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