Peptide
Peptide designates short chains of amino acids linked through peptide bonds, typically ranging from two to approximately fifty amino acids, representing important biological molecules functioning as hormones, neurotransmitters, antimicrobial agents, and signalling molecules, while also serving as valuable therapeutic agents offering high specificity, potent activity, low toxicity, and rational design capabilities. The pharmaceutical industry has successfully developed numerous peptide therapeutics including insulin, GLP-1 agonists for diabetes and obesity, leuprolide for prostate cancer, and octreotide for acromegaly.
Drug development leverages peptide advantages including exquisite target selectivity, high potency, synthetic accessibility enabling rapid analogue generation, and generally favourable safety profiles. Challenges include proteolytic instability, poor oral bioavailability, short circulating half-lives, and manufacturing costs. Medicinal chemistry strategies address limitations through incorporating unnatural amino acids, cyclisation improving stability, fatty acid conjugation extending half-life through albumin binding, and PEGylation reducing renal clearance. Discovery approaches include rational design, high-throughput synthesis and screening of peptide libraries, phage display, and computational design. As chemical synthesis methods improve and delivery technologies enhance oral bioavailability or prolong action duration, peptide therapeutics continue expanding across therapeutic areas offering unique advantages bridging small molecules and protein biologics.
