The University of Southampton
University of Southampton Institutional Repository
Warning ePrints Soton is experiencing an issue with some file downloads not being available. We are working hard to fix this. Please bear with us.

Novel epidithiodiketopiperazines as anti-viral zinc ejectors of the Feline Immunodeficiency Virus (FIV) nucleocapsid protein as a model for HIV infection

Novel epidithiodiketopiperazines as anti-viral zinc ejectors of the Feline Immunodeficiency Virus (FIV) nucleocapsid protein as a model for HIV infection
Novel epidithiodiketopiperazines as anti-viral zinc ejectors of the Feline Immunodeficiency Virus (FIV) nucleocapsid protein as a model for HIV infection
Focused libraries of multi-substituted epidithiodiketopiperazines (ETP) were prepared and evaluated for efficacy of inhibiting the nucleocapsid protein function of the Feline Immunodeficiency Virus (FIV) as a model for HIV. This activity was compared and contrasted to observed toxicity utilising an in-vitro cell culture approach. This resulted in the identification of several promising lead compounds with nanomolar potency in cells with low toxicity and a favorable therapeutic index.
Epidithiodiketopiperazines (ETP), Zinc ejection, Feline Immunodeficiency Virus (FIV), Human Immunodeficiency Virus (HIV), Nucleocapsid protein (NCp)
0968-0896
4174-4184
Asquith, Christopher R.M.
c00d3c3f-08c5-4c9a-bac8-0fc485db1be4
Sil, Bruno C.
83be81f1-53b4-4af9-bdfa-9e8f8b1f66ea
Laitinen, Tuomo
b37037c5-4eac-4533-8246-5a49213bae9b
Tizzard, Graham J.
8474c0fa-40df-43a6-a662-7f3c4722dbf2
Coles, Simon J.
3116f58b-c30c-48cf-bdd5-397d1c1fecf8
Poso, Antii
4563f55e-93b3-4df8-a5a6-1e75a4cd8455
Hofmann-Lehmann, Regina
0c1c2056-848e-469c-8bb9-0258293160de
Hilton, Stephen T.
b3c15d45-c69d-47cd-a367-77a43e3fdbed
Asquith, Christopher R.M.
c00d3c3f-08c5-4c9a-bac8-0fc485db1be4
Sil, Bruno C.
83be81f1-53b4-4af9-bdfa-9e8f8b1f66ea
Laitinen, Tuomo
b37037c5-4eac-4533-8246-5a49213bae9b
Tizzard, Graham J.
8474c0fa-40df-43a6-a662-7f3c4722dbf2
Coles, Simon J.
3116f58b-c30c-48cf-bdd5-397d1c1fecf8
Poso, Antii
4563f55e-93b3-4df8-a5a6-1e75a4cd8455
Hofmann-Lehmann, Regina
0c1c2056-848e-469c-8bb9-0258293160de
Hilton, Stephen T.
b3c15d45-c69d-47cd-a367-77a43e3fdbed

Asquith, Christopher R.M., Sil, Bruno C., Laitinen, Tuomo, Tizzard, Graham J., Coles, Simon J., Poso, Antii, Hofmann-Lehmann, Regina and Hilton, Stephen T. (2019) Novel epidithiodiketopiperazines as anti-viral zinc ejectors of the Feline Immunodeficiency Virus (FIV) nucleocapsid protein as a model for HIV infection. Bioorganic & Medicinal Chemistry, 27 (18), 4174-4184. (doi:10.1016/j.bmc.2019.07.047).

Record type: Article

Abstract

Focused libraries of multi-substituted epidithiodiketopiperazines (ETP) were prepared and evaluated for efficacy of inhibiting the nucleocapsid protein function of the Feline Immunodeficiency Virus (FIV) as a model for HIV. This activity was compared and contrasted to observed toxicity utilising an in-vitro cell culture approach. This resulted in the identification of several promising lead compounds with nanomolar potency in cells with low toxicity and a favorable therapeutic index.

Text
ETP BMC GJT - Accepted Manuscript
Download (516kB)
Text
ETP BMC 22ndJuly2019-CA - Proof
Restricted to Repository staff only
Request a copy

More information

Accepted/In Press date: 28 July 2019
e-pub ahead of print date: 30 July 2019
Published date: 15 September 2019
Keywords: Epidithiodiketopiperazines (ETP), Zinc ejection, Feline Immunodeficiency Virus (FIV), Human Immunodeficiency Virus (HIV), Nucleocapsid protein (NCp)

Identifiers

Local EPrints ID: 434438
URI: http://eprints.soton.ac.uk/id/eprint/434438
ISSN: 0968-0896
PURE UUID: 24a7c04b-5c23-4878-b98e-7d5182c27295
ORCID for Graham J. Tizzard: ORCID iD orcid.org/0000-0002-1577-5779
ORCID for Simon J. Coles: ORCID iD orcid.org/0000-0001-8414-9272

Catalogue record

Date deposited: 23 Sep 2019 16:31
Last modified: 26 Nov 2021 06:12

Export record

Altmetrics

Contributors

Author: Christopher R.M. Asquith
Author: Bruno C. Sil
Author: Tuomo Laitinen
Author: Simon J. Coles ORCID iD
Author: Antii Poso
Author: Regina Hofmann-Lehmann
Author: Stephen T. Hilton

Download statistics

Downloads from ePrints over the past year. Other digital versions may also be available to download e.g. from the publisher's website.

View more statistics

Atom RSS 1.0 RSS 2.0

Contact ePrints Soton: eprints@soton.ac.uk

ePrints Soton supports OAI 2.0 with a base URL of http://eprints.soton.ac.uk/cgi/oai2

This repository has been built using EPrints software, developed at the University of Southampton, but available to everyone to use.

We use cookies to ensure that we give you the best experience on our website. If you continue without changing your settings, we will assume that you are happy to receive cookies on the University of Southampton website.

×