Target Information
| Target General Information | Top | |||||
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| Target ID |
T16633
(Former ID: TTDC00112)
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| Target Name |
Somatostatin receptor type 1 (SSTR1)
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| Synonyms |
Sst(1); Somatostatin receptor 1; SSTR1; SS1R; SRIF-2
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| Gene Name |
SSTR1
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 2 Target-related Diseases | + | ||||
| 1 | Cushing syndrome [ICD-11: 5A70] | |||||
| 2 | Stomach cancer [ICD-11: 2B72] | |||||
| Function |
Receptor for somatostatin with higher affinity for somatostatin-14 than -28. This receptor is coupled via pertussis toxin sensitive G proteins to inhibition of adenylyl cyclase. In addition it stimulates phosphotyrosine phosphataseand Na(+)/H(+) exchanger via pertussis toxin insensitive G proteins.
Click to Show/Hide
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| BioChemical Class |
GPCR rhodopsin
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| UniProt ID | ||||||
| Sequence |
MFPNGTASSPSSSPSPSPGSCGEGGGSRGPGAGAADGMEEPGRNASQNGTLSEGQGSAIL
ISFIYSVVCLVGLCGNSMVIYVILRYAKMKTATNIYILNLAIADELLMLSVPFLVTSTLL RHWPFGALLCRLVLSVDAVNMFTSIYCLTVLSVDRYVAVVHPIKAARYRRPTVAKVVNLG VWVLSLLVILPIVVFSRTAANSDGTVACNMLMPEPAQRWLVGFVLYTFLMGFLLPVGAIC LCYVLIIAKMRMVALKAGWQQRKRSERKITLMVMMVVMVFVICWMPFYVVQLVNVFAEQD DATVSQLSVILGYANSCANPILYGFLSDNFKRSFQRILCLSWMDNAAEEPVDYYATALKS RAYSVEDFQPENLESGGVFRNGTCTSRITTL Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| Drugs and Modes of Action | Top | |||||
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| Approved Drug(s) | [+] 2 Approved Drugs | + | ||||
| 1 | Lutetium Lu 177 dotatate | Drug Info | Approved | Neuroendocrine cancer | [2] | |
| 2 | Pasireotide | Drug Info | Approved | Cushing disease | [3], [4] | |
| Discontinued Drug(s) | [+] 1 Discontinued Drugs | + | ||||
| 1 | FR-121196 | Drug Info | Terminated | Alzheimer disease | [5] | |
| Mode of Action | [+] 4 Modes of Action | + | ||||
| Antagonist | [+] 2 Antagonist drugs | + | ||||
| 1 | Lutetium Lu 177 dotatate | Drug Info | [2] | |||
| 2 | SRA880 | Drug Info | [14] | |||
| Inhibitor | [+] 38 Inhibitor drugs | + | ||||
| 1 | Pasireotide | Drug Info | [1] | |||
| 2 | ODT-8 | Drug Info | [6] | |||
| 3 | Cytotoxin Peptide Conjugate | Drug Info | [10] | |||
| 4 | Des-AA1,2,4,12,13-[D-Trp8]SRIF | Drug Info | [6] | |||
| 5 | Des-AA1,2,4,13-[D-Trp8]SRIF | Drug Info | [6] | |||
| 6 | Des-AA1,2,4,5,13-[D-Trp8]-SRIF | Drug Info | [6] | |||
| 7 | Des-AA1,2,4,5-[D-Trp8]SRIF | Drug Info | [6] | |||
| 8 | Des-AA1,2,5,12,13-[D-Trp8,IAmp9]SRIF | Drug Info | [6] | |||
| 9 | Des-AA1,2,5,12,13-[D-Trp8]SRIF | Drug Info | [6] | |||
| 10 | Des-AA1,2,5-[(NalphaMe)Cys3,D-Nal8,IAmp9]SRIF | Drug Info | [11] | |||
| 11 | Des-AA1,2,5-[(NalphaMe)Cys3,D-Trp8,IAmp9]SRIF | Drug Info | [11] | |||
| 12 | Des-AA1,2,5-[(NalphaMe)D-Nal8,IAmp9]SRIF | Drug Info | [11] | |||
| 13 | Des-AA1,2,5-[(NalphaMe)Lys4,D-Nal8,IAmp9]SRIF | Drug Info | [11] | |||
| 14 | Des-AA1,2,5-[D-Nal8,(NalphaMe)IAmp9,Tyr11]SRIF | Drug Info | [11] | |||
| 15 | Des-AA1,2,5-[D-Nal8,(NalphaMe)IAmp9]SRIF | Drug Info | [11] | |||
| 16 | Des-AA1,2,5-[D-Nal8,IAmp9,(NalphaMe)Cys14]SRIF | Drug Info | [11] | |||
| 17 | Des-AA1,2,5-[D-Nal8,IAmp9,(NalphaMe)Phe11]SRIF | Drug Info | [11] | |||
| 18 | Des-AA1,2,5-[D-Nal8,IAmp9,(NalphaMe)Ser13]SRIF | Drug Info | [11] | |||
| 19 | Des-AA1,2,5-[D-Nal8,IAmp9,(NalphaMe)Thr12]SRIF | Drug Info | [11] | |||
| 20 | Des-AA1,2,5-[D-Nal8,IAmp9]SRIF | Drug Info | [11] | |||
| 21 | Des-AA1,2,5-[D-Trp8,(NalphaMe)IAmp9,Tyr11]SRIF | Drug Info | [11] | |||
| 22 | Des-AA1,2,5-[D-Trp8,(NalphaMe)IAmp9]SRIF | Drug Info | [11] | |||
| 23 | Des-AA1,2,5-[D-Trp8,IAmp9,(NalphaMe)Cys14]SRIF | Drug Info | [11] | |||
| 24 | Des-AA1,2,5-[D-Trp8,IAmp9,(NalphaMe)Ser13]SRIF | Drug Info | [11] | |||
| 25 | Des-AA1,2,5-[D-Trp8,IAmp9,(NalphaMe)Thr12]SRIF | Drug Info | [11] | |||
| 26 | Des-AA1,2,5-[D-Trp8,IAmp9,m-I-Tyr11]Cbm-SRIF | Drug Info | [11] | |||
| 27 | Des-AA1,2,5-[D-Trp8,IAmp9,Tyr11]Cbm-SRIF | Drug Info | [11] | |||
| 28 | Des-AA1,2,5-[D-Trp8,IAmp9]SRIF CH-275 | Drug Info | [11] | |||
| 29 | Des-AA1,2,5-[D-Trp8,Tyr11]SRIF | Drug Info | [11] | |||
| 30 | Des-AA1,2,5-[IAmp9,Tyr11]-SRIF | Drug Info | [11] | |||
| 31 | Des-AA1,4,5,13-[Tyr2,D-Trp8]-SRIF | Drug Info | [6] | |||
| 32 | Des-AA1,5-[Tyr2,D-Trp8,(NalphaMe)IAmp9]Cbm-SRIF | Drug Info | [11] | |||
| 33 | Des-AA1,5-[Tyr2,D-Trp8,(NalphaMe)IAmp9]SRIF | Drug Info | [11] | |||
| 34 | Des-AA1,5-[Tyr2,D-Trp8,IAmp9]Cbm-SRIF | Drug Info | [11] | |||
| 35 | Des-AA1,5-[Tyr2,D-Trp8,IAmp9]SRIF CH-288 | Drug Info | [6] | |||
| 36 | Des-AA5-[D-Trp8]SRIF | Drug Info | [11] | |||
| 37 | SOMATOSTATIN | Drug Info | [13] | |||
| 38 | SRIF-28 | Drug Info | [16] | |||
| Modulator | [+] 2 Modulator drugs | + | ||||
| 1 | FR-121196 | Drug Info | [7], [8] | |||
| 2 | 99mTc-MIP-1407 | Drug Info | [7], [8] | |||
| Agonist | [+] 4 Agonist drugs | + | ||||
| 1 | CGP 23996 | Drug Info | [9] | |||
| 2 | L-797,591 | Drug Info | [12] | |||
| 3 | L-817,818 | Drug Info | [12] | |||
| 4 | SRIF-14 | Drug Info | [15] | |||
| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| Target Profiles in Patients | Top | |||||
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| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| KEGG Pathway | [+] 2 KEGG Pathways | + | ||||
| 1 | cAMP signaling pathway | |||||
| 2 | Neuroactive ligand-receptor interaction | |||||
| Panther Pathway | [+] 2 Panther Pathways | + | ||||
| 1 | Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway | |||||
| 2 | Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway | |||||
| Reactome | [+] 2 Reactome Pathways | + | ||||
| 1 | Peptide ligand-binding receptors | |||||
| 2 | G alpha (i) signalling events | |||||
| WikiPathways | [+] 5 WikiPathways | + | ||||
| 1 | SIDS Susceptibility Pathways | |||||
| 2 | GPCRs, Class A Rhodopsin-like | |||||
| 3 | Peptide GPCRs | |||||
| 4 | GPCR ligand binding | |||||
| 5 | GPCR downstream signaling | |||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
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| REF 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: 355). | |||||
| REF 2 | 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89. | |||||
| REF 3 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 4 | ClinicalTrials.gov (NCT02527993) Treatment of Hypoglycemia Following Gastric Bypass Surgery. | |||||
| REF 5 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001380) | |||||
| REF 6 | Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides. J Med Chem. 2005 Jan 27;48(2):515-22. | |||||
| REF 7 | Nat Rev Drug Discov. 2013 Feb;12(2):87-90. | |||||
| REF 8 | Pasireotide and octreotide stimulate distinct patterns of sst2A somatostatin receptor phosphorylation. Mol Endocrinol. 2010 Feb;24(2):436-46. | |||||
| REF 9 | Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies. Naunyn Schmiedebergs Arch Pharmacol. 1999 Nov;360(5):488-99. | |||||
| REF 10 | An adjustable release rate linking strategy for cytotoxin-peptide conjugates. Bioorg Med Chem Lett. 2003 Mar 10;13(5):799-803. | |||||
| REF 11 | Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. J Med Chem. 2005 Jan 27;48(2):507-14. | |||||
| REF 12 | Rapid identification of subtype-selective agonists of the somatostatin receptor through combinatorial chemistry. Science. 1998 Oct 23;282(5389):737-40. | |||||
| REF 13 | 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. | |||||
| REF 14 | SRA880, in vitro characterization of the first non-peptide somatostatin sst(1) receptor antagonist. Neurosci Lett. 2004 May 6;361(1-3):132-5. | |||||
| REF 15 | 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 16 | Novel octreotide dicarba-analogues with high affinity and different selectivity for somatostatin receptors. J Med Chem. 2010 Aug 26;53(16):6188-97. | |||||
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