Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTJX3UE)

• DTT Name: Somatostatin receptor type 3 (SSTR3)
• Synonyms: SSTR3; SSR-28; SS3R
• Gene Name: SSTR3
• DTT Type: Successful target; [1]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: SSR3_HUMAN
• TTD ID: T13644
• Sequence:
  MDMLHPSSVSTTSEPENASSAWPPDATLGNVSAGPSPAGLAVSGVLIPLVYLVVCVVGLL
  GNSLVIYVVLRHTASPSVTNVYILNLALADELFMLGLPFLAAQNALSYWPFGSLMCRLVM
  AVDGINQFTSIFCLTVMSVDRYLAVVHPTRSARWRTAPVARTVSAAVWVASAVVVLPVVV
  FSGVPRGMSTCHMQWPEPAAAWRAGFIIYTAALGFFGPLLVICLCYLLIVVKVRSAGRRV
  WAPSCQRRRRSERRVTRMVVAVVALFVLCWMPFYVLNIVNVVCPLPEEPAFFGLYFLVVA
  LPYANSCANPILYGFLSYRFKQGFRRVLLRPSRRVRSQEPTVGPPEKTEEEDEEEEDGEE
  SREGGKGKEMNGRVSQITQPGTSGQERPPSRVASKEQQLLPQEASTGEKSSTMRISYL
• Function: Receptor for somatostatin-14 and -28. This receptor is coupled via pertussis toxin sensitive G proteins to inhibition of adenylyl cyclase.
• KEGG Pathway: Neuroactive ligand-receptor interaction (hsa04080)
• Reactome Pathway:
  G alpha (i) signalling events (R-HSA-418594)
  Peptide ligand-binding receptors (R-HSA-375276)

Molecular Interaction Atlas (MIA) of This DTT

1 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Pasireotide	DMHM7JS	Cushing disease	5A70	Approved	[1]

1 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ODT-8	DMBWO5T	N. A.	N. A.	Phase 3	[2]

1 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
FR-121196	DMNRUGA	Alzheimer disease	8A20	Terminated	[3]

26 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
99mTc-MIP-1407	DMYPD5L	Neuroendocrine cancer	2B72.1	Investigative	[3]
BN-81,644	DM1CNU5	Discovery agent	N.A.	Investigative	[4]
BN-81,674	DM7RPQ4	Discovery agent	N.A.	Investigative	[4]
CGP 23996	DMTECXA	Discovery agent	N.A.	Investigative	[5]
Cytotoxin Peptide Conjugate	DM7SVLZ	Discovery agent	N.A.	Investigative	[6]
Des-AA1,2,4,12,13-[D-Trp8]SRIF	DMMWDC5	Discovery agent	N.A.	Investigative	[2]
Des-AA1,2,4,13-[D-Trp8]SRIF	DMR6Z2N	Discovery agent	N.A.	Investigative	[2]
Des-AA1,2,4,5,10,12,13-[D-Trp8]SRIF	DMEVOD2	Discovery agent	N.A.	Investigative	[2]
Des-AA1,2,4,5,13-[D-Trp8]-SRIF	DMYZXEO	Discovery agent	N.A.	Investigative	[2]
Des-AA1,2,4,5-[D-Trp8]SRIF	DMEN4G8	Discovery agent	N.A.	Investigative	[2]
Des-AA1,2,5,12,13-[D-Trp8,IAmp9]SRIF	DMZPXGY	Discovery agent	N.A.	Investigative	[2]
Des-AA1,2,5,12,13-[D-Trp8]SRIF	DM1KJAE	Discovery agent	N.A.	Investigative	[2]
Des-AA1,2,5-[D-Trp8,(NalphaMe)IAmp9]SRIF	DMX2I4P	Discovery agent	N.A.	Investigative	[7]
Des-AA1,2,5-[D-Trp8,IAmp9,m-I-Tyr11]Cbm-SRIF	DMH0DLZ	Discovery agent	N.A.	Investigative	[7]
Des-AA1,2,5-[D-Trp8,IAmp9]SRIF CH-275	DMSXILZ	Discovery agent	N.A.	Investigative	[7]
Des-AA1,2,5-[D-Trp8,Tyr11]SRIF	DM7MZ2V	Discovery agent	N.A.	Investigative	[7]
Des-AA1,4,5,13-[Tyr2,D-Trp8]-SRIF	DMPMAXI	Discovery agent	N.A.	Investigative	[2]
Des-AA1,5-[Tyr2,D-Trp8,IAmp9]Cbm-SRIF	DMV8EWF	Discovery agent	N.A.	Investigative	[7]
Des-AA5-[D-Trp8]SRIF	DMO3CFV	Discovery agent	N.A.	Investigative	[7]
H-D-Phe-c[Cys-Ala-D-Trp-Lys-Thr-Cys]-Thr-NH2	DML8S7J	Discovery agent	N.A.	Investigative	[8]
H-DPhe-c[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-NH2	DMLCIZ8	Discovery agent	N.A.	Investigative	[8]
L-796,778	DMINOFE	Discovery agent	N.A.	Investigative	[9]
NVP ACQ090	DM8R16V	Discovery agent	N.A.	Investigative	[1]
SOMATOSTATIN	DMIOFQE	Acromegaly	5A60.0	Investigative	[10]
SRIF-14	DMDY1M7	Discovery agent	N.A.	Investigative	[11]
SRIF-28	DM0OM9L	Discovery agent	N.A.	Investigative	[12]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Alzheimer's disease	8A00.0	Entorhinal cortex	2.40E-04	-0.09	-0.56
Melanoma	2C82	Skin	2.98E-01	-0.02	-0.04

References

• [1] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 357).
• [2] Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides. J Med Chem. 2005 Jan 27;48(2):515-22.
• [3] Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
• [4] Identification of potent non-peptide somatostatin antagonists with sst(3) selectivity. J Med Chem. 2001 Aug 30;44(18):2990-3000.
• [5] Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies. Naunyn Schmiedebergs Arch Pharmacol. 1999 Nov;360(5):488-99.
• [6] An adjustable release rate linking strategy for cytotoxin-peptide conjugates. Bioorg Med Chem Lett. 2003 Mar 10;13(5):799-803.
• [7] Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. J Med Chem. 2005 Jan 27;48(2):507-14.
• [8] Novel sst2-selective somatostatin agonists. Three-dimensional consensus structure by NMR. J Med Chem. 2006 Jul 27;49(15):4487-96.
• [9] Rapid identification of subtype-selective agonists of the somatostatin receptor through combinatorial chemistry. Science. 1998 Oct 23;282(5389):737-40.
• [10] Discovery of iodinated somatostatin analogues selective for hsst2 and hsst5 with excellent inhibition of growth hormone and prolactin release from ... J Med Chem. 2005 Oct 20;48(21):6643-52.
• [11] A human somatostatin receptor (SSTR3), located on chromosome 22, displays preferential affinity for somatostatin-14 like peptides. FEBS Lett. 1993 Apr 26;321(2-3):279-84.
• [12] Novel octreotide dicarba-analogues with high affinity and different selectivity for somatostatin receptors. J Med Chem. 2010 Aug 26;53(16):6188-97.