Somatostatin receptor subtype

Law SF, Yasuda K, Bell GI, Reisine T. Gia3 and Goa selectively associate with the cloned somatostatin receptor subtype... 

Liapakis G, Fitzpatrick D, Hoeger C, Rivier ], Vandlen R, Reisine T. Identification of ligand binding determinants in the somatostatin receptor subtypes 1 and 2. J Biol Chern 1996 271 20331-20339. 

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. 

Pfeiffer, M., Koch, T., Schroder, H., et al. (2001) Homo- and heterodimerization of somatostatin receptor subtypes. Inactivation of sst(3) receptor function by heterodimerization with sst(2A). J. Biol. Client. 276,14027-14036. 

Roth, A., Kreienkamp, H. J., Meyerhof, W., and Richter, D. (1997) Phosphorylation of four amino acid residues in the carboxyl terminus of the rat somatostatin receptor subtype 3 is crucial for its desensitization and intemahzation. J. Biol. Chem. 272, 23769-23774. 

Souers AJ, VirgiUo AA, Rosenquist A, et al. Identification of a potent heterocychc hgand to somatostatin receptor subtype-5 by the synthesis and screening of f -tum mimetic hbraries. / Am Chem Soc 1999 121 1817-25. 

Positron emission tomography Single-photon-emission computerized tomography Somatostatin receptor Somatostatin receptor subtype 2 Octreotate... 

Figure 2.18 The tetradecapeptide somatostatin is a nanomolar-to-subnanomolar ligand of five different somatostatin receptor subtypes. Compounds 62-66 are structurally simplified analogs from four combinatorial libraries, with up to 350 000 members per library. Each compound shows a remarkable selectivity against the different sstl-sst5 receptor subtypes (Table 2.1). The orientation of the compounds follows a projection of their superposition with a Merck cyclopeptide.

Table 2.1 Somatostatin receptor subtype affinities of the tetradecapeptide somatostatin (Ki values in nM) and compounds 62-66 (Figure 2.18 Kd values in nM) [34].

Veber et al. (31) This approach yielded five compounds (73-77) (Fig. 15.33), each being selective for one of the somatostatin receptor subtypes sstl (73), sst2 (74), sst3 (76), sst4 (76), and sst5 (77). 

Sandoval KE, Farr SA, Banks WA, Crider AM, Morley JE, Witt KA (2013) Somatostatin receptor subtype-4 agonist NNC 26-9100 mitigates the effect of soluble A(3(42) oligomers via a metalloproteinase-dependent mechanism. Brain Res 1520 145-156... 

Other more recent examples of new receptor subtypes include neurokinin, melanocortin and somatostatin receptor subtypes. Neurokinins (substance P, neurokinin A and neurokinin B) act at three receptor subtypes NKj, NKj and NK,. Selective ligands are being explored for the treatment of pain, asthma, depression, etc. The natural melanocortic peptides are derived from the precursor peptide pro-opiomelanocortin... 

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). 

HOFLAND, L.J., et al.. Crucial role for somatostatin receptor subtype 2 in determining the uptake of [Illln-DTPA-D-Phel]octreotide in somatostatin receptor-positive organs, J. Nucl. Med. 44 (2003) 1315-1321. 

While exhibits attractive nuclear properties for targeted radiotherapy (half-life 8.04 d Eoninx v 0-97 MeV (89%), 0.096 MeV (7%) and two gamma photons, 364 keV (81%) and 284 keV (6%)), wider application of 4 labelled somatostatin analogues in radiotherapy targeting somatostatin receptor subtype 2 is hampered by certain drawbacks. First, the 1 based analogues... 

ABmities of somatostatin analogues for somatostatin receptor subtype 2... 

FIG. 6.6. Comparative displacement curves of [ I-Tyr ] octreotide from somatostatin receptor subtype 2 in AR42J cell membranes with increasing concentrations of TATE, Sugar-TATE and DOTATATE. 

---