Peptide Based Drug Discovery for Human Disease Related Membrane Proteins

Peptide drugs are of medium size between small compounds and antibodies. They have many advantages of biological drugs and can also be efficiently large scale produced through chemical synthesis. The world annual revenue of peptide drugs has reached 70 billion dollars and its annual growth rate is as high as 12-14% in recent years. However, thelowstability,shortlife-timeinblood vessels and low membrane permeability of peptide drugs still preclude their wide applications. Aiming at these issues, we have developed and applied the new chemical methods, such as native chemical ligation, sulfurester replacements, palmytolation and mirrorimage protein production, to improve stability and drug affinity of peptide based drug candidates. At the same time, we are trying to obtain three dimensional structures of disease related membrane protein complexes with peptide based drug targets, to illustrate the peptide drug binding interface and physicchemistry mechanism of peptide’s influences to thesemembraneproteindrugtargets. All of these efforts could be applied to speed up high efficient peptide based drug discovery for nuero- or immuno- diseases.

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