TTD Target ID: TTDC00254

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

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Professor in Department of Pharmacy
National University of Singapore, Singapore

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