Target Information
Target General Infomation | |||||
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Target ID |
T62974
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Former ID |
TTDC00034
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Target Name |
Somatostatin receptor type 4
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Gene Name |
SSTR4
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Synonyms |
SS4R; SSTR4
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Target Type |
Clinical Trial
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Disease | Alzheimer disease [ICD9: 331; ICD10: G30] | ||||
HCV infection [ICD9: 070.4, 070.5, 070.70; ICD10: B17.1, B18.2] | |||||
Neuroendocrine cancer [ICD10: C7A] | |||||
Function |
Receptor for somatostatin-14. The activity of this receptor is mediated by G proteins which inhibits adenylyl cyclase. It is functionally coupled not only to inhibition of adenylate cyclase, but also to activation of both arachidonate release and mitogen-activated protein (MAP) kinase cascade. Mediates antiproliferative action of somatostatin in tumor cells.
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T62974
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UniProt ID | |||||
Sequence |
MSAPSTLPPGGEEGLGTAWPSAANASSAPAEAEEAVAGPGDARAAGMVAIQCIYALVCLV
GLVGNALVIFVILRYAKMKTATNIYLLNLAVADELFMLSVPFVASSAALRHWPFGSVLCR AVLSVDGLNMFTSVFCLTVLSVDRYVAVVHPLRAATYRRPSVAKLINLGVWLASLLVTLP IAIFADTRPARGGQAVACNLQWPHPAWSAVFVVYTFLLGFLLPVLAIGLCYLLIVGKMRA VALRAGWQQRRRSEKKITRLVLMVVVVFVLCWMPFYVVQLLNLFVTSLDATVNHVSLILS YANSCANPILYGFLSDNFRRFFQRVLCLRCCLLEGAGGAEEEPLDYYATALKSKGGAGCM CPPLPCQQEALQPEPGRKRIPLTRTTTF |
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Drugs and Mode of Action | |||||
Inhibitor | 177Lu-DOTATATE | Drug Info | [1725888] | ||
Ala11-SRIF-14-amide | Drug Info | [527585] | |||
Ala6-SRIF-14-amide | Drug Info | [527585] | |||
CytotoxinPeptide Conjugate | Drug Info | [526564] | |||
D-Trp8-SRIF-14 | Drug Info | [527585] | |||
Des-AA1,2,4,12,13-[D-Trp8]SRIF | Drug Info | [527385] | |||
Des-AA1,2,4,13-[D-Trp8]SRIF | Drug Info | [527385] | |||
Des-AA1,2,4,5,10,12,13-[D-Trp8]SRIF | Drug Info | [527385] | |||
Des-AA1,2,4,5,13-[D-Trp8]-SRIF | Drug Info | [527385] | |||
Des-AA1,2,4,5,6,12,13-[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,IAmp9]SRIF | Drug Info | [527385] | |||
Des-AA1,2,5,12,13-[D-Trp8]SRIF | Drug Info | [527385] | |||
Des-AA1,2,5-[D-Nal8,IAmp9,(NalphaMe)Thr12]SRIF | Drug Info | [527384] | |||
Des-AA1,2,5-[D-Trp8,(NalphaMe)IAmp9]SRIF | Drug Info | [527384] | |||
Des-AA1,2,5-[D-Trp8,Tyr11]SRIF | Drug Info | [527384] | |||
Des-AA1,2,5-[IAmp9,Tyr11]-SRIF | Drug Info | [527384] | |||
Des-AA1,5-[Tyr2,D-Trp8,(NalphaMe)IAmp9]Cbm-SRIF | Drug Info | [527384] | |||
Des-AA1,5-[Tyr2,D-Trp8,(NalphaMe)IAmp9]SRIF | Drug Info | [527384] | |||
Des-AA5-[D-Trp8]SRIF | Drug Info | [527384] | |||
ODT-8 | Drug Info | [527385] | |||
Pyz11-D-Trp8-SRIF | Drug Info | [527585] | |||
Pyz6-D-Trp8-SRIF | Drug Info | [527585] | |||
Pyz7-D-Trp8-SRIF | Drug Info | [527585] | |||
Radiolabeled octreotide derivative | Drug Info | [527508] | |||
SOMATOSTATIN | Drug Info | [527802] | |||
SRIF-28 | Drug Info | [531062] | |||
Modulator | 99mTc-MIP-1407 | Drug Info | [543790] | ||
FR-121196 | Drug Info | [533791] | |||
Agonist | beta3-tetrapeptide | Drug Info | [526548] | ||
CGP 23996 | Drug Info | [525652] | |||
L-803,087 | Drug Info | [534729] | |||
NNC269100 | Drug Info | [534752] | |||
SRIF-14 | Drug Info | [534701] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG 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 | |||||
PathWhiz Pathway | Gastric Acid Production | ||||
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 525652 | Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies. Naunyn Schmiedebergs Arch Pharmacol. 1999 Nov;360(5):488-99. | ||||
Ref 526548 | Beta(2)/beta(3)-di- and alpha/beta(3)-tetrapeptide derivatives as potent agonists at somatostatin sst(4) receptors. Naunyn Schmiedebergs Arch Pharmacol. 2003 Feb;367(2):95-103. Epub 2003 Jan 24. | ||||
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 527585 | J Med Chem. 2005 Jun 16;48(12):4025-30.Replacement of Phe6, Phe7, and Phe11 of D-Trp8-somatostatin-14 with L-pyrazinylalanine. Predicted and observed effects on binding affinities at hSST2 and hSST4.An unexpected effect of the chirality of Trp8 on NMR spectra in methanol. | ||||
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 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 534701 | Synthesis and biological activities of potent peptidomimetics selective for somatostatin receptor subtype 2. Proc Natl Acad Sci U S A. 1998 Sep 1;95(18):10836-41. | ||||
Ref 534729 | Rapid identification of subtype-selective agonists of the somatostatin receptor through combinatorial chemistry. Science. 1998 Oct 23;282(5389):737-40. | ||||
Ref 534752 | Nonpeptide somatostatin agonists with sst4 selectivity: synthesis and structure-activity relationships of thioureas. J Med Chem. 1998 Nov 19;41(24):4693-705. |
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