Target Information
| Target General Information | Top | |||||
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| Target ID |
T46365
(Former ID: TTDR00116)
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| Target Name |
M-phase inducer phosphatase 2 (MPIP2)
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| Synonyms |
Dual specificity phosphatase Cdc25B; Cdc25B phosphatase; CDC25HU2
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| Gene Name |
CDC25B
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Lung cancer [ICD-11: 2C25] | |||||
| Function |
Required for G2/M phases of the cell cycle progression and abscission during cytokinesis in a ECT2-dependent manner. Directly dephosphorylates CDK1 and stimulates its kinase activity. The three isoforms seem to have a different level of activity. Tyrosine protein phosphatase which functions as a dosage-dependent inducer of mitotic progression.
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| BioChemical Class |
Phosphoric monoester hydrolase
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| UniProt ID | ||||||
| EC Number |
EC 3.1.3.48
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| Sequence |
MEVPQPEPAPGSALSPAGVCGGAQRPGHLPGLLLGSHGLLGSPVRAAASSPVTTLTQTMH
DLAGLGSETPKSQVGTLLFRSRSRLTHLSLSRRASESSLSSESSESSDAGLCMDSPSPMD PHMAEQTFEQAIQAASRIIRNEQFAIRRFQSMPVRLLGHSPVLRNITNSQAPDGRRKSEA GSGAASSSGEDKENDGFVFKMPWKPTHPSSTHALAEWASRREAFAQRPSSAPDLMCLSPD RKMEVEELSPLALGRFSLTPAEGDTEEDDGFVDILESDLKDDDAVPPGMESLISAPLVKT LEKEEEKDLVMYSKCQRLFRSPSMPCSVIRPILKRLERPQDRDTPVQNKRRRSVTPPEEQ QEAEEPKARVLRSKSLCHDEIENLLDSDHRELIGDYSKAFLLQTVDGKHQDLKYISPETM VALLTGKFSNIVDKFVIVDCRYPYEYEGGHIKTAVNLPLERDAESFLLKSPIAPCSLDKR VILIFHCEFSSERGPRMCRFIRERDRAVNDYPSLYYPEMYILKGGYKEFFPQHPNFCEPQ DYRPMNHEAFKDELKTFRLKTRSWAGERSRRELCSRLQDQ Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| HIT2.0 ID | T10AWW | |||||
| Drugs and Modes of Action | Top | |||||
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| Clinical Trial Drug(s) | [+] 1 Clinical Trial Drugs | + | ||||
| 1 | Avastin+/-Tarceva | Drug Info | Phase 3 | Non-small-cell lung cancer | [2] | |
| Discontinued Drug(s) | [+] 1 Discontinued Drugs | + | ||||
| 1 | MX-7065 | Drug Info | Terminated | Solid tumour/cancer | [3] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 17 Inhibitor drugs | + | ||||
| 1 | Avastin+/-Tarceva | Drug Info | [1] | |||
| 2 | MX-7065 | Drug Info | [4] | |||
| 3 | 2-Sulfhydryl-Ethanol | Drug Info | [5] | |||
| 4 | 3-isopropyl-4-(phenylamino)naphthalene-1,2-dione | Drug Info | [6] | |||
| 5 | 3-isopropyl-4-(phenylthio)naphthalene-1,2-dione | Drug Info | [6] | |||
| 6 | 3-isopropyl-4-phenylnaphthalene-1,2-dione | Drug Info | [6] | |||
| 7 | 4-(p-toluidino)-3-isopropylnaphthalene-1,2-dione | Drug Info | [6] | |||
| 8 | 4-ethoxynaphthalene-1,2-dione | Drug Info | [1] | |||
| 9 | 5,6,7,8-tetrahydroanthracene-1,4-dione | Drug Info | [1] | |||
| 10 | 6,7-dibromoquinoline-5,8-dione | Drug Info | [7] | |||
| 11 | ADOCIAQUINONE B | Drug Info | [7] | |||
| 12 | ANTHRAQUINONE | Drug Info | [1] | |||
| 13 | Cysteine Sulfenic Acid | Drug Info | [8] | |||
| 14 | Cysteinesulfonic Acid | Drug Info | [5] | |||
| 15 | Double Oxidized Cysteine | Drug Info | [5] | |||
| 16 | Methyl Mercury Ion | Drug Info | [5] | |||
| 17 | NSC-95397 | Drug Info | [7] | |||
| 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 | ||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
|---|---|---|---|---|---|---|
| Target Poor or Non Binders | ||||||
| Target Regulators | Top | |||||
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| Target-regulating microRNAs | ||||||
| Target-interacting Proteins | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| KEGG Pathway | [+] 4 KEGG Pathways | + | ||||
| 1 | MAPK signaling pathway | |||||
| 2 | Cell cycle | |||||
| 3 | Progesterone-mediated oocyte maturation | |||||
| 4 | MicroRNAs in cancer | |||||
| NetPath Pathway | [+] 3 NetPath Pathways | + | ||||
| 1 | IL2 Signaling Pathway | |||||
| 2 | TGF_beta_Receptor Signaling Pathway | |||||
| 3 | Wnt Signaling Pathway | |||||
| PID Pathway | [+] 4 PID Pathways | + | ||||
| 1 | PLK1 signaling events | |||||
| 2 | FOXM1 transcription factor network | |||||
| 3 | p38 signaling mediated by MAPKAP kinases | |||||
| 4 | Aurora A signaling | |||||
| Reactome | [+] 3 Reactome Pathways | + | ||||
| 1 | Cyclin B2 mediated events | |||||
| 2 | Cyclin A/B1 associated events during G2/M transition | |||||
| 3 | Cyclin A:Cdk2-associated events at S phase entry | |||||
| WikiPathways | [+] 8 WikiPathways | + | ||||
| 1 | Senescence and Autophagy in Cancer | |||||
| 2 | MAPK Signaling Pathway | |||||
| 3 | Retinoblastoma (RB) in Cancer | |||||
| 4 | Prostate Cancer | |||||
| 5 | Integrated Breast Cancer Pathway | |||||
| 6 | Integrated Cancer pathway | |||||
| 7 | Mitotic G2-G2/M phases | |||||
| 8 | Cell Cycle | |||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
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| REF 1 | Bioactivities of simplified adociaquinone B and naphthoquinone derivatives against Cdc25B, MKP-1, and MKP-3 phosphatases. Bioorg Med Chem. 2009 Mar 15;17(6):2276-81. | |||||
| REF 2 | Clinical pipeline report, company report or official report of Roche. | |||||
| REF 3 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016615) | |||||
| REF 4 | Handbook of Assay Development in Drug Discovery, Lisa K. Minor, 2013. Page(11). | |||||
| REF 5 | How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | |||||
| REF 6 | Synthesis of miltirone analogues as inhibitors of Cdc25 phosphatases. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1905-8. | |||||
| REF 7 | Novel naphthoquinone and quinolinedione inhibitors of CDC25 phosphatase activity with antiproliferative properties. Bioorg Med Chem. 2008 Oct 1;16(19):9040-9. | |||||
| REF 8 | 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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