Somatostatin and its Analogs

Author(s): Lichun Sun, David H. Coy

Journal Name: Current Drug Targets

Volume 17 , Issue 5 , 2016

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Graphical 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

Keywords: Hormone, somatostatin, somatostatin analogs, somatostatin receptors, receptor-targeted.

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Article Details

Year: 2016
Published on: 03 March, 2016
Page: [529 - 537]
Pages: 9
DOI: 10.2174/1389450116666141205163548
Price: $65

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