Peptides and proteins are essential to many biological processes. The interaction between the peptide ligands and their receptor targets commonly involves beta-turn structures. Yet poor bioavailability and unfavorable pharmacokinetics significantly compromise the use of peptides as drugs. Thus, there has been a great deal of interest in the design of peptidomimetics (modified peptides) as therapeutic agents by mimicking beta-turn structures. This review highlights the importance of beta-turn in the design of various peptidomimetics for many diseases. This review also outlines several beta-turn mimicking strategies and its application in the design of potent peptide analogues. beta-turn mimetics often tend to be more rigid in positioning the critically important amino acid residues and thus optimize the surface conformation for productive interaction with the receptors.