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Instruments / Technical Area	Publication Details	Published	Actions
I24-Microfocus Macromolecular Crystallography	The structural basis for high affinity binding of α1-acid glycoprotein to the potent anti-tumour compound UCN-01 Erik J. B. Landin , Christopher Williams , Sara A. Ryan , Alice Bochel , Akter Nahida , Christina Redfield , Richard B. Sessions , Neesha Dedi , Richard Taylor , Matthew P. Crump Journal Of Biological Chemistry 12 DOI: 10.1016/j.jbc.2021.101392 Diamond Proposal Number(s): [23269] Open Access Show Abstract ▼ Abstract: The α1-acid glycoprotein (AGP) is an abundant blood plasma protein with important immunomodulatory functions coupled to endogenous and exogenous ligand binding properties. Its affinity for many drug-like structures, however, means AGP can have a significant effect on the pharmokinetics and pharmacodynamics of numerous small molecule therapeutics. Staurosporine, and its hydroxylated forms UCN-01 and UCN-02, are kinase inhibitors that have been investigated at length as anti-tumour compounds. Despite their potency, these compounds display poor pharmokinetics due to binding to both AGP variants, AGP1 and AGP2. Recent renewed interest in UCN-01 as a cytostatic protective agent prompted us to solve the structure of the AGP2/UCN-01 complex by X-ray crystallography, revealing for the first time the precise binding mode of UCN-01. Solution NMR suggests AGP2 undergoes a significant conformational change upon ligand binding, but also that it uses a common set of sidechains with which it captures key groups of UCN-01 and other small molecule ligands. We anticipate that this structure and supporting NMR data will facilitate rational re-design of small molecules that could evade AGP and therefore improve tissue distribution.	Nov 2021
I18-Microfocus Spectroscopy	The development of a XEOL and TR XEOL detection system for the I18 microfocus beamline Diamond light source R. P. Taylor , A. A. Finch , P. D. Quinn , J. F. W. Mosselmans Journal Of Luminescence DOI: 10.1016/j.jlumin.2012.09.018 Diamond Proposal Number(s): [5577] Show Abstract ▼ Abstract: We describe the design and capabilities of a new Continuous Wave X-ray Excited Optical Luminescence (CW-XEOL) and Time Resolved X-ray Excited Optical Luminescence (TR-XEOL) facility on the I18 beamline at the DIAMOND light source, the UK national synchrotron facility. Experimental data from a suite of framework silicates are presented to illustrate the capabilities of the system. Experiments studied include simple (CW-XEOL) spectroscopy, (TR XEOL) lifetime experiments dose and dose rate dependence (CW-XEOL) experiments, spatial (TR XEOL) on heterogeneous sample, wavelength resolved (TR XEOL), Optically Derived X-ray Absorption Spectroscopy, (OD XAS).	Nov 2012

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