The Innovative Targets Portfolio: Basic Life Sciences Research to Novel Therapies, through a Portfolio of Small Molecule Translational Projects
Lead Research Organisation:
University of Dundee
Department Name: UNLISTED
Abstract
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Technical Summary
The University of Dundee and its Drug Discovery Unit (DDU) is converting world-class discovery research into patient benefit through a portfolio of small molecule translational projects, the Innovative Targets Portfolio (ITP). The ITP, initiated by an MRC-DPFS devolved portfolio and extended with Confidence in Concept (CiC) awards, is a collaborative activity between the DDU and groups in and outside Dundee who wish to translate their discovery research.
The primary goal of the ITP is to de-risk novel targets and mechanisms to the stage that the BioPharma industry is willing to partner the project for development into marketed therapies to address unmet medical need. The ITP is a dynamic initiative, with projects entering and leaving the portfolio in a continuous rolling process.
Although the ITP is supported by a range of funding streams, these funds are insufficient to meet the demand from multiple potential collaborators, both within Dundee and across the UK, who have identified novel potential drug targets and are seeking to translate their ideas.
A renewed and expanded CiC award would support multiple hit discovery campaigns and hit series validation projects by the DDU. The aim is to determine the druggability/ligandability of novel targets/mechanisms and to identify high quality hit series, validated in cell-based models. The requested resources will synergise with the ITP team members supported through other funding routes, providing excellent added-value to the Confidence in Concept award.
We believe a portfolio approach is the best way to maximise resource in early stage drug discovery. This approach allows multiple projects to rapidly access an appropriate amount of hit discovery and medicinal chemistry, in a cost-effective way, to assess whether they justify further drug discovery efforts and progression towards in vivo evaluation. This will be achieved using appropriate funding streams e.g. MRC-DPFS/DCS scheme.
The University of Dundee has the infrastructure and experience required to continue to deliver success under further Confidence in Concept award, including: assay development, hit discovery, medicinal and computational chemistry, and pharmacokinetics.
The primary goal of the ITP is to de-risk novel targets and mechanisms to the stage that the BioPharma industry is willing to partner the project for development into marketed therapies to address unmet medical need. The ITP is a dynamic initiative, with projects entering and leaving the portfolio in a continuous rolling process.
Although the ITP is supported by a range of funding streams, these funds are insufficient to meet the demand from multiple potential collaborators, both within Dundee and across the UK, who have identified novel potential drug targets and are seeking to translate their ideas.
A renewed and expanded CiC award would support multiple hit discovery campaigns and hit series validation projects by the DDU. The aim is to determine the druggability/ligandability of novel targets/mechanisms and to identify high quality hit series, validated in cell-based models. The requested resources will synergise with the ITP team members supported through other funding routes, providing excellent added-value to the Confidence in Concept award.
We believe a portfolio approach is the best way to maximise resource in early stage drug discovery. This approach allows multiple projects to rapidly access an appropriate amount of hit discovery and medicinal chemistry, in a cost-effective way, to assess whether they justify further drug discovery efforts and progression towards in vivo evaluation. This will be achieved using appropriate funding streams e.g. MRC-DPFS/DCS scheme.
The University of Dundee has the infrastructure and experience required to continue to deliver success under further Confidence in Concept award, including: assay development, hit discovery, medicinal and computational chemistry, and pharmacokinetics.
Publications

Heap RE
(2017)
Identifying Inhibitors of Inflammation: A Novel High-Throughput MALDI-TOF Screening Assay for Salt-Inducible Kinases (SIKs).
in SLAS discovery : advancing life sciences R & D

Petit A
(2018)
A structural study of the complex between neuroepithelial cell transforming gene 1 (Net1) and RhoA reveals a potential anticancer drug hot spot
in Journal of Biological Chemistry
Description | Diamond XChem screen for FabA |
Amount | £20,000 (GBP) |
Organisation | Diamond Light Source |
Sector | Private |
Country | United Kingdom |
Start | 01/2018 |
End | 03/2018 |
Description | Eastbio PhD studentship |
Amount | £140,000 (GBP) |
Organisation | East of Scotland BioScience (EastBio) |
Sector | Charity/Non Profit |
Country | United Kingdom |
Start | 08/2016 |
End | 08/2020 |
Description | drug discovery funding |
Amount | £14,860 (GBP) |
Organisation | Tenovus Cancer Care |
Department | Tenovus Scotland |
Sector | Charity/Non Profit |
Country | United Kingdom |
Start | 03/2017 |
Description | Open innovation (AZ-OGA) |
Organisation | AstraZeneca |
Country | United Kingdom |
Sector | Private |
PI Contribution | The University of Dundee will use their OGA assay platform to screen the AZ compound libraries in order to identify new classes of OGA inhibitor. If suitable compounds are identified The University of Dundee will conduct structural biology, Medicinal chemistry and associated drug discovery activities to develop the hit compounds toward in vivo leads. |
Collaborator Contribution | AZ will provide access to AZ screening facilities and will provide access to proprietary compound libraries. |
Impact | Project in early stages and no outputs generated to date. |
Start Year | 2016 |
Description | Research Collaboration Agreement with AstraZeneca |
Organisation | AstraZeneca |
Country | United Kingdom |
Sector | Private |
PI Contribution | Dundee presented a drug target that had been screened in the DDU in 2013. Confirmed hits were optimised but not further developable. We discussed with AZ a desire to screen against a different library to look for new start points |
Collaborator Contribution | AZ have provided diversity and fragment libraries to Dundee |
Impact | A new diversity screen will be completed q1 2017 |
Start Year | 2016 |