Synthesis of cancer targeting compounds derived from a fragment-based approach. (360G-Wellcome-090171_Z_09_Z)

£152,502

In the initial phase of this project, the PhD student will synthesise selected fragment type molecules, which mimic the observed5 interaction of TLE1 with the small peptide sequences. These specific fragments will supplement the fragment library, which is routinely used at the I CR. Within the structure based drug design team (SBDD} and the section of structure biology these specific fragments as well as the ICR fragment collection will be screened for binding to TLE1. Fragments with sufficient affinity for TLE1 will be co-crystalized. The PhD student will use these co-crystal structures to design and synthesise more complex and potent inhibitors of TLE1 binding thus completing the first round of testing, crystallography and synthesis. Additional iterative rounds will lead to inhibitors with further improved properties. The overall goal is to obtain inhibitors suitable for investigating the role of TLE1 in a cellular setting and potentially in in vivo models.

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Grant Details

Amount Awarded 152502
Applicant Surname McGrath
Approval Committee Neurosciences And Mental Health
Award Date 2009-06-08T00:00:00+00:00
Financial Year 2008/09
Grant Programme: Title PhD Studentship (Basic & Clinical)
Internal ID 090171/Z/09/Z
Lead Applicant Miss Sally McGrath
Partnership Value 152502
Planned Dates: End Date 2013-09-30T00:00:00+00:00
Planned Dates: Start Date 2009-10-01T00:00:00+00:00
Recipient Org: Country United Kingdom
Region Greater London
Sponsor(s) Prof Paul Workman