Effects of endogenous anticancer oestrogen metabolite on biological activity

January 13, 2014
The researchers designed an imaginative cover feature illustrating the drug molecule as a synthesis of discrete fragments, flanked by renderings of the target protein, tubulin. In the background is an image of cultured cells expressing recombinant tagged tubulin, labelled with a green fluorescent dye.

A publication on anti-cancer drug candidates designed by University of Bath researchers in the Department of Pharmacy & Pharmacology has been awarded Very Important Paper status by the medicinal chemistry journal ChemMedChem.

The paper entitled "Tetrahydroisoquinolinone-based Steroidomimetic and Chimeric Microtubule Disruptors" describes how the researchers designed the prototype using fragments derived from 2-methoxyoestradiol (an endogenous anticancer oestrogen metabolite) and colchicine (a compound extracted from a crocus) as templates. They then combined these together in new hybrid structures and modified them systematically to explore the effects on biological activity.

The work was carried out as part of the assets of Sterix Ltd – a University spin-out company with Imperial College – and, more recently, in collaboration with a specialist group in the USA.

Sterix Ltd was co-founded by Professor Barry Potter from our Department of Pharmacy & Pharmacology and was acquired by the pharmaceutical company Ipsen in 2004.

The paper appeared in this month's issue of the journal, which includes a special invited cover feature designed by the researchers.

Professor Potter said: "It is highly rewarding to see the creation of this new drug class from our synthetic laboratory and its high level pre-clinical development. It is also encouraging to see the ongoing academic peer recognition of our work.

"This work emphasises the continuing strength of medicinal chemistry at the University and demonstrates again that academic scientists can play a key role in discovering – traditionally a preserve of the pharmaceutical industry."

Professor Potter also started work as an invited member of the ChemMedChem International Advisory Board at the beginning of January.

Explore further: Cancer drug developed at University of Bath begins trials

More information: "Tetrahydroisoquinolinone-Based Steroidomimetic and Chimeric Microtubule Disruptors." Dr. Mathew P. Leese, Dr. Fabrice L. Jourdan, Dr. Meriel R. Major, et al. ChemMedChem. Volume 9, Issue 1, pages 85–108, January 2014. DOI: 10.1002/cmdc.201300261

Related Stories

Cancer drug developed at University of Bath begins trials

November 7, 2013
Trials are beginning for Irosustat, a drug pioneered here at the University, which could prolong the lives of thousands of women with advanced breast cancer.

3D structure opens new avenue for drug discovery

April 2, 2012
(PhysOrg.com) -- An international consortium has determined the structure of an important new drug target in complex with a synthetic molecule designed by our researchers, opening up new avenues for drug discovery.

New discovery in quest for better drugs

October 14, 2013
Scientists have combined cutting edge computer modelling with pharmacology and medicinal chemistry to reveal new insights into how the body interacts with novel drug treatments, in research that could lead to the creation ...

Why combination drug treatment ineffective in cancer clinical trials

December 5, 2013
Medical researchers at the University of Alberta have discovered that combination drug therapy didn't work well in clinical trials for cancer patients because one drug was making the other drug ineffective.

Recommended for you

Researchers release first draft of a genome-wide cancer 'dependency map'

July 27, 2017
In one of the largest efforts to build a comprehensive catalog of genetic vulnerabilities in cancer, researchers from the Broad Institute of MIT and Harvard and Dana-Farber Cancer Institute have identified more than 760 genes ...

Cancer-death button gets jammed by gut bacterium

July 27, 2017
Researchers at Michigan Medicine and in China showed that a type of bacterium is associated with the recurrence of colorectal cancer and poor outcomes. They found that Fusobacterium nucleatum in the gut can stop chemotherapy ...

Long-sought mechanism of metastasis is discovered in pancreatic cancer

July 27, 2017
Cells, just like people, have memories. They retain molecular markers that at the beginning of their existence helped guide their development. Cells that become cancerous may be making use of these early memories to power ...

Manmade peptides reduce breast cancer's spread

July 27, 2017
Manmade peptides that directly disrupt the inner workings of a gene known to support cancer's spread significantly reduce metastasis in a mouse model of breast cancer, scientists say.

Blocking the back-door that cancer cells use to escape death by radiotherapy

July 27, 2017
A natural healing mechanism of the body may be reducing the efficiency of radiotherapy in breast cancer patients, according to a new study.

Glowing tumor technology helps surgeons remove hidden cancer cells

July 27, 2017
Surgeons were able to identify and remove a greater number of cancerous nodules from lung cancer patients when combining intraoperative molecular imaging (IMI) - through the use of a contrast agent that makes tumor cells ...

0 comments

Please sign in to add a comment. Registration is free, and takes less than a minute. Read more

Click here to reset your password.
Sign in to get notified via email when new comments are made.