Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
Results
Showing 1 to 5 of 5 for “"fragment screen"”.
-
A fragment-based approach towards understanding molecular recognition of 4’-phosphopantetheine adenylyltransferase from Mycobacterium abscessus
… in this thesis details the application of a fragment-based approach targeting 4’-phosphopantetheine adenylyltransferase (PPAT) from Mycobacterium abscessus (Mabs). A fragment screen of the Abell laboratory 960-member library was conducted by Dr Sherine Thomas (Department of Biochemistry, …
-
To Design and Develop Semi-Saturated and Unsaturated Bicyclic Heterocycles for Fragment-Based Drug Discovery (FBDD) Campaigns
The concept of Fragment-Based Drug-Discovery (FBDD) seeks to overcome current issues associated with High-Throughput Screening (HTS) for the identification of novel hits, which are ultimately elaborated into leads and drug candidates. This thesis focuses on the preparation of either novel or …
-
Developing Chemical Tools for the Inhibition of Activin A Signalling
… activin A through the use of XChem, conducting a fragment screen against mature activin A crystals. I describe the identification of twelve fragment hits that bind in the putative type I receptor binding site and the validation and optimisation of one of these fragments. I then used the structure …
-
Targeting the Rho1 GTPase signalling pathway in <i>Aspergillus fumigatus</i>
… research, I combined X-ray crystallography and fragment-based small molecule screening by BLI (Biolayer interferometry) to investigate the ligandability of <i>Af</i>Rho1. Using X-ray crystallography, the structure of <i>Af</i>Rho1 was solved and a complex structure with one of the hit fragments …
-
"Sugar Coat" Genetic & chemical validation of <i>Aspergillus fumigatus</i> cell wall targets
… plant-type chitinase A1 by high-throughput screening. Analysis of the binding mode by X-ray crystallography confirmed competitive inhibition and further kinetic studies identified two compounds with selectivity towards A. fumigatus plant-type chitinases. The lead compound and a …