Boehringer Ingelheim and University of Dundee Highlight Successful PROTAC Drug Discovery Program and Extend Their Ongoing Anti-Cancer Alliance
June 11, 2019-
Boehringer Ingelheim and University of Dundee achieve milestone in
collaboration aimed at developing novel protein degradation medicines -
Results published in Nature Chemical Biology showcase the use of the
broadly applicable structure-based PROTAC design approach to discover
highly potent and selective drug candidates -
The first PROTAC is made freely available via Boehringer Ingelheim’s
open innovation portal, opnMe -
Structure-based PROTAC design promises to accelerate the development
of therapies against currently intractable cancer drivers
INGELHEIM, Germany & DUNDEE, Scotland–(BUSINESS WIRE)–Following the success of their ongoing alliance, Boehringer Ingelheim
and the University of Dundee extend their collaboration to develop new
medicines that target and destroy key cancer causing proteins. This
brings together the expertise of Professor Alessio Ciulli, one of the
pioneers in the field of Proteolysis targeting chimeras (PROTACs), based
in the School of Life Sciences at Dundee, with Boehringer Ingelheim’s
pharmaceutical expertise and commitment to bring innovative medicines to
patients with cancer.
PROTACs represent a new class of drug candidates with the potential to
tackle compelling cancer targets which have failed traditional medicinal
chemistry approaches. They work by harnessing the cell’s natural
disposal system (the ubiquitin-proteasome). Candidate disease-causing
proteins are labelled as “expired” proteins which the proteasome then
shreds.
“PROTACs are a disruptive therapeutic modality which are bringing
previously deemed undruggable targets within reach. Our collaboration
will continue to work to bring this new class of medicines to patients,”
said Darryl B. McConnell, Ph.D., Senior Vice President and Research Site
Head, Boehringer Ingelheim, Vienna, Austria. “The joint team is making
rapid progress and have successfully reached the first collaboration
milestone setting a solid basis for achieving our goals.”
Since the initiation of the collaboration in 2016 and a significant
expansion in 2018, the application of PROTACs has grown dramatically.
However, designing PROTACs remains challenging and largely empirical in
nature, hindering faster progress in the field. The partners have thus
developed a structure-based design approach as a solid basis to
accelerate further development. In addition, to boost PROTAC research
around the world, Boehringer Ingelheim has made the protein degrader
compound MZ-1, developed at the University of Dundee, freely available
through its opnMe portal in 2018. Further PROTAC molecules are
considered for release on opnMe based on the success of this initiative.
The joint team has reported recent progress in a number of scientific
publications, including most recently in the journal Nature
Chemical Biology. This publication highlights their approach to use
3-dimensional pictures at atomic resolution to design highly potent and
selective drug candidates. The new approach has yielded the first PROTAC
which shreds SMARCA2, a protein that drives the tumors of more than
20,000 new patients with cancer each year and for which drug discovery
approaches have otherwise been unsuccessful to date.
“Our joint publication is a leading example of translating the detailed
understanding we are developing of how PROTACs work, to craft degrader
molecules that effectively tackle previously ‘undruggable’ targets”,
said Alessio Ciulli, Ph.D., Chair of Chemical and Structural Biology at
the University of Dundee, and winner of the 2016 RSC Capps Green Zomaya
Award for medicinal chemistry. “The expansion marks an important
milestone in the development of our alliance. It enables the joint team
to drive the next phase of degrading highly-prized cancer targets
previously intractable via other approaches”
Boehringer Ingelheim is focusing on developing innovative new treatment
approaches providing outstanding value for patients. To achieve this,
the company is increasing its commitment to external innovation, and is
working with top partners from academia and industry worldwide. A
growing network of academic collaborations reflects the company’s focus
on emerging science that could open new avenues leading to the
breakthrough medications of the future.
Please click on the link for “Notes to Editors” and “References”:
Contacts
Boehringer Ingelheim:
Dr. Reinhard Malin
Head of
Communications Innovation Unit
Boehringer Ingelheim Corporate
Center GmbH
Media + PR
[email protected]
P:
+49 6132 77-90815
M: + 49 151 150 20 690
www.boehringer-ingelheim.com