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UID:69dd7b39e93a5
DTSTAMP:20260413T192441
DTSTART:20151202T110000
SEQUENCE:0
TRANSP:OPAQUE
DTEND:20151202T123000
URL:https://murmitoyen.com/events/vanille/udem/detail/624078
LOCATION:Université de Montréal - Pavillon Roger-Gaudry\, 2900\, chemin d
 e la Tour\, Montréal\, QC\, Canada\, H3T 1J6
SUMMARY:Conférence du Professeur Andrei Yudin (Toronto)
DESCRIPTION:Titre : Advances in Peptide Macrocyclization.Endroit : Pavillon
  Roger-Gaudry\, salle G-815 à 11 h.Hôte : Professeur William Lubell.
\nL
 a conférence sera prononcée (en anglais) par le professeur Andrei Yudin\
 , du Département de chimie de l'University of Toronto.
\nRésumé : Macro
 cycles are a class of molecules that continue to attract attention as ther
 apeutic agents and chemical probes. We have developed a synthetic chemistr
 y platform that allows us to streamline the discovery and development of b
 ioactive macrocycles. While this class of molecules is promising\, it does
  present challenges that are atypical for small molecule drugs. The main i
 ssue is that the structural properties responsible for cellular permeabili
 ty of macrocycles are not correlated with those that are responsible for t
 arget engagement. We have identified some emerging principles that govern 
 the behavior of peptide macrocycles obtained through the use of aziridine 
 aldehydes. In addition\, we recently discovered a macrocyclization reactio
 n that results in the installation of unsaturated heterocycles within the 
 large ring frameworks. In this lecture\, I will illuminate our ongoing stu
 dies aimed at the design of integrin inhibitors and will discuss some coun
 terintuitive findings that were made when we attempted to control over cel
 lular permeability. The main lesson is that well-behaved structure-activit
 y relationships are less likely for macrocycles when compared to small mol
 ecules. This lack of predictability will continue to fuel this area of res
 earch for many years.
\nInformation supplémentaireAnnonce PDF de la conf
 érence
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