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PRODID:https://murmitoyen.com/events/vanille/udem/
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UID:69e1cb5251d03
DTSTAMP:20260417T015530
DTSTART:20121001T150000
SEQUENCE:0
TRANSP:OPAQUE
DTEND:20121001T163000
URL:https://murmitoyen.com/events/vanille/udem/detail/143952
LOCATION:Université de Montréal - Pavillon J.-Armand-Bombardier\, 5155\, 
 chemin de la rampe \, Montréal\, QC\, Canada\, H3T 2B2
SUMMARY:Conférence du Professeur David Perrin (UBC)
DESCRIPTION:Titre: Using Boron to Label Peptides with 18F for Functional Ca
 ncer Imaging: The Quest for Kinetic Stability.Cette conférence sera prono
 ncée par le professeur David Perrin du Département de chimie de l'Univer
 sity of British Columbia. Ce dernier sera à Montréal à titre d'examinat
 eur externe d'une soutenance de thèse en chimie.Résumé : By providing h
 igh spatial and temporal resolution in vivo images\, PET imaging will help
  us realize the promise of personalized molecular medicine. Whereas the va
 rious nuclear properties make F18 a choice PET isotope\, the chemical prop
 erties of fluoride complicate its use in biomolecular labelling such that 
 2-4 'hot' steps are required. Given the relatively short half-life of F18 
 (110 minutes)\, a rapid 1-step\, reproducible\, clean\, and high yielding 
 aqueous labelling of an intact biomolecule would be desirable. We hypothes
 ized that biomolecules could be labelled via a pendent boronic ester in a 
 single aqueous step whereby chemoselective F18-capture gives an in vivo st
 able F18-labeled aryltrifluoroborate. While the B-F bond is considered to 
 be one of the strongest single bonds on the periodic table\, we used 19F-N
 MR and radioactive 18F-19F isotopic exchange assays to demonstrate that th
 e B-F bond can be surprisingly labile\, yet tuneable through chemical synt
 hesis for applications in PET. Our findings have mechanistic implications 
 for metal-mediated cross couplings and provide a rubric for developing a n
 ew class of boron reagents for expeditious PET 18F-labeling. Hence\, we la
 belled the drug Marimastat\, a potent MMP (matrix metalloprotease) inhibit
 or to provide the first images of MMP activity in metastatic breast cancer
  xenografts.  This approach now works with LLP2A\, RGD\, diamino-acid ure
 as\, folic acid\, oligos\, and biotin\, all of which are important imaging
  agents. Click reactions are also possible and taken together these result
 s suggests that boron represents a viable platform for labelling most larg
 e biomolecules. Our talk will start with fundamental results obtained to u
 nderstand the aqueous stability of aryltrifluoroborates. These results the
 n guided the synthetic design of substructures for use in PET imaging. Our
  talk will end with in vivo PET images of cancer in mice Information suppl
 émentaire
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TZID:America/Montreal
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