Bioinformatics Tools for Pharmaceutical Drug Product Development

3Role of Bioinformatics in Peptide-Based Drug Design and Its Serum Stability

Vivek Chavda¹*, Prashant Kshirsagar² and Nildip Chauhan^2†

¹Department of Pharmaceutics and Pharmaceutical Technology, L M College of Pharmacy, Ahmedabad, India

²Drug Product Development, Enzene Biosciences Limited, Pune Maharashtra, India

Abstract

Naturally occurring peptides are becoming the area of interest in peptide dug design and development now a day. Peptides stability can be increased by changing both the end of terminal amino acid using its D-form by means of glyocylation, sulfation or phosphorylation on the tyrosine residue. Pegylation is one of the powerful processes to form a conjugation of peptide which turn into reducing immunogenicity and increasing water solubility. Several approaches are made to improve peptide stability while reducing proteolytic enzyme susceptibility. One of the approaches is to identify the site of proteolytic cleavage and incorporation of chemical modification by non-natural amino acid and replacement of amide bond. Other approaches are modification of N and C terminal end, cyclization of side chain or backbone or inclusion of peptide which will provide stabilization. Here, we are also focusing on the improvement of serum stability of the same.

Keywords: Peptides, serum stability, N-terminal and C-terminal amino acids, receptor

3.1 Introduction

Peptides are made up of amino acids, when amino acids in defined ordered linked through peptide bond and form a chain. ...