Target Information

Target General Infomation
Target ID
T64830
Former ID
TTDC00253
Target Name
Somatostatin receptor type 5
Gene Name
SSTR5
Synonyms
SS5R; Somatostatin receptor 5; SSTR5
Target Type
Successful
Disease Alzheimer disease [ICD9: 331; ICD10: G30]
Cushing's disease [ICD9: 255; ICD10: E24.0]
Neuroendocrine cancer [ICD10: C7A]
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.
BioChemical Class
GPCR rhodopsin
Target Validation
T64830
UniProt ID
P35346
Sequence
MEPLFPASTPSWNASSPGAASGGGDNRTLVGPAPSAGARAVLVPVLYLLVCAAGLGGNTL
VIYVVLRFAKMKTVTNIYILNLAVADVLYMLGLPFLATQNAASFWPFGPVLCRLVMTLDG
VNQFTSVFCLTVMSVDRYLAVVHPLSSARWRRPRVAKLASAAAWVLSLCMSLPLLVFADV
QEGGTCNASWPEPVGLWGAVFIIYTAVLGFFAPLLVICLCYLLIVVKVRAAGVRVGCVRR
RSERKVTRMVLVVVLVFAGCWLPFFTVNIVNLAVALPQEPASAGLYFFVVILSYANSCAN
PVLYGFLSDNFRQSFQKVLCLRKGSGAKDADATEPRPDRIRQQQEATPPAHRAAANGLMQ
TSKL
Drugs and Mode of Action
Drug(s) Pasireotide Drug Info Approved Cushing's disease [525297], [551871]
ODT-8 Drug Info Phase 3 Discovery agent [523209]
FR-121196 Drug Info Terminated Alzheimer disease [544870]
Modulator 99mTc-MIP-1407 Drug Info [543791]
FR-121196 Drug Info [533791]
Agonist CGP 23996 Drug Info [534665]
L-817,818 Drug Info [534729]
SRIF-14 Drug Info [534665]
Inhibitor CytotoxinPeptide Conjugate Drug Info [526564]
D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Asp-NH2 Drug Info [527802]
Des-AA1,2,4,12,13-[D-Trp8]SRIF Drug Info [527385]
Des-AA1,2,4,13-[D-Trp8]SRIF Drug Info [527385]
Des-AA1,2,4,5,13-[D-Trp8]-SRIF Drug Info [527385]
Des-AA1,2,4,5-[D-Trp8]SRIF Drug Info [527385]
Des-AA1,2,5,12,13-[D-Trp8]SRIF Drug Info [527385]
Des-AA1,2,5-[D-Trp8,Tyr11]SRIF Drug Info [527384]
Des-AA5-[D-Trp8]SRIF Drug Info [527384]
H-D-Phe-Cys-Tyr-D-Trp-Lys-Val-Cys-Thr-NH2 Drug Info [527802]
H-D-Phe-c[Cys-Ala-D-Trp-Lys-Thr-Cys]-Thr-NH2 Drug Info [528320]
H-DPhe-c[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-NH2 Drug Info [528320]
ODT-8 Drug Info [527385]
Pasireotide Drug Info [543791]
PTR-3046 Drug Info [529856]
Radiolabeled octreotide derivative Drug Info [527508]
SOMATOSTATIN Drug Info [527802]
SRIF-28 Drug Info [531062]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway cAMP signaling pathway
Neuroactive ligand-receptor interaction
PANTHER Pathway Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway
Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway
Reactome Peptide ligand-binding receptors
G alpha (i) signalling events
WikiPathways GPCRs, Class A Rhodopsin-like
Peptide GPCRs
GPCR ligand binding
GPCR downstream signaling
References
Ref 523209ClinicalTrials.gov (NCT01220167) Three-way Crossover Comparative Water-effect Bioavailability to Compare Ondansetron ODFS 8mg With and Without Water With Zofran ODT 8mg Without Water in 18 Healthy Participants Under Fasting Conditions. U.S. National Institutes of Health.
Ref 525297ClinicalTrials.gov (NCT02527993) Treatment of Hypoglycemia Following Gastric Bypass Surgery.
Ref 544870Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001380)
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 526564Bioorg Med Chem Lett. 2003 Mar 10;13(5):799-803.An adjustable release rate linking strategy for cytotoxin-peptide conjugates.
Ref 527384J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan.
Ref 527385J Med Chem. 2005 Jan 27;48(2):515-22.Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides.
Ref 527508J 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.
Ref 527802J 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 pituitarycells.
Ref 528320J Med Chem. 2006 Jul 27;49(15):4487-96.Novel sst2-selective somatostatin agonists. Three-dimensional consensus structure by NMR.
Ref 529856J Med Chem. 2009 Jan 8;52(1):95-104.Highly potent 4-amino-indolo[2,3-c]azepin-3-one-containing somatostatin mimetics with a range of sst receptor selectivities.
Ref 531062J Med Chem. 2010 Aug 26;53(16):6188-97.Novel octreotide dicarba-analogues with high affinity and different selectivity for somatostatin receptors.
Ref 533791Role 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.
Ref 534665[125I][Tyr3]octreotide labels human somatostatin sst2 and sst5 receptors. Eur J Pharmacol. 1998 May 8;348(2-3):311-20.
Ref 534729Rapid identification of subtype-selective agonists of the somatostatin receptor through combinatorial chemistry. Science. 1998 Oct 23;282(5389):737-40.
Ref 543791(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).

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