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DTSTART;TZID=Europe/Stockholm:20211208T140000
DTEND;TZID=Europe/Stockholm:20211208T150000
DTSTAMP:20260403T225250
CREATED:20211124T131507Z
LAST-MODIFIED:20211206T105940Z
UID:60019-1638972000-1638975600@www.scilifelab.se
SUMMARY:SciLifeLab Drug Discovery Seminar & DDD Exit event: Thomas Helleday
DESCRIPTION:Pharmacological targeting of MTHFD2 suppresses acute myeloid leukemia by inducing thymidine depletion and replication stress\n\n\n\n\n\n\n\nProfessor Thomas Helleday\, Karolinska Institutet \n\n\n\nSciLifeLab Drug Discovery Seminars\, hosted by the DDD platform\, is a series of educational lectures about recent developments\, technologies\, and trends in drug discovery and development that aims to enlighten\, and spark a discussion\, within the Swedish drug discovery community. \n\n\n\nAbstract \n\n\n\nThe folate metabolism enzyme MTHFD2 is consistently overexpressed in cancer but its roles are not fully characterized and current candidate inhibitors have limited potency for clinical development. Here we demonstrate a role for MTHFD2 in DNA replication and genomic stability in cancer cells\, and present optimised potent and selective nanomolar MTHFD2 inhibitors (MTHFD2i); protein co-crystal structures demonstrated binding to the active site of MTHFD2 and target engagement and that works in vitro and in vivo. \n\n\n\nThe results demonstrate a functional link between MTHFD2-dependent cancer metabolism and replication stress that can be exploited therapeutically with this new class of inhibitors. The work\, done in collaboration with the SciLifeLab DDD platform\, is accepted in the journal Nature Cancer and is the base for the creation of a new company: One-carbon therapeutics AB.  \n\n\n\nregistration
URL:https://www.scilifelab.se/event/scilifelab-drug-discovery-seminar-ddd-exit-event/
LOCATION:Air&Fire\, SciLifeLab Stockholm\, Tomtebodavägen 23A\, Solna\, Sweden
CATEGORIES:Event
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