Target Information
Target General Infomation | |||||
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Target ID |
T64830
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Former ID |
TTDC00253
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Target Name |
Somatostatin receptor type 5
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Gene Name |
SSTR5
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Synonyms |
SS5R; Somatostatin receptor 5; SSTR5
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Target Type |
Successful
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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.
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T64830
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UniProt ID | |||||
Sequence |
MEPLFPASTPSWNASSPGAASGGGDNRTLVGPAPSAGARAVLVPVLYLLVCAAGLGGNTL
VIYVVLRFAKMKTVTNIYILNLAVADVLYMLGLPFLATQNAASFWPFGPVLCRLVMTLDG VNQFTSVFCLTVMSVDRYLAVVHPLSSARWRRPRVAKLASAAAWVLSLCMSLPLLVFADV QEGGTCNASWPEPVGLWGAVFIIYTAVLGFFAPLLVICLCYLLIVVKVRAAGVRVGCVRR RSERKVTRMVLVVVLVFAGCWLPFFTVNIVNLAVALPQEPASAGLYFFVVILSYANSCAN PVLYGFLSDNFRQSFQKVLCLRKGSGAKDADATEPRPDRIRQQQEATPPAHRAAANGLMQ TSKL |
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Drugs and Mode of Action | |||||
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 523209 | ClinicalTrials.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 525297 | ClinicalTrials.gov (NCT02527993) Treatment of Hypoglycemia Following Gastric Bypass Surgery. | ||||
Ref 526564 | Bioorg Med Chem Lett. 2003 Mar 10;13(5):799-803.An adjustable release rate linking strategy for cytotoxin-peptide conjugates. | ||||
Ref 527384 | J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. | ||||
Ref 527385 | J Med Chem. 2005 Jan 27;48(2):515-22.Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides. | ||||
Ref 527508 | 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. | ||||
Ref 527802 | 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 pituitarycells. | ||||
Ref 528320 | J Med Chem. 2006 Jul 27;49(15):4487-96.Novel sst2-selective somatostatin agonists. Three-dimensional consensus structure by NMR. | ||||
Ref 529856 | J 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 531062 | J Med Chem. 2010 Aug 26;53(16):6188-97.Novel octreotide dicarba-analogues with high affinity and different selectivity for somatostatin receptors. | ||||
Ref 533791 | 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. | ||||
Ref 534665 | [125I][Tyr3]octreotide labels human somatostatin sst2 and sst5 receptors. Eur J Pharmacol. 1998 May 8;348(2-3):311-20. |
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