| Date |
Topic |
Notes |
Reading:
required and optional |
| |
Introductory material |
•Course_Syllabus
•Instructions for Final Paper |
•Drug design glossary;
|
| T Jan 19 |
LMG: Introduction to course; Drug discovery timeline part 1 |
•Lecture1 pdf |
•Drug discovery tutorial;
•DrugResearcher.com |
| Th Jan 21 |
LMG: Introduction to protein-ligand binding |
•Lecture2 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
•updates 3.0, 3.1, 3.2
3.3, 3.4, 3.5, 3.6, 3.7,
3.8, 3.9, 3.10 |
| T Jan 26 |
LMG: Physical methods in drug discovery |
•Lecture3 pdf |
•Petsko and Ringe
5.1-5.3
•Fluorescence html;
•Cooper SPR pdf;
•Freire ITC pdf;
•Blundell X-ray pdf;
•Giralt NMR pdf;
•Pellecchia NMR pdf
(or .doc version)
|
| Th Jan 28 |
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 2 |
SCG: Pharmacokinetics and pharmacodynamics |
•Lecture5 pdf
•Lecture5 inked pdf |
•Goodman chapt1 pdf;
|
| Th Feb 4 |
SCG: Introduction to transmembrane receptors |
•Lecture6 pdf
•Lecture6 inked pdf |
•SSprang G prot primer pdf;
•Fillmore_GPCR_2004 pdf;
•Kroeze GPCR pdf;
•Petsko and Ringe
3.6-3.8, update 1-6
|
| T Feb 9 |
Quiz |
•2009 quiz
•2010 quiz key |
|
| Th Feb 11 |
Preston Hensley, Consultant: Drug Discovery Challenges |
•Hensley pdf (12 MB) |
|
| T Feb 16 |
No class: Monday class schedule |
|
|
| Th Feb 18 |
Discussion: Drug Discovery Challenges
Leaders: Will H., Jan P., Whitney S., Joe W.
|
|
|
| T Feb 23 |
Jonathan Greer, Abbott: Structure-Based Drug Design |
•Greer pdf (19 MB) |
•Anderson_2003 pdf;
•Petros_2006 pdf;
•Goodwill_2001 pdf;
•Hajduk_2007 pdf;
•NIH pub pdf (7 MB) |
| Th Feb 25 |
Discussion: Structure-based drug design
Leaders: Nilima K., Mark O, Minal P., Stephen P.
|
|
|
| T Mar 2 |
Pat Walters, Vertex: Computational chemistry |
•Walters pdf |
•Virtual screening pdf;
•Chemical libraries pdf |
| Th Mar 4 |
Discussion: Computational chemistry
Leaders: Andrew C., Dicky G., Sam N., Bryan S.
|
|
|
| T Mar 9 |
Chris Lipinski, Melior Discovery: Reducing Lead Time |
•Lipinski pdf |
•Hit-to-lead pdf;
•Online resources pdf |
| Th Mar 11 |
Discussion: Lead time
Leaders: Mariel F., Dan K., Jamie L., Fabian R., Daniel S.
|
|
|
| |
Spring Break |
|
|
| T Mar 23 |
Angela Cacace, Bristol-Myers Squibb: High Throughput Screening |
•Cacace pdf |
•HTS history pdf;
•HTS stats pdf;
•HTS assays pdf |
| Th Mar 25 |
Discussion: HTS
Leaders: Meenal D., Nick F., Adriana K., Lori M., Amit S.
|
|
|
| T Mar 30 |
Field Trip to Vertex Pharmaceuticals |
•Vertex Schedule pdf;
•Directions to Vertex
|
|
| Th Apr 1 |
Discussion: Field Trip
Leaders: Sean B., Caroline D., Josh G., Keith R., Joseph Y.
|
|
|
| T Apr 6 |
Joanna Swain, Adnexus: Protein Pharmaceuticals |
•Swain preview pdf |
•Fibronectin libraries pdf |
| Th Apr 8 |
Discussion: Biologicals
Leaders: Lindsay D., Kari F., Melissa F., Kaitlyn M., Katie S.
|
|
|
| T Apr 13 |
Alan Smith, Genzyme: Biologic Case Study |
•Smith CV pdf;
•Smith publications pdf |
|
| Th Apr 15 |
Frederick Monsma, Merck: GPCR Case Study |
•Monsma pdf |
•Orphan GPCRs pdf;
•oGPCR ligand pdf;
•GPCR antagonist pdf |
| T Apr 20 |
Discussion: Biologics
Leaders: Dave B., Christina M., Dave P., Serap P., Kristine P.
|
|
|
| Th Apr 22 |
Discussion: GPCRs
Leaders: Nick B., Brad D., John H, Amanda H., Steve M.
|
|
|
| T Apr 27 |
Stewart Fisher, Astra Zeneca: Identifying New Antibacterial Agents |
•Fisher pdf |
•MurI pdf;
•MurI review pdf |
| Th Apr 29 |
Discussion: Antibacterials
Leaders: Daniella G., Brendan J., Gladys M., Mark Z.
|
|
|
| T May 4 |
Wrap up;
Papers due |
Plagiarism links |
|
