COURSE

The GPCR Retreat is proud to offer it's first short course, run as a satellite to the GPCR Retreat itself. This year, the course will focus on generating and analyzing data to understand biased signalling from in vitro to in vivo. The coordinators of this short course are Michel Bouvier, Graciela Pineyro and Terry Hébert. It will feature a hands-on session using GraphPad Prism to analyze data.  You can provide your own or use the course data set which will be provided to you in due time. Further instructions will be send to registrants. 

DATE:   October 2nd, 2014 from 10:00 to 14:00 (the morning before
             the GPCR retreat)

REGISTRATION FEES:    GPCR Retreat registrant ________ Free
                                   Academic Attendee ____________ $100
                                   Non-Academic Attendee ________ $350

HOW TO REGISTER:

  • GPCR Retreat Registrant: Check the appropriate box in the registration site here
  • Other Attendees:  Download and fill the registration form.


COURSE PROGRAM

10:00     Welcome 
            Course organizers: Michel Bouvier, Graciela Pineyro and Terry Hébert

10:10     The concept of biased signalling and detection using label-free methods 
            Michel Bouvier, Université de Montréal

10:40      Use of standard assays and biosensors to identify signalling bias 
             Terry Hébert, McGill University

11:10      Analysing signalling data to quantify pharmacological bias.
             Graciela Pineyro, Université de Montréal

11:40       Advantages and disadvantages of different methods to quantify bias;
              conceptual and practical considerations

              Ongun Onaran, Ankara University, Turkey

12:10       Validating an established signalling signature in vivo
              Conrad Cowan, Trevena Inc.

12:40       Biased signalling in drug discovery: promises and challenges
              Patrick Sexton, Monash University, Autralia

13:10       Hands on training for analysis of biased signalling using PRISM 
              Course lecturers


You can download the slides of the each session of the course by clicking on:

 


PREPARATION FOR THE COURSE

Below you will find a list of suggested readings that will prepare you for our discussions. If you cannot download them, please contact Terry Hébert (terence.hebert@mcgill.ca). 

Bring your laptops if you intend to participate in the hands-on data analysis session. You should also download a copy of Prism version 6 (http://www.graphpad.com/demos/)  for this session if you don’t already have it. It can be downloaded on a free trial basis for 30 days, so we recommend that you download the trial copy in mid-September.

 Closer to the date of the course, we will provide a data set that you can use.

As part of your take home materials, we will also make our slide sets available to you after the course.

 

READINGS

Kenakin, T. and Christoulos, A. (2013)  Signalling bias in new drug discovery: detection, quantification and therapeutic impact. Nature Rev. Drug Disc. 12:205-216

Violin, J.D. et al., (2014) Biased ligands at G-protein-coupled receptors: promise and progress. Trends Pharmacol. Sci. 35:308-316

Rominger, D.H. et al., (2014) Biased ligands: pathway validation for novel GPCR therapeutics. Curr. Opin. Pharmacol. 1Impedance Responses Reveal b2-Adrenergic Receptor Signaling Pluridimensionality and Allow Classification of Ligands with Distinct Signaling Profiles. PloS ONE 7:e29420

Stallert, W. et al, (2012). Impedance Responses Reveal b2-Adrenergic Receptor Signaling Pluridimensionality and Allow Classificaion of Ligands with Distinct Signaling Profiles. PloS ONE 7:e29429. 

Charfi, I. et al., (2014) Identifying ligand-specific signalling within biased responses: focus on δ opioid receptor ligands. Br. J. Pharmacol., in press- doi: 10.1111/bph.12705.

van der Westhuizen, E.T. et al., (2014) Quantification of Ligand Bias for Clinically Relevant b2-Adrenergic Receptor Ligands: Implications for Drug Taxonomy. Mol. Pharmacol. 85:492-509

Soergel, D.G. et al., (2014a) First clinical experience with TRV130: pharmacokinetics and pharmacodynamics in healthy volunteers. J. Clinic Pharmacol. 54:351-357 

Soergel, D.G. et al., (2014b). Biased agonism of the u-opioid receptor by TRV130 increases analgesia and reduces on-target adverse effects versus morphine: A randomized, double-blind, placebo-controlled, crossover study in healthy volonteers. Pain. In press DOI:10.1016/j.pain.2014.06.011

DeWire, S.M. et al (2013). A G protein-biased ligand at the u-opioid receptor is potently analgesic with reduced gastrointestinal and respiratory dysfunction compared with morphine. J. Pharmacol Exp Ther 344:708-717.

   © 2014 GPCR Retreat                                                                                           Contact us at mail@gpcr-retreat.com