Peptide therapeutics has made tremendous progress in the past decade. Many
of the inherent weaknesses of peptides which hampered their development as therapeutics
are now more or less effectively tackled with recent scientific and technological advancements
in integrated drug discovery settings. These include recent developments in
synthetic organic chemistry, high-throughput recombinant production strategies, highresolution
analytical methods, high-throughput screening options, ingenious drug delivery
strategies and novel formulation preparations. Here, we will briefly describe the key
methodologies and strategies used in the therapeutic peptide development processes with
selected examples of the most recent developments in the field. The aim of this review is
to highlight the viable options a medicinal chemist may consider in order to improve a
specific pharmacological property of interest in a peptide lead entity and thereby rationally
assess the therapeutic potential this class of molecules possesses while they are traditionally
(and incorrectly) considered ‘undruggable’.