BEGIN:VCALENDAR PRODID:-//eluceo/ical//2.0/EN VERSION:2.0 CALSCALE:GREGORIAN BEGIN:VEVENT UID:da6f58c7c5bc92cb36b5485a287576b4 DTSTAMP:20260516T144341Z SUMMARY:Dr Tom D. Heightman\, VP and Head of Chemistry\, Astex Pharmaceutic als UK DESCRIPTION:11:30 – 11:45  \nDr Robert Channon:  From Bench to Bedside:   Nucleic Acid Sensors via Paper-Based Oligonucleotide-Templated Reaction s \n11:45 – 12:00  \nTiffany Chan:  Targeted delivery of therapeutic a gents across the blood-brain barrier using focused ultrasound\n12:00 – 1 3:00 \nMain Visiting Speaker – Dr Tom D. Heightman:  Fragment Based Dru g Discovery and Chemical Biology\nAbstract:\nFragment based drug discovery at Astex uses X-ray crystallographic and biophysical screening to detect the binding of small molecular fragments. Although such fragments bind wit h weak affinities\, their small size allows them to adopt well aligned ori entations that maximize their interaction with the target protein. Selecti on of fragment hits with vectors suitable for growing and optimization\, s upported by fast iterative structure-based design\, allows potent inhibito rs to be constructed with a highly complementary structure to the target p rotein. The approach allows molecular weight and lipophilicity to be stric tly controlled\, providing leads with high ligand efficiency\, which is of particular importance when addressing challenging targets with dispersed pharmacophores such as protein-protein interactions.\n This talk will des cribe key aspects of fragment-based drug discovery at Astex\, including sc reening\, X-ray structure guided design\, ligand conformational analysis i n solution\, and development of new synthesis methodology for fragment vec tor growth enablement\, illustrated by recent projects which successfully progressed from fragment screens into pre-clinical and clinical drug candi dates. The lecture will close with some highlights from recent work to exp lore a “click and play” approach to chemical biology experiments inclu ding cellular imaging\, target engagement and in-cell formation of PROTACs .\nBiography:\nTom obtained his Chemistry MA at Oxford\, and PhD at the ET H Zurich with Prof A. Vasella. In his subsequent 20-year medicinal chemist ry career he has made significant contributions to the discovery of over 3 0 leads and 15 pre-clinical candidates\, of which 7 progressed to IND and 5 so far to Phase 2 trials.\n\n1998-2008: GlaxoSmithKline in Harlow\, UK – positions of increasing responsibility\, becoming Head of Lead Discove ry for Neurology CEDD 2006-2008. \n2008-2010: Structural Genomics Consorti um at Oxford University\, PI for Chemical Biology and Project Manager for SGC’s Epigenetics Chemical Probes Consortium.\n2011-2019: Astex in Cambr idge\, UK\, VP and Head of Chemistry working on fragment-based drug discov ery in oncology and CNS\, responsible for all chemistry aspects up to IND. \n2019 (from July): AstraZeneca\, VP Global Head of Oncology Chemistry.\nF ellow of the Royal Society of Chemistry\, member of BMCS committee 2005-20 13 and Chemistry-Biology Interface Division Council 2011-2017.\nLecturer a t Oxford Life Science Interface DTC 2009-2012 & Wellcome Trust Drug Discov ery training course 2010-2018.\nSAB member\, Imperial College Chemical Bio logy CDT.\nCo-authored over 100 publications/patents and delivered over 40 invited lectures.\n URL:https://www.imperial.ac.uk/events/97432/dr-tom-d-heightman-vp-and-head- of-chemistry-astex-pharmaceuticals-uk/ DTSTART;TZID=Europe/London:20190625T113000 DTEND;TZID=Europe/London:20190625T130000 LOCATION:United Kingdom END:VEVENT BEGIN:VTIMEZONE TZID:Europe/London BEGIN:DAYLIGHT DTSTART:20190625T113000 TZNAME:BST TZOFFSETTO:+0100 TZOFFSETFROM:+0100 END:DAYLIGHT END:VTIMEZONE END:VCALENDAR