoides. Structures were assigned using extensive 1D and 2D NMR spectroscopy as well as HRESIMS analysis. The compounds were tested for antiparasitic activities against Leishmania major and Trypanosoma brucei, and for protease inhibition against several cysteine proteases such as falcipain, rhodesain, cathepsin L, cathepsin B, and viral proteases SARS-CoV M(pro), and PL(pro). The compounds showed antiparasitic activities against T. brucei and time-dependent inhibition of cathepsin L-like proteases with K(i) values in the low micromolar range.
- Addresses
- Julius-von-Sachs Institute for Biological Sciences, University of Würzburg, Julius-von-Sachs-Platz 3, Würzburg 97082, Germany.
- Autoren
- Sheila M Pimentel-Elardo
- Verena Buback
- Tobias AM Gulder
- Tim S Bugni
- Jason Reppart
- Gerhard Bringmann
- Chris M Ireland
- Tanja Schirmeister
- Ute Hentschel
- DOI
- 10.3390/md9101682
- eISSN
- 1660-3397
- Externe Identifier
- PubMed Identifier: 22072992
- PubMed Central ID: PMC3210601
- Funding acknowledgements
- NCI NIH HHS: R01 CA036622
- Open access
- true
- ISSN
- 1660-3397
- Ausgabe der Veröffentlichung
- 10
- Zeitschrift
- Marine drugs
- Schlüsselwörter
- Animals
- Axinella
- Leishmania major
- Trypanosoma brucei brucei
- Streptomyces
- Cathepsin B
- Cysteine Endopeptidases
- Viral Proteins
- Protease Inhibitors
- Antiprotozoal Agents
- Trypanocidal Agents
- Magnetic Resonance Spectroscopy
- Cathepsin L
- Heterocyclic Compounds, 4 or More Rings
- Coronavirus 3C Proteases
- Severe acute respiratory syndrome-related coronavirus
- Sprache
- eng
- Medium
- Print-Electronic
- Online publication date
- 2011
- Open access status
- Open Access
- Paginierung
- 1682 - 1697
- Datum der Veröffentlichung
- 2011
- Status
- Published
- Publisher licence
- CC BY
- Datum der Datenerfassung
- 2011
- Titel
- New tetromycin derivatives with anti-trypanosomal and protease inhibitory activities.
- Sub types
- Research Support, Non-U.S. Gov't
- research-article
- Journal Article
- Research Support, N.I.H., Extramural
- Ausgabe der Zeitschrift
- 9
Files
https://www.mdpi.com/1660-3397/9/10/1682/pdf?version=1424781264 https://www.ncbi.nlm.nih.gov/pmc/articles/pmid/22072992/pdf/?tool=EBI https://europepmc.org/articles/PMC3210601?pdf=render
Datenquelle: Europe PubMed Central
- Abstract
- Four new tetromycin derivatives, tetromycins 1-4 and a previously known one, tetromycin B (5) were isolated from Streptomyces axinellae Pol001(T) cultivated from the Mediterranean sponge Axinella polypoides. Structures were assigned using extensive 1D and 2D NMR spectroscopy as well as HRESIMS analysis. The compounds were tested for antiparasitic activities against Leishmania major and Trypanosoma brucei, and for protease inhibition against several cysteine proteases such as falcipain, rhodesain, cathepsin L, cathepsin B, and viral proteases SARS-CoV M(pro), and PL(pro). The compounds showed antiparasitic activities against T. brucei and time-dependent inhibition of cathepsin L-like proteases with K(i) values in the low micromolar range.
- Date of acceptance
- 2011
- Autoren
- Sheila M Pimentel-Elardo
- Verena Buback
- Tobias AM Gulder
- Tim S Bugni
- Jason Reppart
- Gerhard Bringmann
- Chris M Ireland
- Tanja Schirmeister
- Ute Hentschel
- Autoren-URL
- https://www.ncbi.nlm.nih.gov/pubmed/22072992
- DOI
- 10.3390/md9101682
- eISSN
- 1660-3397
- Externe Identifier
- PubMed Central ID: PMC3210601
- Funding acknowledgements
- NCI NIH HHS: R01 CA036622
- Ausgabe der Veröffentlichung
- 10
- Zeitschrift
- Mar Drugs
- Schlüsselwörter
- Streptomyces axinellae
- anti-trypanosomal
- marine sponge
- protease inhibition
- tetromycin
- Animals
- Antiprotozoal Agents
- Axinella
- Cathepsin B
- Cathepsin L
- Coronavirus 3C Proteases
- Cysteine Endopeptidases
- Heterocyclic Compounds, 4 or More Rings
- Leishmania major
- Magnetic Resonance Spectroscopy
- Protease Inhibitors
- Severe acute respiratory syndrome-related coronavirus
- Streptomyces
- Trypanocidal Agents
- Trypanosoma brucei brucei
- Viral Proteins
- Sprache
- eng
- Country
- Switzerland
- Paginierung
- 1682 - 1697
- PII
- md9101682
- Datum der Veröffentlichung
- 2011
- Status
- Published
- Datum, an dem der Datensatz öffentlich gemacht wurde
- 2013
- Titel
- New tetromycin derivatives with anti-trypanosomal and protease inhibitory activities.
- Sub types
- Journal Article
- Research Support, N.I.H., Extramural
- Research Support, Non-U.S. Gov't
- Ausgabe der Zeitschrift
- 9
Datenquelle: PubMed
- Beziehungen:
- Eigentum von