Structural Basis of Gabapentinoid Drug Action (360G-Wellcome-202355_Z_16_Z)

£2,000

Gabapentinoids are blockbuster drugs used to treat conditions including neuropathic pain and epilepsy. They act by binding α2δ voltage-gated Ca2+ channel subunits. The focus of this summer project is to investigate the structure of α2δ to help understand its role in presynaptic Ca2+ entry and reveal the molecular basis of gabapentinoid binding. We have developed constructs for α2δ expression in High5 insect cells and HEK293T eukaryotic cells. We will express and purify different regions of α2δ, taking advantage of enzymes at our disposal for modifying glycosylation and pre-protein cleavage. Co-crystallisation screens will be set up with natural and synthetic small molecules including pregabalin and gabapentin. Successful crystal hits will be tested for x-ray diffraction using an in-house x-ray source. In the final fortnight of reserach, the student will perform crosslinking coupled to mass spectrometry experiments to determine the interaction sites of different subunits within the calcium channel complex, depending on the progress of crystallisation experiments.

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Grant Details

Amount Awarded 2000
Applicant Surname Liu
Approval Committee Internal Decision Panel
Award Date 2016-04-01T00:00:00+00:00
Financial Year 2015/16
Grant Programme: Title Vacation Scholarships
Has the grant transferred? No
Internal ID 202355/Z/16/Z
Lead Applicant Mr Chenge Liu
Planned Dates: End Date 2016-09-10T00:00:00+00:00
Planned Dates: Start Date 2016-07-11T00:00:00+00:00
Recipient Org: City London
Recipient Org: Country United Kingdom
Region London
Research conducted at multiple locations? No
Total amount including partnership funding 2000