| Date |
Topic |
Notes |
Reading:
required and optional |
| |
Introductory material |
•Course_syllabus
•Example summary
•Plagiarism links
|
•Drug design glossary;
|
| T Jan 22 |
JAH: Introduction to course; Drug discovery timeline part 1 |
•Lec1 pdf |
•Drug discovery tutorial;
•Behind the surge |
| Th Jan 24 |
JAH: Introduction to protein-ligand binding |
•Lec2 pdf |
•Drug discovery tutorial;
(up to Lead Opt/Med Chem)
•Petsko and Ringe
1.4, 1.12, 1.14, 1.15, 1.16,
2.1, 2.3, 2.4, 3.1, 4.9, 5.1-5.3
•updates 3.0, 3.1, 3.2
3.3, 3.4, 3.5, 3.6, 3.7,
3.8, 3.9, 3.10
•Fluorescence html;
•Cooper SPR pdf;
•Freire ITC pdf;
•Blundell X-ray pdf;
•Giralt NMR pdf;
•Pellecchia NMR pdf |
| T Jan 29 |
SCG: Drug discovery timeline part 2: Lead optimization to clinical trials |
•Lec3 pdf |
•Drug discovery tutorial;
(from Lead Opt/Med Chem)
•Phase 1 mishap html;
•Phase 3 withdrawal html;
•Vertex HCV fast track
•ClinicalTrials.gov |
| Th Jan 31 |
SCG: Pharmacokinetics and pharmacodynamics |
•Lec4 pdf |
•Goodman chapt1 pdf;
•PK applets
•Tox red flags |
| T Feb 5 |
SCG: Introduction to transmembrane receptors |
•Lec5 pdf |
•SSprang G prot primer pdf;
•Fillmore_GPCR_2004 pdf;
•Rasmussen_2011 pdf;
•Kroeze GPCR pdf;
•Petsko and Ringe
3.6-3.8, update 1-6
|
| Th Feb 7 |
Meaghan Richmond, AstraZeneca: Patents and Intellectual Property |
•Patent example 1
•Patent example 2 |
•Patents in Pharma
•Patents at the Core
•OHC_Pharma
•Genetics and Patenting
•Protecting the Assets
•Critics Target Patent Deals |
| T Feb 12 |
Mark Murcko, Disruptive Biomedical: Overview of Drug Discovery |
•Murcko pdf (50MB) |
|
| Th Feb 14 |
Discussion: Richmond & Murcko
Discussion leaders: Nate B, Lola F, Mine C, & Katrina R
|
|
|
| T Feb 19 |
No class meeting: Monday class schedule |
|
|
| Th Feb 21 |
Beth Garner, Abbott: HPV Vaccine Development
Note: Special time 9am!
(Video repeat of talk shown at 1pm)
|
•Garner 2012 pdf;
•Garner 2013 pdf |
•HPV strategy pdf;
•HPV vaccine trial pdf;
•HPV phase 4 pdf |
| T Feb 26 |
Discussion: Garner
Discussion leaders: Brett H, Dan D, Jeff B, & Dana T
|
|
|
| Th Feb 28 |
Quiz
|
•2012 Quiz |
|
| T Mar 5 |
Martyn Banks, Bristol-Myers Squibb: High-Throughput Screening |
•Banks pdf |
•HTS trends pdf;
•HTS robotics pdf;
•High content screening pdf;
•Compound management pdf |
| Th Mar 7 |
Discussion: Banks
Discussion leader: Carolyn C, Sam K, Stephanie M, & Maureen H
|
|
|
| T Mar 12 |
Chris Lipinski, Melior Discovery: Reducing Lead Time |
•Lipinski pdf
•Lipinski essay pdf |
•Hit-to-lead pdf;
•False positives pdf |
| Th Mar 14 |
Discussion: Lipinski
Discussion leaders: Derek M, Ketan M, Sarah T, Singyuk H, & Xin L
|
|
|
| |
Spring Break |
|
|
| T Mar 26 |
Joanna Swain, Adnexus: Protein Pharmaceuticals |
•Swain 2009 pdf |
•Adnectins pdf |
| Th Mar 28 |
Discussion: Swain
Discussion leaders: Jake P, Emily S, Lydia L, & Brittany deR
|
|
|
| T Apr 2 |
Ravi Kurumbail, Pfizer: Applications of Structure-Based Drug Design
|
•Kurumbail pdf |
•South_2003 pdf;
•Kurumbail_1996 pdf; |
| Th Apr 4 |
Discussion: Kurumbail
Discussion leaders: Karan H, Kari P, Fatih C, David S, & Matt M
|
|
|
| F Apr 5 |
Field Trip to Vertex Pharmaceuticals (optional) |
•Directions to Vertex
•Vertex schedule |
|
| T Apr 9 |
Discussion: Vertex trip
Discussion leaders: Max N, Danielle L, Bib Y, Scott D, & Anthony M
|
|
|
| Th Apr 11 |
No class meeting |
|
|
| T Apr 16 |
Woody Sherman, Schrödinger: Computational Chemistry |
|
•Improving selectivity pdf;
•Molecular interactions pdf
|
| Th Apr 18 |
Discussion: Sherman
Discussion leaders: Jing L, Keith B, YingQi Z, & Yunlong Z
|
|
|
| T Apr 23 |
Thomas Keating, AstraZeneca: Infectious Disease Drug Discovery |
•Keating pdf |
•TMK validation pdf;
•Sulfonylpiperidines pdf;
•TMK inhibitors pdf |
| Th Apr 25 |
Discussion: Keating
Discussion leaders: Vanessa C, Sally C, Kristina B, & Andrew S
|
|
|
| T Apr 30 |
Wrap up
|
•Exam docx |
|
