Title:Somatostatin and its Analogs
Volume: 17
Issue: 5
Author(s): Lichun Sun and David H. Coy
Affiliation:
Keywords:
Hormone, somatostatin, somatostatin analogs, somatostatin receptors, receptor-targeted.
Abstract: Somatostatin (SST) is a cyclic hormone-release inhibitory peptide that has high binding affinity
to all of its five SST receptors (SSTRs). SST negatively regulates cell proliferation and the release
of multiple hormones via activation of its cognate receptors. A variety of SST analogs, some with
high affinity and selectivity of receptor subtypes, have been synthesized and developed. Certain longacting
SST analogs such as octreotide, lanreotide and pasireotide have been clinically applied to the
treatment of human diseases such as those caused by excessive release of growth hormone (acromegaly),
or adrenocorticotropic hormone (Cushing’s syndrome), and for the treatment of carcinoid syndrome. Investigations
into new biological activities of these long-acting SSTs and their possible clinical applications are also still ongoing.
Also, novel SST analogs are being designed and developed to target different receptor subtype(s) or mimic natural SST’s
multiple biological properties. Additionally, since SSTRs, especially SSTR2, are aberrantly expressed in many cancer
cells and tumor blood vessels, internalizing SST analogs is currently being used as drug-delivery vehicle for the application
of receptor-targeted therapeutics. This review will discuss recent advances in the development and applications of
SST and its analogs
