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.
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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 | |||||
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Target-regulating Transcription Factors |
Target Profiles in Patients | Top | |||||
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Target Expression Profile (TEP) |
Target Affiliated Biological Pathways | Top | |||||
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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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