Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT2BC4G)

• DTT Name: Somatostatin receptor type 5 (SSTR5)
• Synonyms: Somatostatin receptor 5; SSTR5; SS5R
• Gene Name: SSTR5
• DTT Type: Successful target; [1]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: SSR5_HUMAN
• TTD ID: T64830
• Sequence:
  MEPLFPASTPSWNASSPGAASGGGDNRTLVGPAPSAGARAVLVPVLYLLVCAAGLGGNTL
  VIYVVLRFAKMKTVTNIYILNLAVADVLYMLGLPFLATQNAASFWPFGPVLCRLVMTLDG
  VNQFTSVFCLTVMSVDRYLAVVHPLSSARWRRPRVAKLASAAAWVLSLCMSLPLLVFADV
  QEGGTCNASWPEPVGLWGAVFIIYTAVLGFFAPLLVICLCYLLIVVKVRAAGVRVGCVRR
  RSERKVTRMVLVVVLVFAGCWLPFFTVNIVNLAVALPQEPASAGLYFFVVILSYANSCAN
  PVLYGFLSDNFRQSFQKVLCLRKGSGAKDADATEPRPDRIRQQQEATPPAHRAAANGLMQ
  TSKL
• Function: Receptor for somatostatin 28 and to a lesser extent for somatostatin-14. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase. Increases cell growth inhibition activity of SSTR2 following heterodimerization.
• KEGG Pathway:
  cAMP signaling pathway (hsa04024)
  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]

19 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	[1]
CGP 23996	DMTECXA	Discovery agent	N.A.	Investigative	[4]
Cytotoxin Peptide Conjugate	DM7SVLZ	Discovery agent	N.A.	Investigative	[5]
D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Asp-NH2	DM0YQHM	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-AA1,2,4,5,13-[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]SRIF	DM1KJAE	Discovery agent	N.A.	Investigative	[2]
Des-AA1,2,5-[D-Trp8,Tyr11]SRIF	DM7MZ2V	Discovery agent	N.A.	Investigative	[7]
Des-AA5-[D-Trp8]SRIF	DMO3CFV	Discovery agent	N.A.	Investigative	[7]
H-D-Phe-Cys-Tyr-D-Trp-Lys-Val-Cys-Thr-NH2	DM1EGC3	Discovery agent	N.A.	Investigative	[6]
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-817,818	DM8YT7X	Discovery agent	N.A.	Investigative	[9]
PTR-3046	DMZGFE8	Discovery agent	N.A.	Investigative	[10]
SOMATOSTATIN	DMIOFQE	Acromegaly	5A60.0	Investigative	[6]
SRIF-14	DMDY1M7	Discovery agent	N.A.	Investigative	[4]
SRIF-28	DM0OM9L	Discovery agent	N.A.	Investigative	[11]

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	2.74E-01	-0.04	-0.26
Melanoma	2C82	Skin	2.70E-01	-0.12	-0.27

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: 359).
• [2] Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides. J Med Chem. 2005 Jan 27;48(2):515-22.
• [3] Role of somatostatin in the augmentation of hippocampal long-term potentiation by FR121196, a putative cognitive enhancer. Eur J Pharmacol. 1993 Sep 7;241(1):27-34.
• [4] [125I][Tyr3]octreotide labels human somatostatin sst2 and sst5 receptors. Eur J Pharmacol. 1998 May 8;348(2-3):311-20.
• [5] An adjustable release rate linking strategy for cytotoxin-peptide conjugates. Bioorg Med Chem Lett. 2003 Mar 10;13(5):799-803.
• [6] 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.
• [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] Highly potent 4-amino-indolo[2,3-c]azepin-3-one-containing somatostatin mimetics with a range of sst receptor selectivities. J Med Chem. 2009 Jan 8;52(1):95-104.
• [11] Novel octreotide dicarba-analogues with high affinity and different selectivity for somatostatin receptors. J Med Chem. 2010 Aug 26;53(16):6188-97.