Target Information
Target General Information | Top | |||||
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Target ID |
T45674
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Target Name |
Sigma intracellular receptor 2 (TMEM97)
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Synonyms |
Transmembrane protein 97; Sigma2 receptor; Sigma-2 receptor; Meningioma-associated protein 30; MAC30
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Gene Name |
TMEM97
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Target Type |
Clinical trial target
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[1] | ||||
Disease | [+] 1 Target-related Diseases | + | ||||
1 | Schizophrenia [ICD-11: 6A20] | |||||
Function |
Intracellular orphan receptor that binds numerous drugs and which is highly expressed in various proliferating cancer cells. Corresponds to the sigma-2 receptor, which is thought to play important role in regulating cell survival, morphology and differentiation. Under investigation for its potential diagnostic and therapeutic uses. May play a role as a regulator of cellular cholesterol homeostasis. May function as sterol isomerase. May alter the activity of some cytochrome P450 proteins.
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BioChemical Class |
TMEM97/sigma-2 receptor
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UniProt ID | ||||||
Sequence |
MGAPATRRCVEWLLGLYFLSHIPITLFMDLQAVLPRELYPVEFRNLLKWYAKEFKDPLLQ
EPPAWFKSFLFCELVFQLPFFPIATYAFLKGSCKWIRTPAIIYSVHTMTTLIPILSTFLF EDFSKASGFKGQRPETLHERLTLVSVYAPYLLIPFILLIFMLRSPYYKYEEKRKKK 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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Clinical Trial Drug(s) | [+] 2 Clinical Trial Drugs | + | ||||
1 | MIN-101 | Drug Info | Phase 3 | Schizophrenia | [2] | |
2 | CT1812 | Drug Info | Phase 2 | Alzheimer disease | [3] | |
Preclinical Drug(s) | [+] 1 Preclinical Drugs | + | ||||
1 | ANAVEX 1007 | Drug Info | Preclinical | Pancreatic cancer | [4] | |
Mode of Action | [+] 3 Modes of Action | + | ||||
Antagonist | [+] 3 Antagonist drugs | + | ||||
1 | MIN-101 | Drug Info | [1] | |||
2 | CT1812 | Drug Info | [5], [6] | |||
3 | SM 21 | Drug Info | [11] | |||
Ligand | [+] 52 Ligand drugs | + | ||||
1 | Aryl azepine derivative 1 | Drug Info | [7] | |||
2 | Aryl azepine derivative 2 | Drug Info | [7] | |||
3 | Benzamide derivative 1 | Drug Info | [8] | |||
4 | Benzamide derivative 10 | Drug Info | [7] | |||
5 | Benzamide derivative 11 | Drug Info | [7] | |||
6 | Benzamide derivative 2 | Drug Info | [8] | |||
7 | Benzamide derivative 3 | Drug Info | [8] | |||
8 | Benzamide derivative 4 | Drug Info | [8] | |||
9 | Benzamide derivative 7 | Drug Info | [7] | |||
10 | Benzamide derivative 8 | Drug Info | [7] | |||
11 | Benzamide derivative 9 | Drug Info | [7] | |||
12 | Bicyclo-heptan-2-amine derivative 1 | Drug Info | [8] | |||
13 | Bicyclo-heptan-2-amine derivative 2 | Drug Info | [8] | |||
14 | Bicyclo-heptan-2-amine derivative 3 | Drug Info | [8] | |||
15 | Bicyclo-heptan-2-amine derivative 4 | Drug Info | [8] | |||
16 | Fused aryl carbocycle derivative 1 | Drug Info | [7] | |||
17 | Fused aryl carbocycle derivative 2 | Drug Info | [7] | |||
18 | Fused aryl carbocycle derivative 3 | Drug Info | [7] | |||
19 | Fused aryl carbocycle derivative 4 | Drug Info | [7] | |||
20 | Fused aryl carbocycle derivative 8 | Drug Info | [7] | |||
21 | Fused aryl carbocycle derivative 9 | Drug Info | [7] | |||
22 | Isoindoline derivative 1 | Drug Info | [7] | |||
23 | Isoindoline derivative 2 | Drug Info | [7] | |||
24 | Isoindoline derivative 3 | Drug Info | [7] | |||
25 | Isoindoline derivative 4 | Drug Info | [7] | |||
26 | Isoindoline derivative 5 | Drug Info | [7] | |||
27 | N-substituted 9-azabicyclo[3.3.1]nonan-3alpha-yl-phenylcarbamate analog 1 | Drug Info | [8] | |||
28 | N-substituted 9-azabicyclo[3.3.1]nonan-3alpha-yl-phenylcarbamate analog 2 | Drug Info | [8] | |||
29 | N-substituted 9-azabicyclo[3.3.1]nonan-3alpha-yl-phenylcarbamate analog 3 | Drug Info | [8] | |||
30 | Piperazine derivative 7 | Drug Info | [8] | |||
31 | Piperazinyl methyl quinazolinone derivative 1 | Drug Info | [7] | |||
32 | Piperazinyl methyl quinazolinone derivative 2 | Drug Info | [7] | |||
33 | Piperazinyl methyl quinazolinone derivative 3 | Drug Info | [7] | |||
34 | Piperazinyl norbenzomorphane compound 1 | Drug Info | [7] | |||
35 | Piperazinyl norbenzomorphane compound 2 | Drug Info | [7] | |||
36 | Piperazinyl norbenzomorphane compound 3 | Drug Info | [7] | |||
37 | Piperazinyl norbenzomorphane compound 4 | Drug Info | [7] | |||
38 | Piperidine derivative 5 | Drug Info | [8] | |||
39 | Piperidine derivative 6 | Drug Info | [8] | |||
40 | PMID28051882-Compound-Figure9 | Drug Info | [8] | |||
41 | PMID28051882-Compound-XI | Drug Info | [8] | |||
42 | PMID28051882-Compound-XIV | Drug Info | [8] | |||
43 | PMID30185082-Compound-14 | Drug Info | [7] | |||
44 | PMID30185082-Compound-27 | Drug Info | [7] | |||
45 | PMID30185082-Compound-28 | Drug Info | [7] | |||
46 | PMID30185082-Compound-53 | Drug Info | [7] | |||
47 | PMID30185082-Compound-54 | Drug Info | [7] | |||
48 | PMID30185082-Compound-55 | Drug Info | [7] | |||
49 | PMID30185082-Compound-56 | Drug Info | [7] | |||
50 | PMID30185082-Compound-57 | Drug Info | [7] | |||
51 | PMID30185082-Compound-63 | Drug Info | [7] | |||
52 | PMID30185082-Compound-64 | Drug Info | [7] | |||
Agonist | [+] 2 Agonist drugs | + | ||||
1 | ANAVEX 1007 | Drug Info | [4] | |||
2 | 1,3-ditolylguanidine | Drug Info | [9], [10] |
Cell-based Target Expression Variations | Top | |||||
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Cell-based Target Expression Variations |
Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Tissue Distribution
of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues.
The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects
(Nat Rev Drug Discov, 20: 64-81, 2021).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Human Similarity Proteins
Human Tissue Distribution
Human Pathway Affiliation
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There is no similarity protein (E value < 0.005) for this target
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Note:
If a protein has TS (tissue specficity) scores at least in one tissue >= 2.5, this protein is called tissue-enriched (including tissue-enriched-but-not-specific and tissue-specific). In the plots, the vertical lines are at thresholds 2.5 and 4.
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KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
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Neuroactive ligand-receptor interaction | hsa04080 | Affiliated Target |
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Class: Environmental Information Processing => Signaling molecules and interaction | Pathway Hierarchy |
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 |
References | Top | |||||
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REF 1 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 2 | ClinicalTrials.gov (NCT03397134) Study to Evaluate Efficacy and Safety of Roluperidone (MIN-101) in Adult Patients With Negative Symptoms of Schizophrenia. U.S. National Institutes of Health. | |||||
REF 3 | ClinicalTrials.gov (NCT04735536) Pilot Clinical Study of CT1812 in Mild to Moderate Alzheimer's Disease Using EEG. U.S. National Institutes of Health. | |||||
REF 4 | 2011 Pipeline of Anavex. | |||||
REF 5 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 6 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 7 | The sigma-2 (-2) receptor: a review of recent patent applications: 2013-2018.Expert Opin Ther Pat. 2018 Sep;28(9):655-663. | |||||
REF 8 | Are sigma modulators an effective opportunity for cancer treatment A patent overview (1996-2016).Expert Opin Ther Pat. 2017 May;27(5):565-578. | |||||
REF 9 | 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: 2553). | |||||
REF 10 | Sigma1 and sigma2 receptor binding affinity and selectivity of SA4503 and fluoroethyl SA4503. Synapse. 2006 May;59(6):350-8. | |||||
REF 11 | The analgesic tropane analogue (+/-)-SM 21 has a high affinity for sigma2 receptors. Life Sci. 1999;64(10):PL131-7. |
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