Target Information
| Target General Information | Top | |||||
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| Target ID |
T43721
(Former ID: TTDR01269)
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| Target Name |
Corticosteroid 11-beta-dehydrogenase 2 (HSD11B2)
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| Synonyms |
NAD-dependent 11-beta-hydroxysteroid dehydrogenase; HSD11B2; 11-beta-hydroxysteroid dehydrogenase type 2; 11-beta-HSD2; 11-DH2; 11 beta-hydroxysteroid dehydrogenase type 2; 11 beta-HSD2
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| Gene Name |
HSD11B2
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Type 2 diabetes mellitus [ICD-11: 5A11] | |||||
| Function |
Catalyzes the conversion of cortisol to the inactive metabolite cortisone. modulates intracellular glucocorticoid levels, thus protecting the nonselective mineralocorticoid receptor from occupation by glucocorticoids.
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| BioChemical Class |
Short-chain dehydrogenases reductase
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| UniProt ID | ||||||
| EC Number |
EC 1.1.1.-
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| Sequence |
MERWPWPSGGAWLLVAARALLQLLRSDLRLGRPLLAALALLAALDWLCQRLLPPPAALAV
LAAAGWIALSRLARPQRLPVATRAVLITGCDSGFGKETAKKLDSMGFTVLATVLELNSPG AIELRTCCSPRLRLLQMDLTKPGDISRVLEFTKAHTTSTGLWGLVNNAGHNEVVADAELS PVATFRSCMEVNFFGALELTKGLLPLLRSSRGRIVTVGSPAGDMPYPCLGAYGTSKAAVA LLMDTFSCELLPWGVKVSIIQPGCFKTESVRNVGQWEKRKQLLLANLPQELLQAYGKDYI EHLHGQFLHSLRLAMSDLTPVVDAITDALLAARPRRRYYPGQGLGLMYFIHYYLPEGLRR RFLQAFFISHCLPRALQPGQPGTTPPQDAAQDPNLSPGPSPAVAR Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| HIT2.0 ID | T92E71 | |||||
| Drugs and Modes of Action | Top | |||||
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| Clinical Trial Drug(s) | [+] 1 Clinical Trial Drugs | + | ||||
| 1 | RG-7234 | Drug Info | Phase 2 | Type-2 diabetes | [2] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 5 Inhibitor drugs | + | ||||
| 1 | RG-7234 | Drug Info | [1] | |||
| 2 | 11-keto-beta-boswellicacid | Drug Info | [3] | |||
| 3 | 3-acetyl-11-keto-beta-boswellic acid | Drug Info | [3] | |||
| 4 | Ganoderic acid A | Drug Info | [3] | |||
| 5 | [(125)I] RB129 | Drug Info | [4] | |||
| 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 | ||
| Target Poor or Non Binders | Top | |||||
|---|---|---|---|---|---|---|
| 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 | Steroid hormone biosynthesis | |||||
| 2 | Aldosterone-regulated sodium reabsorption | |||||
| NetPath Pathway | [+] 1 NetPath Pathways | + | ||||
| 1 | EGFR1 Signaling Pathway | |||||
| Pathwhiz Pathway | [+] 1 Pathwhiz Pathways | + | ||||
| 1 | Steroidogenesis | |||||
| Reactome | [+] 1 Reactome Pathways | + | ||||
| 1 | Glucocorticoid biosynthesis | |||||
| WikiPathways | [+] 2 WikiPathways | + | ||||
| 1 | Prostaglandin Synthesis and Regulation | |||||
| 2 | Glucocorticoid & Mineralcorticoid Metabolism | |||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
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| REF 1 | New Therapeutic Strategies for Type 2 Diabetes: Small Molecule Approaches. 2012. Chapter 5. Page(131). | |||||
| REF 2 | ClinicalTrials.gov (NCT00823680) A Study of RO5093151 and RO5027838 in Patients With Type 2 Diabetes Mellitus on a Stable Dose of Metformin. U.S. National Institutes of Health. | |||||
| REF 3 | 11beta-Hydroxysteroid dehydrogenase 1 inhibiting constituents from Eriobotrya japonica revealed by bioactivity-guided isolation and computational a... Bioorg Med Chem. 2010 Feb 15;18(4):1507-15. | |||||
| REF 4 | Abnormal expression of 11 beta-hydroxysteroid dehydrogenase type 2 in human pituitary adenomas: a prereceptor determinant of pituitary cell proliferation. Oncogene. 2003 Mar 20;22(11):1663-7. | |||||
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