Mass Spectrometry of Proteins and Peptides in Drug Discovery

* Overview of protein mass spectrometry.

This chapter will give an overview on ionization methods, MS instrumentation and general strategies related to proteins / peptides analysis..

* Recombinant proteins and post-translationally modified proteins.

This chapter will present MS studies on characterization of recombinant proteins, therapeutic proteins, and post-translational modified proteins such as glycol-proteins, phosphorylated proteins. The discussion will also focus on micro-heterogeneity in protein bulk drug, specific strategies for enhancing yield of recombinant protein production..

* Proteomics in drug discovery.

This chapter will cover identification, quantification and characterization of proteins in global analysis of gene expression related to target proteins in drug discovery. These studies can provide comparative information on proteins and protein modifications found in disease samples with respect to those in healthy samples..

* Protein-ligand interaction and inhibitor screening.

This chapter will describe non-covalent complexes between target proteins and ligands as well as inhibitor screening in drug discovery..

* Proteins / peptides biomarkers.

This chapter will detail applications of biomarkers with respect to disease states, clinical experiments and toxicology studies..

* Microwave-assisted MS.

This chapter will illustrate principles and applications of microwave-assisted reactions, followed by mass spectrometric analysis in characterizing proteins and peptides. Using this novel approach, reactions (i.e. enzymatic digestion) can be carried out in minutes, in contrast to the hours required by conventional methods..

* Imaging MS.

This chapter will provide fundamentals and applications of imaging MS techniques in determining or mapping of proteins and peptides in tissue sections of biological samples. This is a relatively new technique which can be used to characterize the expression of proteins and other

Birendra N. Pramanik, PhD, was a Distinguished Fellow at Schering-Plough Research Institute (SPRI), where he directed the spectroscopy, mass spectrometry, and NMR programs.Guodong Chen, PhD, is Principal Scientist in Bioanalytical and Discovery Analytical Sciences at Bristol-Myers Squibb in Princeton, New Jersey. He heads a mass spectrometry group in support of drug discovery as well as development programs in small molecule pharmaceuticals and biologics.