| Date |
Topic |
Notes |
Reading:
required and optional |
| |
Introductory material |
•Course_Syllabus
•Instructions for Final Paper |
•Drug design glossary;
•Petsko and Ringe
(from UMass sites only)
|
| T Jan 27 |
LMG: Introduction to course; Drug discovery timeline part 1 |
•Lecture1 pdf |
•Drug discovery tutorial;
•DrugResearcher.com |
| Th Jan 29 |
LMG: Introduction to protein-ligand binding |
•Lecture2 pdf |
•Drug discovery tutorial;
(up to Lead Opt/Med Chem)
•Petsko and Ringe
1.4, 1.9, 1.12, 1.14, 1.15,
2.1, 2.3, 2.4, 3.0-3.6 |
| T Feb 3 |
LMG: Physical methods in drug discovery |
•Lecture3 pdf |
•Petsko and Ringe
5.1-5.3
•Lim, Mayer, & Pawson
(update to Petsko & Ringe)
3.0-3.7, 3.10, 3.8-3.9
•Fluorescence html;
•Cooper SPR pdf;
•Freire ITC pdf;
•Blundell X-ray pdf;
•Giralt NMR pdf;
•Pellecchia NMR pdf
(or .doc version)
|
| Th Feb 5 |
SCG: Drug discovery timeline part 2: Lead optimization to clinical trials |
•Lecture4 pdf |
Drug discovery tutorial;
(from Lead Opt/Med Chem)
•Phase 1 mishap html;
•Phase 3 withdrawal html;
•ClinicalTrials.gov |
| T Feb 10 |
SCG: Pharmacokinetics and pharmacodynamics |
•Lecture5 pdf |
•Goodman chapt1 pdf;
|
| Th Feb 12 |
SCG: Introduction to transmembrane receptors |
•Lecture6 pdf |
•SSprang G prot primer pdf;
•Fillmore_GPCR_2004 pdf;
•Kroeze GPCR pdf
|
| T Feb 17 |
Quiz |
|
•Practice Quiz |
| Th Feb 19 |
Preston Hensley, Consultant: Drug Discovery Challenges |
•Hensley pdf |
•Pharma Report pdf |
| T Feb 24 |
Discussion: Drug discovery pipeline |
|
|
| Th Feb 26 |
Jean Lachowicz, Schering Plough Research Institute: GPCRs as Drug Targets |
•Lachowicz pdf
•Lachowicz_all pdf |
•Rodent learning pdf;
•GPCR structures 2009 pdf |
| T Mar 3 |
Discussion: GPCRs |
|
|
| Th Mar 5 |
Angela Cacace, Bristol-Myers Squibb: High Throughput Screening |
•Cacace pdf |
•HTS history pdf;
•HTS stats pdf;
•HTS assays pdf |
| T Mar 10 |
Discussion: HTS |
|
|
| Th Mar 12 |
Chris Lipinski, Melior Discovery: Reducing Lead Time |
•Lipinski pdf |
•Chemical space pdf;
•Network pharmacology pdf;
•Drug target numbers pdf;
•Outsourcing pdf;
•Lipinski profile;
•Lipinski laureation;
|
| |
Spring Break |
|
|
| T Mar 24 |
Discussion: Lead Time |
|
|
| Th Mar 26 |
Field Trip to Vertex Pharmaceuticals |
•Directions to Vertex pdf;
•Vertex schedule pdf |
|
| T Mar 31 |
Discussion: Field Trip |
|
|
| Th Apr 2 |
Jonathan Greer, Abbott: Structure-Based Drug Design |
|
•Fragment based DD pdf |
| T Apr 7 |
Discussion: Structure-based drug design |
|
|
| Th Apr 9 |
Pat Walters, Vertex: Combinatorial Libraries |
•Walters pdf |
•Virtual screening pdf;
•Chemical libraries pdf |
| T Apr 14 |
Discussion: Combinatorial libraries, computational chem |
|
|
| Th Apr 16 |
Joanna Swain, Adnexus: Protein Pharmaceuticals |
•Swain preview pdf |
•Alternate scaffolds pdf;
•Screening libraries pdf |
| T Apr 21 |
No Class: Monday class schedule |
|
|
| Th Apr 23 |
Discussion: Biologicals |
|
|
| T Apr 28 |
John Talley, Ironwood Pharma: Discovery and Development of COX-2 Inhibitors |
•Talley_2008 pdf;
•Talley_pdf |
•NSAIDs and NO pdf;
•NSAIDs and NO 2 pdf;
•Celecoxib cardio pdf;
•Ulcer study pdf;
•Celebrex clinical trial pdf;
•Binding studies pdf;
•Myocardial infarct pdf;
•Cardio risk pdf;
•Breast cancer pdf;
•Cox2 safety pdf;
•Forbes profile;
•Whitehead story |
| Th Apr 30 |
Discussion: Cox-2 inhibitors |
|
|
| T May 5 |
Stewart Fisher, Astra Zeneca: Identifying New Antibacterial Agents |
•Fisher pdf |
•MurI pdf;
•MurI review pdf |
| Th May 7 |
Discussion: Antibacterials |
|
|
| T May 12 |
Wrap up;
Papers due |
|
|
