CONFERENCE SERIES: Drug Targets

Recorded at: Discovery on Target

Digital Course: Allosteric Modulators of GPCRs

 

 



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About this Product: 

Allosteric modulators represent a novel paradigm to therapeutically target G-protein-coupled receptors (GPCRs). However, identification and characterization of allosteric modulators using standard functional assays remain elusive due to the ‘context-dependent phenomena’. This course will discuss important aspects of hit identification and validation of allosteric modulators in GPCR research activity.

 

 


 About this Product:
3 Presentations
88 Slides
Over 120 Minutes
Digital Download: $345.00
Single Copy: $345.00
Site License: $1380.00

Conference At A Glance: 

Background 

  • Advantages and disadvantages of allosteric modulators
  • General GPCR/Ligand Definitions: affinity, efficacy, EC50 shifting, models of receptor activation (ternary comples, etc.)
  • Binding vs functional assays
  • Mechanism validation (orthosteric, allosteric or bitopic)
  • Different types of allosteric modulators v. competitive antagonists: PAMs, NAMs, SAMs

Complexities and Challenges in Drug Discovery 

  • Modulation bias & context dependent pharmacology
  • HTS screening
  • In vitro strategies
  • In vivo strategies

Practicalities 

  • Making compounds and screening them
  • Molecular switches and flat/steep SAR
  • Multiple allosteric sites
  • Probe dependence
  • Dealing with functional heterodimers
  • Case study with mGLU R5

Speaker Biographies 

 Corey Hopkins Corey Hopkins, Research Assistant Professor of Pharmacology, Vanderbilt University
Corey Hopkins is Research Assistant Professor of Pharmacology at Vanderbilt University. He is an experienced and highly trained medicinal chemist who has extensive experience in all aspects of medicinal chemistry (hit-to-lead, lead identification, lead optimization, SAR, ADME, pre-IND studies). He is currently the chemistry team leader for the development of novel mGlu4 positive allosteric modulators for the treatment of Parkinson’s disease through a grant from the Michael J. Fox Foundation. In this capacity, Dr. Hopkins is responsible for all aspects of the chemistry effort (design of novel scaffolds, coordination in vitro/in vivo pharmacokinetic studies, in vivo biology studies). This program has now advanced to pre-IND studies for clinical candidate advancement with several compounds exhibiting significant effects in pre-clinical rodent models of PD along with promising pre-clinical toxicology studies. In addition to his efforts with the mGlu4 project, Dr. Hopkins oversees a team of chemists working on the development of novel M1 positive allosteric modulators for the potential treatment of the cognitive deficits in Alzheimer’s and schizophrenia. Dr. Hopkins has been involved in small molecule drug discovery in both industry and academia for more than a decade. As a medicinal chemist with Sanofi Pharmaceuticals he was a key contributor on a number of projects within the CNS, skeletal and inflammatory related therapeutic targets, such as multiple sclerosis, depression, rheumatoid arthritis and osteoporosis; culminating in several projects advancing into development status. During his graduate work, he worked on the total synthesis of complex natural products, synthetic methodology development, and pharmacophore profiling for Cdc25 phosphatase inhibitors. Dr. Hopkins has been the author or co-author on more than 30 original research manuscripts and more than 15 patents along with numerous review articles, book chapters and invited research talks. 

Stephan Schann, Ph.D., Head of Research, Research, Domain TherapeuticsStephan Schann
Stephan Schann currently holds the Head of Research position at Domain Therapeutics, a biopharmaceutical company focusing on GPCR drug discovery and early development. He is managing different projects from the gene to the preclinical candidate on targets such as mGluR4 PAM, mGluR2 NAM, mGluR3 PAM or GLP-1R PAM for CNS and metabolic indications. He is also responsible for DTect-All™, the technological platform used for drug discovery on challenging GPCRs. Before that, Stephan spent 6 years at Faust Pharmaceuticals, a CNS clinical biopharmaceutical company, where he set up the medicinal chemistry activity. Prior to his position at Faust, Stephan was Team Leader at EvotecOAI, Abingdon, UK from 2001 to 2003. Stephan received his PhD in medicinal chemistry from University de Strasbourg, France in 2001 working on the synthesis of the first imidazoline I1-selective ligands.

Debra KendallDebra Kendall, Distinguished Professor and Head of the Department of Pharmaceutical Sciences, University of Connecticut
Debra Kendall is Distinguished Professor and Head of the Department of Pharmaceutical Sciences at the University of Connecticut. The overall goal of her research is to understand the structure and function of the cannabinoid receptor family (CB1 and CB2). Her recent work includes examining the allosteric modulation of CB1 and she has identified examples of allosteric ligand biased signaling via G protein independent pathways. This includes distinguishing roles of β-arrestin 1 and β-arrestin 2 in this process. In collaboration with Dai Lu (Texas A&M Health Science Center), newly synthesized allosteric modulators have been characterized by SAR analysis and by studying the initial stages of signal transduction. Her laboratory has employed biophysical analyses using purified components as well as genetic and cellular analysis using whole cells. Her work is supported by NIH and is described in numerous journal publications. Dr. Kendall was elected a fellow of the American Association for the Advancement of Science (AAAS). She also has been the recipient of a National Science Foundation Career Advancement Award and is an appointed member of the Connecticut Academy of Arts and Sciences. She serves on several NIH study sections and she is on the editorial board of PLOS ONE. She earned her Ph.D. at Northwestern University and did postdoctoral work at the Rockefeller University.

Who may be interested in this product (titles):
Researchers, Scientists, Students, Post-docs, Professors, Group Leaders, Directors, Managers from Pharma, Biotechs, Contract Research Organizations, Academia and Government working in fields such as Cell Biology, Biology, Molecular Pharmacology, Drug Discovery, High throughput Screening, Assay Development, GPCR screening, Signal Transduction, Neuroscience, CNS, Diabetes, Cardio-Metabolic Diseases, Inflammation, Pain, Translational Medicine, Structure Based Design, Computational Chemistry, Discovery Chemistry.

About Discovery On Target:
Cambridge Healthtech Institute hosted its 11th Annual International Drug Discovery on Target meeting showcasing current and emerging "hot" targets for the pharmaceutical industry September 24-26, 2013 in Boston, MA. Spanning three days, the meeting attracted over 800+ attendees, composed of scientists/technologists, executives, directors, and managers from biopharma, academic, and healthcare organizations. The meeting is comprised of 12 meeting tracks which include Targeting Epigenetic Readers; Targeting Histone Methyltransferases; Next Generation Histone Deacetylase Inhibitors; Targeting Histone Demethylases; GPCR-Based Drug Discovery; GPCR-Targeted Therapeutics; Functional Genomics Screening Strategies; Novel Strategies for Kinase Inhibitors; Antibodies against Membrane Protein Targets, and Cardio-Metabolic Drug Targets. The 2013 event offered 150+ scientific presentations across these 12 conference tracks and 10 pre-conference short courses, 30+ interactive breakout discussion groups, an exhibit hall of 40+ companies, and dedicated poster viewing and networking sessions. The 11th Annual International Drug Discovery on Target assembles an impressive group of 175+ distinguished speakers who look forward to sharing their knowledge, best practices, and expertise with all attendees. Complete details can be found at www.DiscoveryOnTarget.com.

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The exhibit hall was sold out in 2013, so please contact us early to reserve your place. To customize your sponsorship or exhibit package for 2014, contact:

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CONFERENCES


October 8 – 9

Targeting Epigenetic Readers and
Chromatin Remodelers
 

Targeting the Ubiquitin Proteasome System  

Big Data Analytics and Solutions  

GPCR-Based Drug Discovery  

RNAi for Functional Genomics Screening
– Part 1
 

Protein-Protein Interactions as Drug Targets  

Antibodies Against Membrane Protein Targets
– Part 1
 


October 9 – 10

Targeting Histone Methyltransferases and Demethylases  

Screening Drug Transporter Proteins  

Maximizing Efficiency in Discovery  

GPCR-Targeted Therapeutics  

Genome Editing for Functional Genomics
Screens – Part 2
 

Cancer Metabolism  

Antibodies Against Membrane Protein Targets
– Part 2
 


SYMPOSIUM


October 7

Next Generation Histone Deacetylase Inhibitors  


SHORT COURSES


October 7

SC1: Designing Scalable Software Systems for Big Data Analytics  

SC2: Approaches for Biologically-Relevant Chemical Diversity  

SC3: Setting Up Effective RNAi Screens: From Design to Data to Validation  

SC4: Targeting Protein-Protein Interactions  

SC5: GPCR Structure-Based Drug Discovery  

SC6: Advances in Metagenomic Drug Discovery for New Anti-Infective Agents  

SC7: Targeting of GPCRs with Monoclonal Antibodies  

SC8: A Primer to Gene Editing: Tools and Applications  

SC9: Introduction to Targeted Covalent Inhibitors  


October 9

SC10: Setting Up Effective Functional Screens Using 3D Cell Cultures  

SC11: Integration of BDDCS and Extended Clearance Principles  

SC12: Introduction to Allosteric Modulators and Biased Ligands of GPCRs  

SC13: Introduction to Drug Metabolism