Somatostatin receptors, human

Sun L., Fuselier J.A., Murphy W.A., Coy D.H. Antisense peptide nucleic acids conjugated to somatostatin analogs and targeted at the n-myc oncogene display enhanced cytotoxity to human neuroblastoma 1M.R.32 cells expressing somatostatin receptors. Peptides 2002 23 1557-1565. 

Patel, R. C., Lange, D. C. and Patel, Y. C. (2002). Photobleaching fluorescence resonance energy transfer reveals ligand-induced oligomer formation of human somatostatin receptor subtypes. Methods 27, 340-8. 

Teijeiro R, Bios R, Costoya JA et al (2002) Activation of human somatostatin receptor 2 promotes apoptosis through a mechanism that is independent from induction of p53. Cell Physiol Biochem 12 31-38... 

K. Gademann, M. Ernst, D. Seebach, D. Hoyer, The Cyclo-P-Tetrapeptide (P-HPhe-p-HThr-P-HLys-P-HTrp) Synthesis, NMR Structure in Methanol Solution, and Affinity for Human Somatostatin Receptors , Helv. Chim. Acta 2000, 83, 16 - 33. 

D. Seebach, M. Rueping, P. I. Arvidsson, T. Kimmerlin, P. Micuch, C. Noti, D. Langenegger, D. Hoyer, Linear, Peptidase-Resistant p /p -Di-and o/p -Tetrapeptide Derivatives with Nano-molar Affinities to a Human Somatostatin Receptor , Helv. Chem. Acta 2001,84,3503-3510. 

Fig. 1 Primary amino acid sequence comparison between five members of the human somatostatin receptor family. The amino acid sequences are aligned, using the single-letter amino acid code. Gaps introduced in the sequences to optimize the alignments are represented with dashes (-). The boxes indicate amino acids that are identical in all five receptor subtypes. The highest level of homology occurs within the seven canonical transmembrane domains of the human SST receptors (indicated above the sequences) and these domains have been derived by a combination of hydropathy analysis and comparison with the transmembrane domains of the other G-protein coupled receptors. The high level of homology among the members of the SST receptor family in the seven membrane spanning domains is shared by other G-protein coupled receptors that are coupled to inhibition of adenylyl cyclase.

Dimech, J. et al. (1993) Antagonist effects of seglitide (MK 678) at somatostatin receptors in guinea-pig isolated right atria. Br. J. Pharmacol.. 109.898-899. Wilkinson. G.F. et al. (1996) Potent antagonism by BlM-23056 at the human recombinant somatostatin ssts receptor. Br.J. Pharmacol.. 118, 445-447. Alexander. S.P.H. et al. (1998) Receptors and ion channel nomenclature supplement. Ninth Edition. Trends Pharmacol. Set.. Suppl., 19,1-98. 

REUBI, J.C., et al., Affinity profiles for human somatostatin receptors subtypes SST1-SST5 of somatostatin radiotracers selected for scintigraphic and radio-therapeutic use, Eur. J. Nucl. Med. 27 (2000) 273-282. 

DOTATATE is an octapeptide somatostatin analogue that can bind to the human somatostatin receptor subtypes with high affinity. It was obtained commercially from piCHEM R D (Austria). 

Somatostatin receptors are known to be overexpressed in various types of human tumour, hence radiopharmaceuticals seeking those receptors are widely considered for targeted tumour therapy. To date, five somatostatin receptor... 

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