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Details of Grant 

EPSRC Reference: EP/P020291/1
Title: Diversity-Oriented Synthesis of Stapled Peptides
Principal Investigator: Spring, Professor D
Other Investigators:
Researcher Co-Investigators:
Project Partners:
AstraZeneca
Department: Chemistry
Organisation: University of Cambridge
Scheme: EPSRC Fellowship
Starts: 01 December 2017 Ends: 30 November 2020 Value (£): 1,205,345
EPSRC Research Topic Classifications:
Biological & Medicinal Chem. Protein chemistry
EPSRC Industrial Sector Classifications:
Pharmaceuticals and Biotechnology
Related Grants:
Panel History:
Panel DatePanel NameOutcome
28 Feb 2017 EPSRC Physical Sciences - Fellowship Interview February 2017 Announced
24 Jan 2017 EPSRC Physical Sciences - January 2017 Announced
Summary on Grant Application Form
The pharmaceutical industry has historically had great success in developing therapeutics against targets such as enzymes and receptor proteins. Recent years have witnessed a shift towards exploring new and more challenging biological targets. Protein-protein interactions (PPIs) represent an incredibly rich source of new potential drug targets, as they are irrefutably linked to human diseases, including various cancers. Unfortunately, PPIs remain a large and underexploited class of drug-targets as traditional small molecule approaches are often not ideal for inhibiting PPI interfaces. Conformationally-constrained peptides (often referred to as 'stapled peptides') has emerged as a promising strategy to address these historically 'undruggable' targets and provide new and valuable insights into the complex mechanisms that underlie many diseases with high unmet medical needs.

This proposal aims to develop a new enabling platform for the efficient production of diverse conformationally-constrained peptides with tailored properties that are directly relevant to the pharmaceutical industry. The technique will be exceptional in its efficiency, adaptability and simplicity of implementation, and would represent a major step-change from current chemistry approaches to access constrained peptides with specific chemical/biological profiles. The proposed work has the potential to define a general strategy for the rapid discovery and optimisation of next-generation cancer therapeutics, and deliver a vast array of new high-quality probes for chemical biology studies.

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Organisation Website: http://www.cam.ac.uk