InstructThe latest webinar in the Instruct-ERIC Structure Meets Function series this month includes speakers who have accessed cutting-edge structural biology services through Instruct. The webinar series offers an insight into the very cutting edge of structural biology research, utilising the latest techniques available through Instruct-ERIC facilities and centres.
The webinar taking place 11:00 CET on 17 November will feature two speakers who have contributed significantly to the Fragment-Screen project coordinated by Instruct-ERIC. Antje Gohla will outline their work on the role of Vitamin B6 (VB6) in cancer progression and anti-tumour immunity, utilising CrystalDirect technology. Josan Marquez of EMBL Grenoble will then provide wider context of how fragment-screening projects are accelerated by CrystalDirect and X-Ray techniques.
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Speaker: Antje Gohla
Institution: University of Würzburg
Talk Title: Generating tools to probe the antineoplastic roles of vitamin B6
Abstract: Vitamin B6 (VB6) is a micronutrient with important but insufficiently understood roles in cancer progression and anti-tumour immunity. Pharmacological tools to elucidate its roles in different cancer entities are currently lacking. We focus on pyridoxal phosphatase (PDXP), a negative regulator of VB6, to control the cellular metabolism of bioactive VB6. Phosphatases are notoriously difficult to target and indeed, a high throughput, PDXP activity-based screening campaign identified only a single small-molecule PDXP inhibitor. However, this molecule is inappropriate as a lead compound for further PDXP inhibitor development efforts. To identify new ligands, we conducted high throughput crystallization of PDXP and fragment screening based on the CrystalDirect technology and CRIMS software at the HTX lab. The screening of 1200 PDXP crystals yielded 25 fragment hits that bind the PDXP active site or an adjacent site. These molecules are now used in further screens and to initiate medicinal chemistry developments.
Speaker: Josan Marquez
Institution: EMBL Grenoble
Talk Title: TBD
