生长激素抑制素及其类似物

Title:Somatostatin and its Analogs

Volume: 17 Issue: 5

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

Affiliation:

关键词: 激素，生长激素抑制素，生长激素抑制素类似物，生长激素抑制素受体，靶向受体。

摘要: 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

Cite this article as:

Lichun Sun and David H. Coy , Somatostatin and its Analogs, Current Drug Targets 2016; 17 (5) . https://dx.doi.org/10.2174/1389450116666141205163548