Target Information
Target General Information | Top | |||||
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Target ID |
T64830
(Former ID: TTDC00253)
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Target Name |
Somatostatin receptor type 5 (SSTR5)
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Synonyms |
Somatostatin receptor 5; SSTR5; SS5R
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Gene Name |
SSTR5
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Target Type |
Successful target
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[1] | ||||
Disease | [+] 1 Target-related Diseases | + | ||||
1 | Cushing syndrome [ICD-11: 5A70] | |||||
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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UniProt ID | ||||||
Sequence |
MEPLFPASTPSWNASSPGAASGGGDNRTLVGPAPSAGARAVLVPVLYLLVCAAGLGGNTL
VIYVVLRFAKMKTVTNIYILNLAVADVLYMLGLPFLATQNAASFWPFGPVLCRLVMTLDG VNQFTSVFCLTVMSVDRYLAVVHPLSSARWRRPRVAKLASAAAWVLSLCMSLPLLVFADV QEGGTCNASWPEPVGLWGAVFIIYTAVLGFFAPLLVICLCYLLIVVKVRAAGVRVGCVRR RSERKVTRMVLVVVLVFAGCWLPFFTVNIVNLAVALPQEPASAGLYFFVVILSYANSCAN PVLYGFLSDNFRQSFQKVLCLRKGSGAKDADATEPRPDRIRQQQEATPPAHRAAANGLMQ TSKL Click to Show/Hide
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3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
HIT2.0 ID | T54G5E |
Drugs and Modes of Action | Top | |||||
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Approved Drug(s) | [+] 1 Approved Drugs | + | ||||
1 | Pasireotide | Drug Info | Approved | Cushing disease | [2], [3] | |
Discontinued Drug(s) | [+] 1 Discontinued Drugs | + | ||||
1 | FR-121196 | Drug Info | Terminated | Alzheimer disease | [4] | |
Mode of Action | [+] 3 Modes of Action | + | ||||
Inhibitor | [+] 17 Inhibitor drugs | + | ||||
1 | Pasireotide | Drug Info | [1] | |||
2 | ODT-8 | Drug Info | [5] | |||
3 | Cytotoxin Peptide Conjugate | Drug Info | [8] | |||
4 | D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Asp-NH2 | Drug Info | [9] | |||
5 | Des-AA1,2,4,12,13-[D-Trp8]SRIF | Drug Info | [5] | |||
6 | Des-AA1,2,4,13-[D-Trp8]SRIF | Drug Info | [5] | |||
7 | Des-AA1,2,4,5,13-[D-Trp8]-SRIF | Drug Info | [5] | |||
8 | Des-AA1,2,4,5-[D-Trp8]SRIF | Drug Info | [5] | |||
9 | Des-AA1,2,5,12,13-[D-Trp8]SRIF | Drug Info | [5] | |||
10 | Des-AA1,2,5-[D-Trp8,Tyr11]SRIF | Drug Info | [10] | |||
11 | Des-AA5-[D-Trp8]SRIF | Drug Info | [10] | |||
12 | H-D-Phe-Cys-Tyr-D-Trp-Lys-Val-Cys-Thr-NH2 | Drug Info | [9] | |||
13 | H-D-Phe-c[Cys-Ala-D-Trp-Lys-Thr-Cys]-Thr-NH2 | Drug Info | [11] | |||
14 | H-DPhe-c[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-NH2 | Drug Info | [11] | |||
15 | PTR-3046 | Drug Info | [13] | |||
16 | SOMATOSTATIN | Drug Info | [9] | |||
17 | SRIF-28 | Drug Info | [14] | |||
Modulator | [+] 2 Modulator drugs | + | ||||
1 | FR-121196 | Drug Info | [6] | |||
2 | 99mTc-MIP-1407 | Drug Info | [1] | |||
Agonist | [+] 3 Agonist drugs | + | ||||
1 | CGP 23996 | Drug Info | [7] | |||
2 | L-817,818 | Drug Info | [12] | |||
3 | SRIF-14 | Drug Info | [7] |
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 | |||||
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Co-Targets |
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 | [+] 4 WikiPathways | + | ||||
1 | GPCRs, Class A Rhodopsin-like | |||||
2 | Peptide GPCRs | |||||
3 | GPCR ligand binding | |||||
4 | 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: 359). | |||||
REF 2 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
REF 3 | ClinicalTrials.gov (NCT02527993) Treatment of Hypoglycemia Following Gastric Bypass Surgery. | |||||
REF 4 | 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 5 | Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides. J Med Chem. 2005 Jan 27;48(2):515-22. | |||||
REF 6 | 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 7 | [125I][Tyr3]octreotide labels human somatostatin sst2 and sst5 receptors. Eur J Pharmacol. 1998 May 8;348(2-3):311-20. | |||||
REF 8 | An adjustable release rate linking strategy for cytotoxin-peptide conjugates. Bioorg Med Chem Lett. 2003 Mar 10;13(5):799-803. | |||||
REF 9 | 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 10 | Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. J Med Chem. 2005 Jan 27;48(2):507-14. | |||||
REF 11 | Novel sst2-selective somatostatin agonists. Three-dimensional consensus structure by NMR. J Med Chem. 2006 Jul 27;49(15):4487-96. | |||||
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 | 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. | |||||
REF 14 | 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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