Target
Information |
Name | Somatostatin receptor type 3 |
Type of target | Clinical trial target |
Synonyms | SS3R |
SSR-28 |
Disease | Cushing's disease [ICD9: 255.0 ICD10: E24.0] | [1][2] |
Drug(s) | Pasireotide |  | Phase III | Pancreatic Cancer | [3] |
Pasireotide |  | Phase I | Neuroendocrine Tumor; Carcinoid Tumor; Pancreatic Neuroendocrine Tumor | [3] |
Pathway | Neuroactive ligand-receptor interaction |
UniProt ID | P32745 |
Function | Receptor for somatostatins-14 and -28. This receptor is coupled via pertussis toxin sensitive G proteins to inhibition of adenylyl cyclase. |
Sequence | MDMLHPSSVSTTSEPENASSAWPPDATLGNVSAGPSPAGLAVSGVLIPLVYLVVCVVGLL
GNSLVIYVVLRHTASPSVTNVYILNLALADELFMLGLPFLAAQNALSYWPFGSLMCRLVM
AVDGINQFTSIFCLTVMSVDRYLAVVHPTRSARWRTAPVARTVSAAVWVASAVVVLPVVV
FSGVPRGMSTCHMQWPEPAAAWRAGFIIYTAALGFFGPLLVICLCYLLIVVKVRSAGRRV
WAPSCQRRRRSERRVTRMVVAVVALFVLCWMPFYVLNIVNVVCPLPEEPAFFGLYFLVVA
LPYANSCANPILYGFLSYRFKQGFRRVLLRPSRRVRSQEPTVGPPEKTEEEDEEEEDGEE
SREGGKGKEMNGRVSQITQPGTSGQERPPSRVASKEQQLLPQEASTGEKSSTMRISYL//
|
Target Validation | Click to Find Target Validation Information. |
Inhibitor | CytotoxinPeptide Conjugate |  | [4] |
CytotoxinPeptide Conjugate |  | [4] |
CytotoxinPeptide Conjugate |  | [4] |
Des-AA1,2,4,12,13-[D-Trp8]SRIF |  | [5] |
Des-AA1,2,4,13-[D-Trp8]SRIF |  | [5] |
Des-AA1,2,4,5,10,12,13-[D-Trp8]SRIF |  | [5] |
Des-AA1,2,4,5,13-[D-Trp8]-SRIF |  | [5] |
Des-AA1,2,4,5-[D-Trp8]SRIF |  | [5] |
Des-AA1,2,5,12,13-[D-Trp8,IAmp9]SRIF |  | [5] |
Des-AA1,2,5,12,13-[D-Trp8]SRIF |  | [5] |
Des-AA1,2,5-[D-Trp8, (NalphaMe)IAmp9]SRIF |  | [6] |
Des-AA1,2,5-[D-Trp8,IAmp9,m-I-Tyr11]Cbm-SRIF |  | [6] |
Des-AA1,2,5-[D-Trp8,IAmp9]SRIF CH-275 |  | [6] |
Des-AA1,2,5-[D-Trp8,Tyr11]SRIF |  | [6] |
Des-AA1,4,5,13-[Tyr2,D-Trp8]-SRIF |  | [5] |
Des-AA1,5-[Tyr2,D-Trp8,IAmp9]Cbm-SRIF |  | [6] |
Des-AA5-[D-Trp8]SRIF |  | [6] |
Edotreotide |  | [7] |
H-D-Phe-c[Cys-Ala-D-Trp-Lys-Thr-Cys]-Thr-NH2 |  | [8] |
H-DPhe-c[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-NH2 |  | [8] |
ODT-8 |  | [5] |
Radiolabeled octreotide derivative |  | [7] |
Radiolabeled octreotide derivative |  | [7] |
Radiolabeled octreotide derivative |  | [7] |
Radiolabeled octreotide derivative |  | [7] |
Radiolabeled octreotide derivative |  | [7] |
Radiolabeled octreotide derivative |  | [7] |
Radiolabeled octreotide derivative |  | [7] |
Radiolabeled octreotide derivative |  | [7] |
Radiolabeled octreotide derivative |  | [7] |
Radiolabeled octreotide derivative |  | [7] |
Radiolabeled octreotide derivative |  | [7] |
Radiolabeled octreotide derivative |  | [7] |
Radiolabeled octreotide derivative |  | [7] |
SOMATOSTATIN |  | [9] |
SRIF-28 |  | [10] |
Somatostatin Analogue |  | [11] |
Somatostatin Analogue |  | [11] |
Somatostatin Analogue |  | [11] |
Somatostatin Analogue |  | [11] |
Agonist | Pasireotide |  | [3] |
Multitarget | Pasireotide |  | [3] |
Cross References |
3D Structure
Related Literature
On-Line
Medical Dictionary |
Ref 1 | The somatostatin analog SOM230 (pasireotide) ameliorates injury of the intestinal mucosa and increases survival after total-body irradiation by inhibiting exocrine pancreatic secretion. Radiat Res. 2009 Jun;171(6):698-707. To Reference |
Ref 2 | Somatostatin analog octreotide LAR in gastro-entero-pancreatic tumors. Expert Rev Anticancer Ther. 2009 May;9(5):557-66. To Reference |
Ref 3 | Treatment strategies for acromegaly. Expert Opin Emerg Drugs. 2005 Nov;10(4):875-90. To Reference |
Ref 4 | Bioorg Med Chem Lett. 2003 Mar 10;13(5):799-803.An adjustable release rate linking strategy for cytotoxin-peptide conjugates. To Reference |
Ref 5 | J Med Chem. 2005 Jan 27;48(2):515-22.Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides. To Reference |
Ref 6 | J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. To Reference |
Ref 7 | J Med Chem. 2005 Apr 21;48(8):2778-89.N-terminal sugar conjugation and C-terminal Thr-for-Thr(ol) exchange in radioiodinated Tyr3-octreotide: effect on cellular ligand trafficking in vitro and tumor accumulation in vivo. To Reference |
Ref 8 | J Med Chem. 2006 Jul 27;49(15):4487-96.Novel sst2-selective somatostatin agonists. Three-dimensional consensus structure by NMR. To Reference |
Ref 9 | J Med Chem. 2005 Oct 20;48(21):6643-52.Discovery of iodinated somatostatin analogues selective for hsst2 and hsst5 with excellent inhibition of growth hormone and prolactin release from rat pituitary cells. To Reference |
Ref 10 | J Med Chem. 2010 Aug 26;53(16):6188-97.Novel octreotide dicarba-analogues with high affinity and different selectivity for somatostatin receptors. To Reference |
Ref 11 | J Med Chem. 1999 Apr 22;42(8):1341-7.Comparison of four 64Cu-labeled somatostatin analogues in vitro and in a tumor-bearing rat model: evaluation of new derivatives for positron emission tomography imaging and targeted radiotherapy. To Reference |