UMass Amherst
   Chem/Biochem 597A: Drug Design Spring 08
T&Th 1:00-2:15pm
LGRT 1634

Instructors:   Lila M. Gierasch (gierasch@biochem.umass.edu, 1224 Lederle Tower, 5-6094)
  Scott C. Garman (garman@biochem.umass.edu, 1021K Lederle Tower, 7-4488)

Today is
Glossary

 

Date Topic Notes

Reading:

required and optional

  Introductory material Course_Syllabus
Drug design glossary;
Petsko and Ringe
   (from UMass sites only)
T Jan 29 LMG: Introduction to course; Drug discovery timeline part 1 Lecture1 pdf Drug discovery tutorial;
DrugResearcher.com
Th Jan 31 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 5 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 7 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 12 SCG: Pharmacokinetics and pharmacodynamics Lecture5 pdf Goodman chapt1 pdf;
Th Feb 14 SCG: Introduction to transmembrane receptors Lecture6 pdf SSprang G prot primer pdf;
Fillmore_GPCR_2004 pdf;
Kroeze GPCR pdf
T Feb 19 No class; Monday class schedule    
Th Feb 21 Quiz Instructions for Final Paper Practice Quiz
T Feb 26 Preston Hensley, Pfizer: Drug Discovery Challenges Hensley pdf Pharma Report pdf
Th Feb 28 Discussion: Drug discovery pipeline    
T Mar 4 Jonathan Greer, Abbott: Structure-Based Drug Design Greer pdf Fragment based DD pdf
Th Mar 6 Discussion: Structure-based drug design    
T Mar 11 Angela Cacace, Bristol-Myers Squibb: High Throughput Screening

Cacace pdf;

Cacace actual pdf

HTS history pdf;
HTS stats pdf
Th Mar 13 Discussion: HTS    
  Spring Break    
T Mar 25 Chris Lipinski, Melior Discovery: Reducing Lead Time Lipinski pdf Chemical space pdf
Th Mar 27 Discussion: Lead time    
T Apr 1 Pat Walters, Vertex: Combinatorial Libraries Walters pdf Virtual screening pdf;
Chemical libraries pdf
Th Apr 3 Discussion: Combinatorial libraries, computational chem    
T Apr 8 Field Trip to Vertex Pharmaceuticals Directions to Vertex pdf Vertex schedule pdf
Th Apr 10 Discussion    
T Apr 15 Jean Lachowicz, Schering Plough Research Institute: GPCRs as Drug Targets Lachowicz pdf Rodent learning pdf
Th Apr 17 Discussion: GPCRs    
T Apr 22 Joanna Swain, Adnexus: Protein Pharmaceuticals Swain pdf Protein therapeutics pdf
Th Apr 24 Discussion: Biologicals    
T Apr 29 John Talley, Ironwood Pharma: Discovery and Development of COX-2 Inhibitors Talley 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 May 1 Discussion: Cox-2 inhibitors    
T May 6 Stewart Fisher, Astra Zeneca: Identifying New Antibacterial Agents Fisher pdf MurI pdf
Th May 8 Discussion: Antibacterials    
T May 13 Wrap up;
Papers due
   

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