Target Information
| Target General Information | Top | |||||
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| Target ID |
T25703
(Former ID: TTDC00134)
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| Target Name |
Heme oxygenase 1 (HMOX1)
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| Synonyms |
HO1; HO-1; HO
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| Gene Name |
HMOX1
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Neonatal hyperbilirubinaemia [ICD-11: KA87] | |||||
| Function |
Heme oxygenase cleaves the heme ring at the alpha methene bridge to form biliverdin. Biliverdin is subsequently converted to bilirubin by biliverdin reductase. Under physiological conditions, the activity of heme oxygenase is highest in the spleen, where senescent erythrocytes are sequestrated and destroyed. Exhibits cytoprotective effects since excess of free heme sensitizes cells to undergo apoptosis.
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| BioChemical Class |
Paired donor oxygen oxidoreductase
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| UniProt ID | ||||||
| EC Number |
EC 1.14.14.18
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| Sequence |
MERPQPDSMPQDLSEALKEATKEVHTQAENAEFMRNFQKGQVTRDGFKLVMASLYHIYVA
LEEEIERNKESPVFAPVYFPEELHRKAALEQDLAFWYGPRWQEVIPYTPAMQRYVKRLHE VGRTEPELLVAHAYTRYLGDLSGGQVLKKIAQKALDLPSSGEGLAFFTFPNIASATKFKQ LYRSRMNSLEMTPAVRQRVIEEAKTAFLLNIQLFEELQELLTHDTKDQSPSRAPGLRQRA SNKVQDSAPVETPRGKPPLNTRSQAPLLRWVLTLSFLVATVAVGLYAM Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| ADReCS ID | BADD_A02356 | |||||
| HIT2.0 ID | T86ROZ | |||||
| Drugs and Modes of Action | Top | |||||
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| Clinical Trial Drug(s) | [+] 1 Clinical Trial Drugs | + | ||||
| 1 | Stannsoporfin | Drug Info | Phase 2 | Neonatal hyperbilirubinemia | [2] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 10 Inhibitor drugs | + | ||||
| 1 | Stannsoporfin | Drug Info | [1] | |||
| 2 | 1-(adamantan-1-yl)-2-(1H-imidazol-1-yl)ethanone | Drug Info | [3] | |||
| 3 | 12-Phenylheme | Drug Info | [4] | |||
| 4 | 2-Phenylheme | Drug Info | [4] | |||
| 5 | 2-Propanol, Isopropanol | Drug Info | [4] | |||
| 6 | Biliverdine Ix Alpha | Drug Info | [4] | |||
| 7 | Formic Acid | Drug Info | [4] | |||
| 8 | Heme | Drug Info | [3] | |||
| 9 | Tin protoporphyrin | Drug Info | [5] | |||
| 10 | Verdoheme | Drug Info | [6] | |||
| 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 Regulators | Top | |||||
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| Target-regulating microRNAs | ||||||
| Target-regulating Transcription Factors | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| BioCyc | [+] 1 BioCyc Pathways | + | ||||
| 1 | Heme degradation | |||||
| KEGG Pathway | [+] 4 KEGG Pathways | + | ||||
| 1 | Porphyrin and chlorophyll metabolism | |||||
| 2 | HIF-1 signaling pathway | |||||
| 3 | Mineral absorption | |||||
| 4 | MicroRNAs in cancer | |||||
| Pathwhiz Pathway | [+] 1 Pathwhiz Pathways | + | ||||
| 1 | Porphyrin Metabolism | |||||
| PID Pathway | [+] 2 PID Pathways | + | ||||
| 1 | Validated transcriptional targets of AP1 family members Fra1 and Fra2 | |||||
| 2 | HIF-1-alpha transcription factor network | |||||
| Reactome | [+] 1 Reactome Pathways | + | ||||
| 1 | Iron uptake and transport | |||||
| WikiPathways | [+] 9 WikiPathways | + | ||||
| 1 | Oxidative Stress | |||||
| 2 | Transcriptional activation by NRF2 | |||||
| 3 | NRF2 pathway | |||||
| 4 | Nuclear Receptors Meta-Pathway | |||||
| 5 | miR-targeted genes in squamous cell - TarBase | |||||
| 6 | miR-targeted genes in muscle cell - TarBase | |||||
| 7 | miR-targeted genes in lymphocytes - TarBase | |||||
| 8 | miR-targeted genes in leukocytes - TarBase | |||||
| 9 | miR-targeted genes in epithelium - TarBase | |||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
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| REF 1 | Chemoprevention of severe neonatal hyperbilirubinemia. Semin Perinatol. 2004 Oct;28(5):365-8. | |||||
| REF 2 | ClinicalTrials.gov (NCT01887327) Study Evaluating the Safety and Efficacy of Two Doses of Stannsoporfin in Combination With Phototherapy in Neonates With Hyperbilirubinemia. U.S. National Institutes of Health. | |||||
| REF 3 | The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. | |||||
| REF 4 | How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | |||||
| REF 5 | Adenovirus-mediated heme oxygenase-1 gene delivery inhibits injury-induced vascular neointima formation. Circulation. 2001 Nov 27;104(22):2710-5. | |||||
| REF 6 | DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Nucleic Acids Res. 2011 Jan;39(Database issue):D1035-41. | |||||
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