Principles of Drug Discovery

THEORY 1.

An overview of modern drug discovery process:

Target identification, target validation, lead identification and lead Optimization. Economics of drug discovery.

Target Discovery and validation-Role of Genomics, Proteomics and Bioinformatics.

Role of Nucleic acid microarrays, Protein microarrays, Antisense technologies, siRNAs, antisense oligonucleotides, Zinc finger proteins. Role of transgenic animals in target validation.

Lead Identification- combinatorial chemistry & high throughput screening, in silico lead discovery techniques, Assay development for hit identification.

Protein structure Levels of protein structure, Domains, motifs, and folds in protein structure. Computational prediction of protein structure: Threading and homology modeling methods. Application of NMR and X-ray crystallography in protein structure prediction Rational Drug Design Traditional vs rational drug design, Methods followed in traditional drug design, High throughput screening, Concepts of Rational Drug Design, Rational Drug Design Methods: Structure and Pharmacophore based approaches Hrs Hrs Hrs Virtual Screening techniques: Drug likeness screening, Concept of pharmacophore