Homepage for
Drug Discovery (CHEM-4330/6330)
and Drug Discovery Laboratory (CHEM-4340)
Instructor: Mark P. Wentland, Department of
Chemistry and Chemical Biology
CHEM-4330 (undergraduate) and
CHEM-6330 (graduate) will examine how bioinformatics, functional genomics and
other modern biotechnologies are used to speed the discovery of new drugs,
especially those small organic molecules to treat human diseases with large
unmet therapeutic need. Special emphasis will be placed on molecular target
identification and validation as well as high-throughput screening to identify
a lead. Topics to be discussed will include transgenic mice, RNA interference,
DNA and protein microarrays, homogenous time-resolved fluorescence bioassays,
phage-display, combinatorial chemistry and parallel synthesis. 3 credit hours.
Prerequisites - For CHEM-4330: CHEM-2220 or CHEM-2260 or permission of
instructor; for CHEM-6330: CHEM-6210 or permission of instructor.
CHEM-4340 (Drug Discovery Laboratory associated with CHEM-4330) enables
students to reduce to practice the chemical and biological aspects of
high-throughput screening used to discover lead molecules. Colorimetric and
fluorescence plate readers will be used in 96-well plate format to generate
enzyme inhibition data for small libraries of organic molecules. Students will
use these inhibition data and published X-ray structural data to develop a
pharmacophore model and rationalize a structure-activity relationship. 1 credit
hour. Prerequisite - CHEM-4330 or concurrent with CHEM-4330.
Course topics in graphical form.
Example of a lecture module: High Troughtput Screening (HTS)
Example of a laboratory experiment: 96-Well Plate
Colorimetric Assay for Ki
Determination of (±)-2-Benzylsuccinic Acid, an Inhibitor of Carboxypeptidase A
For enrolled students - detailed course information will be distributed via RPI LMS
Drug Discovery and DD Laboratory are required courses for Rensselaer's Bioinformatics
and Molecular Biology Major and are electives for Chemistry, Biology,
Biochemistry/Biophysics, and other majors.