Latest News for 12/2019
27 Nov 2019
Researchers in the Ciulli group report a first study describing the idea of a macrocyclic PROTAC. The research was published in the prestigious chemistry journal Angewandte Chemie. PROTACs (for proteolysis-targeting chimeras) are double-headed molecules composed of a ligand for a target protein and a ligand for an E3 ubiquitin ligase, chemically joined by a flexible linker. The PROTAC simultaneously recruits the target protein and the E3 ligase into close proximity, and this leads to the target protein being destroyed inside the cell.
29 Oct 2019
School of Life Science’s Professor Alessio Ciulli was amongst a selected group of world’s leading expert scientists and key opinion leaders who spoke at the Galien Forum on October 24, 2019, at the Alexandria Center in New York City. Alessio’s panel, entitled ‘Drugging the Undruggable with Novel Approaches to Small Molecule Design’, was chaired by Pfizer’s Chief Scientific Officer and President, Worldwide Research, Development and Medical, Mikael Dolsten.
29 Aug 2019
Hannah Tovell a PhD student in Dario Alessi lab working in collaboration with Claire Crafter (AstraZeneca) and Alessio Ciulli and Andrea Testa in his lab have elaborated a compound that we have termed SGK3-PROTAC1 that induces selective degradation of SGK3 protein kinase. Hannah was able to show that SGK3-PROTAC1 suppressed proliferation of ZR-75-1 and CAMA-1 cancer cell lines treated with a PI3K inhibitor (GDC0941) more effectively than could be achieved by a conventional SGK isoform inhibitor (14H), underscoring the benefit of the PROTAC approach.
University of Dundee and Eisai enter partnership for cancer drug discovery using targeted protein...08 Jul 2019
The University of Dundee has announced a new partnership with Eisai, one of the world’s leading research-based pharmaceutical companies, aiming to create innovative new drugs for the cancer field. The collaboration combines the world-leading PROTACs expertise and technology of Professor Alessio Ciulli from the Division of Biological Chemistry and Drug Discovery in the School with Eisai’s discovery research and clinical development experiences in oncology.
11 Jun 2019
In an article published today in the prestigious journal Nature Chemical Biology, scientists at the University of Dundee and Boehringer Ingelheim have made an important first stride toward drugging undruggable cancer targets using an innovative approach to drug discovery.
10 Jun 2019
Researchers in the laboratory of Professor Alessio Ciulli have revealed atomic-resolution images of how an E3 ubiquitin ligase enzyme involved in immune and cell signalling latches on to its protein partners. This is important because these binding events are required for the protein to function properly inside the cell.
15 Apr 2019
Hannah Tovell an Alessi lab PhD student working closely with the Ciulli lab has published an improved HaloPROTAC method to induce post–translational knockdown of endogenous proteins. This approach makes use of CRISPR/Cas9 genome editing technology to introduce a Halo tag onto the N or C terminus of any desired target protein that can then be targeted for degradation by a HaloPROTAC probe (see Figure).
27 Mar 2019
In an article in the journal Nature, Megan Scudellari reflects on the short history of PROTACs - a new type of drug design that is galvanising the Pharmaceutical industry, with the first PROTAC drug from Arvinas about to enter phase-1 clinical trials.
07 Jan 2019
· Boehringer Ingelheim to make BET degrader compound MZ 1 available through its opnMe.com portal · Support of open access to boost progress in biomedical and drug discovery research
10 Oct 2017
Researchers in the laboratory of Professor Alessio Ciulli have designed a small molecule that tricks a particular E3 ubiquitin ligase protein to destroy another of its kind. E3 ligases act like ‘molecular assassins’ in cells as they naturally tag unwanted proteins for cellular degradation. There are believed to be over 600 E3 ligases in the human cell and many are involved in human diseases, providing many attractive targets for drug discovery.