Mechanism based drug descovery. (360G-Wellcome-102360_Z_13_Z)

£160,623

Tankyrase recognises a peptide motif, with consensus RXX(P/G)XGXX, in substra tes through its ankyrin repeat clusters (ARCs). My aim is to develop tool compounds to disrupt the sankyrase : substrate protein-protein interaction (PPI). Targeting the ARCs is a novel method of inhibiting tankyrase function. Several approaches will be taken to develop non-peptidic inhibitors targeting the ARCs,by modification of a short peptide binding partner from the tankyrase substrate 3BP2. A peptidomimetic approach aims to find non-peptidic replacements for residues that mimic the peptide sidechain and backbone interactions. A fragment-based approached will also be taken to widen the chemical space sampled and if fragments are found that have binding affinity to ARCs, tha t can be detected crystallographically, then these can be incorporated into the peptide or grown chemically into more drug-like molecules. The peptidomimetic and fragment-based approaches will complement each other,and both ultimately have the same goal of designing potent tool compounds that are selective for TNKS and TNKS2 over other PARP family members,are cell permeable unlike the parent peptide,and have good aqueous solubility.

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Grant Details

Amount Awarded 160623
Applicant Surname Pollock
Approval Committee PhD Studentships
Award Date 2013-06-24T00:00:00+00:00
Financial Year 2012/13
Grant Programme: Title PhD Studentship (Basic & Clinical)
Internal ID 102360/Z/13/Z
Lead Applicant Miss Katie Pollock
Partnership Value 160623
Planned Dates: End Date 2017-09-30T00:00:00+00:00
Planned Dates: Start Date 2013-10-01T00:00:00+00:00
Recipient Org: Country United Kingdom
Region Greater London
Sponsor(s) Prof Paul Workman