dc.contributor.author |
Patel, Kamal D |
en |
dc.contributor.author |
De Zoysa, Gayan |
en |
dc.contributor.author |
Kanamala, Manju |
en |
dc.contributor.author |
Patel, Krunal |
en |
dc.contributor.author |
Pilkington, Lisa |
en |
dc.contributor.author |
Barker, David |
en |
dc.contributor.author |
Reynisson, Jóhannes |
en |
dc.contributor.author |
Wu, Zimei |
en |
dc.contributor.author |
Sarojini Amma, Vijayalekshmi |
en |
dc.date.accessioned |
2020-02-13T03:40:44Z |
en |
dc.date.issued |
2020-01 |
en |
dc.identifier.issn |
0022-2623 |
en |
dc.identifier.uri |
http://hdl.handle.net/2292/49993 |
en |
dc.description.abstract |
Cell-penetrating peptide conjugated peptide aldehydes Tat-A and Tat-B showed low micromolar anticancer and antifungal activities and synergistic action in combination with cisplatin and amphotericin B against cancer and fungal cells, respectively. Tat-A and Tat-B were significantly more potent than Ixazomib in inhibiting the human 20S proteasomes with IC50 values in the low nanomolar range. Treatment with Tat-A and Tat-B caused membrane disruption and pore formation in HeLa and BE(2)-C cells and inhibition and eradication of C. albicans biofilms. Apoptotic cell death of the treated HeLa and BE(2)-C cells was demonstrated by Annexin V/PI staining. Flow cytometry analyses showed that more than 78% (HeLa) and 92% (BE(2)-C cells showed signs of apoptosis and necrosis upon treatment with Tat-A and Tat-B. This study forms the first report that documents the benefits of cell-penetrating peptide conjugation to enhance the potential of peptide aldehydes as therapeutics. |
en |
dc.format.medium |
Print-Electronic |
en |
dc.language |
eng |
en |
dc.relation.ispartofseries |
Journal of medicinal chemistry |
en |
dc.rights |
Items in ResearchSpace are protected by copyright, with all rights reserved, unless otherwise indicated. Previously published items are made available in accordance with the copyright policy of the publisher. |
en |
dc.rights.uri |
https://researchspace.auckland.ac.nz/docs/uoa-docs/rights.htm |
en |
dc.title |
Novel Cell-Penetrating Peptide Conjugated Proteasome Inhibitors: Anticancer and Antifungal Investigations. |
en |
dc.type |
Journal Article |
en |
dc.identifier.doi |
10.1021/acs.jmedchem.9b01694 |
en |
pubs.issue |
1 |
en |
pubs.begin-page |
334 |
en |
pubs.volume |
63 |
en |
dc.rights.holder |
Copyright: The author |
en |
pubs.end-page |
348 |
en |
pubs.publication-status |
Published |
en |
dc.rights.accessrights |
http://purl.org/eprint/accessRights/RestrictedAccess |
en |
pubs.subtype |
Journal Article |
en |
pubs.elements-id |
790674 |
en |
pubs.org-id |
Medical and Health Sciences |
en |
pubs.org-id |
Pharmacy |
en |
pubs.org-id |
Science |
en |
pubs.org-id |
Chemistry |
en |
dc.identifier.eissn |
1520-4804 |
en |
pubs.record-created-at-source-date |
2019-12-05 |
en |
pubs.dimensions-id |
31801019 |
en |