Target Information
| Target General Information | Top | |||||
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| Target ID |
T60366
(Former ID: TTDS00313)
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| Target Name |
Ornithine decarboxylase (ODC1)
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| Synonyms |
ODC
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| Gene Name |
ODC1
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | African trypanosomiasis [ICD-11: 1F51] | |||||
| Function |
Polyamines are essential for cell proliferation and are implicated in cellular processes, ranging from DNA replication to apoptosis. Catalyzes the first and rate-limiting step of polyamine biosynthesis that converts ornithine into putrescine, which is the precursor for the polyamines, spermidine and spermine.
Click to Show/Hide
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| BioChemical Class |
Carbon-carbon lyase
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| UniProt ID | ||||||
| EC Number |
EC 4.1.1.17
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| Sequence |
MNNFGNEEFDCHFLDEGFTAKDILDQKINEVSSSDDKDAFYVADLGDILKKHLRWLKALP
RVTPFYAVKCNDSKAIVKTLAATGTGFDCASKTEIQLVQSLGVPPERIIYANPCKQVSQI KYAANNGVQMMTFDSEVELMKVARAHPKAKLVLRIATDDSKAVCRLSVKFGATLRTSRLL LERAKELNIDVVGVSFHVGSGCTDPETFVQAISDARCVFDMGAEVGFSMYLLDIGGGFPG SEDVKLKFEEITGVINPALDKYFPSDSGVRIIAEPGRYYVASAFTLAVNIIAKKIVLKEQ TGSDDEDESSEQTFMYYVNDGVYGSFNCILYDHAHVKPLLQKRPKPDEKYYSSSIWGPTC DGLDRIVERCDLPEMHVGDWMLFENMGAYTVAAASTFNGFQRPTIYYVMSGPAWQLMQQF QNPDFPPEVEEQDASTLPVSCAWESGMKRHRAACASASINV Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| ADReCS ID | BADD_A01759 ; BADD_A02053 ; BADD_A05554 | |||||
| HIT2.0 ID | T02WMA | |||||
| Drugs and Modes of Action | Top | |||||
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| Approved Drug(s) | [+] 1 Approved Drugs | + | ||||
| 1 | Eflornithine | Drug Info | Approved | African trypanosomiasis | [2], [3] | |
| Discontinued Drug(s) | [+] 1 Discontinued Drugs | + | ||||
| 1 | Putrescine | Drug Info | Discontinued in Phase 2 | Burn and burn infection | [4], [5] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 18 Inhibitor drugs | + | ||||
| 1 | Eflornithine | Drug Info | [1], [6] | |||
| 2 | Putrescine | Drug Info | [6] | |||
| 3 | (2R,5R)-delta-methyl-alpha-acetylenic putrescine | Drug Info | [1] | |||
| 4 | 1-Amino-3-(aminoxy)-2-propanol Dihydrochloride | Drug Info | [7] | |||
| 5 | 3-(Aminooxy)propan-1-amine hydrochloride | Drug Info | [7] | |||
| 6 | 3-methoxy-4-hydroxylonchocarpin | Drug Info | [8] | |||
| 7 | 4-hydroxylonchocarpin | Drug Info | [8] | |||
| 8 | Alpha-monofluoromethyl-3,4-dehydroornithine | Drug Info | [1] | |||
| 9 | Alpha-monofluoromethyl-3,4-dehydroornithine ethyl ester | Drug Info | [1] | |||
| 10 | Alpha-monofluoromethyl-3,4-dehydroornithine methyl ester | Drug Info | [1] | |||
| 11 | AMXT-1501 | Drug Info | [9] | |||
| 12 | APA | Drug Info | [10], [11] | |||
| 13 | G418 | Drug Info | [6] | |||
| 14 | LONCHOCARPUSONE | Drug Info | [8] | |||
| 15 | N'-Pyridoxyl-Lysine-5'-Monophosphate | Drug Info | [6] | |||
| 16 | N-Pyridoxyl-Glycine-5-Monophosphate | Drug Info | [6] | |||
| 17 | Pyridoxine-5'-Phosphate | Drug Info | [6] | |||
| 18 | ZAPOTIN | Drug Info | [12] | |||
| 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 | |||||
|---|---|---|---|---|---|---|
| Target-regulating Transcription Factors | ||||||
| Target Profiles in Patients | Top | |||||
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| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
|---|---|---|---|---|---|---|
| BioCyc | [+] 1 BioCyc Pathways | + | ||||
| 1 | Putrescine biosynthesis I | |||||
| NetPath Pathway | [+] 3 NetPath Pathways | + | ||||
| 1 | TCR Signaling Pathway | |||||
| 2 | IL2 Signaling Pathway | |||||
| 3 | TGF_beta_Receptor Signaling Pathway | |||||
| Panther Pathway | [+] 2 Panther Pathways | + | ||||
| 1 | Ornithine degradation | |||||
| 2 | CCKR signaling map ST | |||||
| Pathwhiz Pathway | [+] 1 Pathwhiz Pathways | + | ||||
| 1 | Spermidine and Spermine Biosynthesis | |||||
| PID Pathway | [+] 1 PID Pathways | + | ||||
| 1 | Validated targets of C-MYC transcriptional activation | |||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
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| REF 1 | Plasmodium falciparum and Plasmodium berghei: effects of ornithine decarboxylase inhibitors on erythrocytic schizogony. Exp Parasitol. 1987 Oct;64(2):237-43. | |||||
| REF 2 | 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. (Ligand id: 5176). | |||||
| REF 3 | Opportunities and challenges in antiparasitic drug discovery. Nat Rev Drug Discov. 2005 Sep;4(9):727-40. | |||||
| REF 4 | 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. (Ligand id: 2388). | |||||
| 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 800013366) | |||||
| REF 6 | How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | |||||
| REF 7 | Selective delivery of 2-hydroxy APA to Trypanosoma brucei using the melamine motif. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4364-6. | |||||
| REF 8 | New bioactive flavonoids and stilbenes in cub resin insecticide. J Nat Prod. 1999 Feb;62(2):205-10. | |||||
| 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: 1276). | |||||
| REF 10 | 2-substituted 3-(aminooxy)propanamines as inhibitors of ornithine decarboxylase: synthesis and biological activity. J Med Chem. 1992 Apr 17;35(8):1339-44. | |||||
| REF 11 | Antileishmanial effect of 3-aminooxy-1-aminopropane is due to polyamine depletion. Antimicrob Agents Chemother. 2007 Feb;51(2):528-34. | |||||
| REF 12 | Synthesis and cancer chemopreventive activity of zapotin, a natural product from Casimiroa edulis. J Med Chem. 2007 Jan 25;50(2):350-5. | |||||
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