Akbulut, Y, Gaunt, HJ, Muraki, K et al. (12 more authors) (2015) (−)-Englerin A is a Potent and Selective Activator of TRPC4 and TRPC5 Calcium Channels. Angewandte Chemie International Edition, 54 (12). pp. 3787-3791. ISSN 1433-7851
Abstract
Current therapies for common types of cancer such as renal cell cancer are often ineffective and unspecific, and novel pharmacological targets and approaches are in high demand. Here we show the unexpected possibility for the rapid and selective killing of renal cancer cells through activation of calcium-permeable nonselective transient receptor potential canonical (TRPC) calcium channels by the sesquiterpene (−)-englerin A. This compound was found to be a highly efficient, fast-acting, potent, selective, and direct stimulator of TRPC4 and TRPC5 channels. TRPC4/5 activation through a high-affinity extracellular (−)-englerin A binding site may open up novel opportunities for drug discovery aimed at renal cancer.
Metadata
| Item Type: | Article |
|---|---|
| Authors/Creators: |
|
| Keywords: | antitumor agents; calcium ions; ion channels; natural products |
| Dates: |
|
| Institution: | The University of Leeds |
| Academic Units: | The University of Leeds > Faculty of Medicine and Health (Leeds) > School of Medicine (Leeds) > Leeds Institute of Genetics, Health and Therapeutics (LIGHT) > Academic Unit of Cardiovascular Medicine (Leeds) The University of Leeds > Faculty of Medicine and Health (Leeds) > School of Medicine (Leeds) > Leeds Institute of Cancer and Pathology (LICAP) > Clinical Cancer Research (Leeds) |
| Depositing User: | Symplectic Publications |
| Date Deposited: | 13 Sep 2016 10:01 |
| Last Modified: | 04 Nov 2016 07:23 |
| Published Version: | http://dx.doi.org/10.1002/anie.201411511 |
| Status: | Published |
| Publisher: | Wiley |
| Identification Number: | 10.1002/anie.201411511 |
| Related URLs: | |
| Open Archives Initiative ID (OAI ID): | oai:eprints.whiterose.ac.uk:94473 |
CORE (COnnecting REpositories)
CORE (COnnecting REpositories)