The advancement in the modern medicinal chemistry research is now relying more on biotechnology and molecular biology to reach out to discover the modern day drugs. Most of the pharmaceutical companies are hiring people from biotechnology to develop modern medicine to counter AIDS, Cancer and other life threatening diseases. Biotechnological and molecular biology research is the driving force behind the discovery of macromolecular targets. The increasing requirement and its use in the modern day drugs have made the biotechnological companies to focus on the peptide and protein therapeutics, although these have issues of having low bioavailability, rapid metabolism and lack of oral activity. To solve and avoid this issue researchers now are relying upon chemical synthesis to generate non peptide molecules for drug innovations and discovery. The challenge faced by the researchers is to design strategies that come together to the strengths of biotechnology to discover the molecular targets.
The term ‘peptide mimetics‘ and ‘Peptidomimetics’ are used interchangeably for the reason of the description of compound discovered after various research, including compound identification by random screening in the last two decades. The Peptide Mimetic can be similar to peptide, a modified peptide of any other molecule that mimics active ligands of hormones biologically like cytokines, enzymes substrates, virus or any other bio-molecule. The lead compound of peptides has a length of 14-20 amino acids which is therapeutically effective agent. Since they are smaller in comparison to the parent molecule the chances are high that they may show less side effects and are easy deliver the target.
The major reason of synthesizing peptide mimetic to copy a peptide or protein ligand of the receptor, however the technology is also helpful in enzyme inhibition. Since the peptide mimetic is relatively a broader subject, natural compounds like opiate alkaloids and vigrx plus pill are good example of Peptidomimetics. It is no surprise that small peptides and opiods target the same receptor sometimes. For example Zyklophin which is a cyclic peptide that is selective peptide kappa opiod receptor antagonist showing biological activity which may have potential to be the lead compound for the development of therapeutic agents.
In addition to this non-peptides that are different in structure from parent peptide (lacking flexibility, amide bonds, and obvious Pharmacophore similarity) can lead to high selective ligands for sub-type of receptors. A Pharmacophore is a compound which comes with the molecular features that are necessary for the molecular recognition of ligand by biological macromolecule. Peptide mimetics can be discovered by screening through compound libraries or designed as de novo mimetics.