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Development of dendrimeric somatostatin analogues

Jolanta Dyniewicz 1,2Zofia Lipkowska 1,3Andrzej W. Lipkowski 1,2

1. Polish Scientific Network of Medicinal Chemistry of Peptides, Warsaw 02-106, Poland
2. Mossakowski Medical Research Centre, Polish Academy of Sciences, Pawińskiego 5, Warsaw 02-106, Poland
3. Polish Academy of Science, Institute of Organic Chemistry, Kasprzaka 44/52, Warsaw 01-224, Poland

Abstract

Low molecular weight dendrimeric peptides are very prospective compounds. Their terminal functional groups can be functionalized towards specific medical purpose. Cancer disease is in many countries primary cause of deaths. However, number of available therapies is still limited. In this field somatostatin analogues constitute new promising class of molecules targeting new type of receptor.

Somatostatin (SST) is a peptide that was originally characterized as a physiological inhibitor of growth hormone. In addition, SST has another multiple functions. It regulates endocrine and exocrine secretion, possesses antiproliferative properties and acts as a neurotransmitter/neuromodulator. These diverse physiological effects are mediated by a family of G-protein-coupled receptors, called somatostatin receptors sst1-sst5. Presently, there are several cyclic synthetic somatostatin analogues (eg octreotide, lanreotide), clinically used for cancer therapy and gastrointestinal disorders, that primarily ineract with receptors sst2.

Our goal is to use peptide dendrimers to design molecules with somatostatin-like biological activity. For this purpose, restricted somatostatin sequences have been attached to dendrimer branches in order to mimic topography of active structure(s) responsible for interactions with somatostatin receptors.

Acknowledgement: This project has been partially supported by grant from the Ministry of Science and High Education, N204 239436.

 

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Related papers

Presentation: Poster at VII Multidyscyplinarna Konferencja Nauki o Leku, by Jolanta Dyniewicz
See On-line Journal of VII Multidyscyplinarna Konferencja Nauki o Leku

Submitted: 2010-03-16 13:58
Revised:   2010-03-16 14:35