Next Article in Journal
A Green Slab Waveguide for Plasmonic Sensors Based on Bacterial Cellulose
Previous Article in Journal
Amaryllidaceae Alkaloids from Zephyrantes Carinata and Their Evaluation as Cholinesterases (AChE and BChE) Inhibitors
Open AccessExtended Abstract

Development of Novel, Potent Phosphatidyl–Choline-Specific Phospholipase C Inhibitors

1
School of Chemical Sciences, University of Auckland, Auckland 1142, New Zealand
2
Auckland Cancer Society Research Centre, University of Auckland, Grafton, Auckland 1023, New Zealand
*
Author to whom correspondence should be addressed.
Presented at the 2nd Molecules Medicinal Chemistry Symposium (MMCS): Facing Novel Challenges in Drug Discovery, Barcelona, Spain, 15–17 May 2019.
Proceedings 2019, 22(1), 67; https://doi.org/10.3390/proceedings2019022067
Published: 12 August 2019
(This article belongs to the Proceedings of The Molecules Medicinal Chemistry Symposium)
PDF [129 KB, uploaded 12 August 2019]

Abstract

The phosphatidyl–choline-specific phospholipase C (PC-PLC) enzyme has been shown to be an important enzyme involved in various cell-signaling processes. Furthermore, PC-PLC has been shown to be upregulated in various cancer cell lines, thereby presenting itself as a potential anti-cancer therapeutic target. Current PC-PLC inhibitors, including the literature standard inhibitor D609 possess characteristics making them unsuitable for clinical use. We have discovered a new class of potent PC-PLC inhibitors with much improved activity and drug-like properties than D609. The synthesis and SAR study of this class of active compounds is presented.
Keywords: PC-PLC; SAR study; enzyme inhibition; phospholipase C PC-PLC; SAR study; enzyme inhibition; phospholipase C
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
SciFeed

Share & Cite This Article

MDPI and ACS Style

Pilkington, L.I.; Leung, E.; Barker, D. Development of Novel, Potent Phosphatidyl–Choline-Specific Phospholipase C Inhibitors. Proceedings 2019, 22, 67.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Metrics

Article Access Statistics

1

Comments

[Return to top]
Proceedings EISSN 2504-3900 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top