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UID:69da13c4b4800
DTSTAMP:20260411T052628
DTSTART:20140924T110000
SEQUENCE:0
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DTEND:20140924T123000
URL:https://murmitoyen.com/events/vanille/udem/detail/453631
LOCATION:Polytechnique Montréal - Pavillon J.-Armand-Bombardier\, 5155\, a
 venue Decelles\, Montréal\, QC\, Canada\, H3T 2B1
SUMMARY:Conférence du Professeur Jeremy Wulff (Victoria)
DESCRIPTION:Titre : Synthesis of Conformationally-Controlled Polycycles for
  Use as Enzyme Inhibitor Scaffolds: a Case Study in the Engineering of Nov
 el Sialidase Inhibitors for Influenza and Cancer Treatment.La conférence 
 sera prononcée (en anglais) par le professeur Jeremy Wulff\, du départem
 ent de chimie de l'University of Victoria.Résumé : Conformational contro
 l of large inhibitors (for example by macrocyclization) is often found to 
 improve potency and reduce off-target binding. In principle\, internal rig
 idification of small molecule inhibitors should provide similar benefits\,
  but for various reasons this is less commonly practiced in the pharmaceut
 ical industry. In an academic setting\, however\, this strategy has the po
 tential to lead to more structurally-interesting targets (fun!) that come 
 with a number of improved pharmaceutical properties (useful!).   In this
  presentation\, we will describe a novel route to a growing family of conf
 ormationally-controlled bicyclic and tricyclic sulfones\, as well as the a
 pplication of those scaffolds to the creation of enzyme inhibitors that ad
 dress a key conformational problem in the field of influenza treatment. We
  will also present some very recent (and still not well understood) data o
 n the application of these inhibitors to the problem of selective sialidas
 e inhibition in cancer\, where we have identified one compound that revers
 ibly – and completely! – blocks the migration of prostate cancer cells
 . This marks the first time that a small molecule sialidase inhibitor has 
 been shown to affect cancer cell motility\, and opens the door to new fami
 lies of chemotherapeutics.Information supplémentaire
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