Download Trinity Research & Innovation-Licensing Opportunity Technology Overview

TRINITY COLLEGE DUBLIN
Trinity Research & Innovation-Licensing Opportunity
Dual Inhibitors of Tumor Angiogenesis & Vasculature
Novel inhibitors of tumor angiogenesis and vasculature with a dual mechanism of action
Technology Overview
Tumor angiogenesis (blood vessel formation) and tumor vasculature have recently emerged as important targets in cancer
treatment, applicable to multiple tumor types. Enzymes, specifically expressed in endothelial and sub-endothelial cells during
tumor angiogenesis but not in normal vasculature represent an important target for inhibiting tumor growth and metastasis. The
recent advance in identifying the role played by tubulin inhibitors in causing tumor vasculature shutdown also represents an
attractive target for inhibiting tumor angiogenesis/vasculature.
Researchers at Trinity College Dublin have developed novel hybrid inhibitors of tumor angiogenesis and vasculature with
a dual mechanism of action, namely prevention of tubulin polymerization and enzyme inhibition. These novel compounds have
the necessary built-in functionality to (i) inhibit endothelial cell proliferation and motility, (iii) prevent capillary tube formation,
and (iv) cause tumour vasculature shutdown.
Advantages:
The dual-mechanism of action compounds will target the
tumour more effectively than drugs which only target one
specific mode of action.
Principal Inventor(s):
Dr. John Walsh
The chemistry of these compounds is versatile such that
pro drug variations can be synthesized.
Publications:
The novel anti-tubulin component of the hybrid is more
efficacious than current therapies such as combrestatin A-4
and as this technology is a monotherapy and will be less
toxic than cocktail therapies that are currently being
employed.
TCD Ref: JW01-151-01
N/A
Contact:
Development Stage:
The efficacy of the compounds at nanomolar concentrations
has been demonstrated successfully in vitro utilizing tubulin
polymerizeration assays. Lead compounds have been tested
successfully in ex vivo aortic ring. Further developmental
work is currently underway to examine the compounds for
efficacy and toxicity in a variety of animal tumor models in
vivo.
Emily Vereker, PhD
Technology Transfer Case Manager-Life Sciences
Tel: +1 353 1 896-4152
Email: [email protected]