Target Information
| Target General Information | Top | |||||
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| Target ID |
T58470
(Former ID: TTDR00224)
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| Target Name |
Cyclin A2 (CCNA2)
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| Synonyms |
Cyclin-A2; Cyclin-A; Cyclin A; CCNA
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| Gene Name |
CCNA2
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| Target Type |
Literature-reported target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Retina cancer [ICD-11: 2D02] | |||||
| Function |
Functions through the formation of specific serine/threonine protein kinase holoenzyme complexes with the cyclin-dependent protein kinases CDK1 or CDK2. The cyclin subunit confers the substrate specificity of these complexes and differentially interacts with and activates CDK1 and CDK2 throughout the cell cycle. Cyclin which controls both the G1/S and the G2/M transition phases of the cell cycle.
Click to Show/Hide
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| UniProt ID | ||||||
| Sequence |
MLGNSAPGPATREAGSALLALQQTALQEDQENINPEKAAPVQQPRTRAALAVLKSGNPRG
LAQQQRPKTRRVAPLKDLPVNDEHVTVPPWKANSKQPAFTIHVDEAEKEAQKKPAESQKI EREDALAFNSAISLPGPRKPLVPLDYPMDGSFESPHTMDMSIILEDEKPVSVNEVPDYHE DIHTYLREMEVKCKPKVGYMKKQPDITNSMRAILVDWLVEVGEEYKLQNETLHLAVNYID RFLSSMSVLRGKLQLVGTAAMLLASKFEEIYPPEVAEFVYITDDTYTKKQVLRMEHLVLK VLTFDLAAPTVNQFLTQYFLHQQPANCKVESLAMFLGELSLIDADPYLKYLPSVIAGAAF HLALYTVTGQSWPESLIRKTGYTLESLKPCLMDLHQTYLKAPQHAQQSIREKYKNSKYHG VSLLNPPETLNL Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| HIT2.0 ID | T86UXL | |||||
| Drugs and Modes of Action | Top | |||||
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| Discontinued Drug(s) | [+] 1 Discontinued Drugs | + | ||||
| 1 | PD-0183812 | Drug Info | Terminated | Retinoblastoma | [2] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 23 Inhibitor drugs | + | ||||
| 1 | PD-0183812 | Drug Info | [1] | |||
| 2 | 2,5-dichloro-N-p-tolylthiophene-3-sulfonamide | Drug Info | [3] | |||
| 3 | 3-((3,5-diamino-1H-pyrazol-4-yl)diazenyl)phenol | Drug Info | [4] | |||
| 4 | 4-(phenyldiazenyl)-1H-pyrazole-3,5-diamine | Drug Info | [4] | |||
| 5 | 4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol | Drug Info | [4] | |||
| 6 | 6-(3-Amino-benzyloxy)-9H-purin-2-ylamine | Drug Info | [5] | |||
| 7 | 6-(3-Methyl-benzyloxy)-9H-purin-2-ylamine | Drug Info | [5] | |||
| 8 | 6-(Cyclohex-3-enylmethoxy)-9H-purin-2-ylamine | Drug Info | [5] | |||
| 9 | 6-Cyclohexylmethoxy-pyrimidine-2,4,5-triamine | Drug Info | [6] | |||
| 10 | 6-O-Cyclohexylmethyl Guanine | Drug Info | [7] | |||
| 11 | aloisine A | Drug Info | [8] | |||
| 12 | GW-8510 | Drug Info | [9] | |||
| 13 | MERIOLIN 1 | Drug Info | [10] | |||
| 14 | MERIOLIN 2 | Drug Info | [10] | |||
| 15 | MERIOLIN 3 | Drug Info | [10] | |||
| 16 | MERIOLIN 4 | Drug Info | [10] | |||
| 17 | MERIOLIN 5 | Drug Info | [10] | |||
| 18 | MERIOLIN 6 | Drug Info | [10] | |||
| 19 | MERIOLIN 7 | Drug Info | [10] | |||
| 20 | MERIOLIN 8 | Drug Info | [10] | |||
| 21 | NU-6027 | Drug Info | [6] | |||
| 22 | Purvalanol A | Drug Info | [11] | |||
| 23 | RESCOVITINE | 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 microRNAs | ||||||
| Target-regulating Transcription Factors | ||||||
| Target-interacting Proteins | ||||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
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| REF 1 | Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases. J Med Chem. 2000 Nov 30;43(24):4606-16. | |||||
| REF 2 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014130) | |||||
| REF 3 | Activity of substituted thiophene sulfonamides against malarial and mammalian cyclin dependent protein kinases, Bioorg. Med. Chem. Lett. 20(13):3863-3867 (2010). | |||||
| REF 4 | 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. J Med Chem. 2006 Nov 2;49(22):6500-9. | |||||
| REF 5 | Probing the ATP ribose-binding domain of cyclin-dependent kinases 1 and 2 with O(6)-substituted guanine derivatives. J Med Chem. 2002 Aug 1;45(16):3381-93. | |||||
| REF 6 | 4-Alkoxy-2,6-diaminopyrimidine derivatives: inhibitors of cyclin dependent kinases 1 and 2. Bioorg Med Chem Lett. 2003 Jan 20;13(2):217-22. | |||||
| REF 7 | N2-substituted O6-cyclohexylmethylguanine derivatives: potent inhibitors of cyclin-dependent kinases 1 and 2. J Med Chem. 2004 Jul 15;47(15):3710-22. | |||||
| REF 8 | Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects. J Med Chem. 2003 Jan 16;46(2):222-36. | |||||
| REF 9 | Discovery and in vitro evaluation of potent TrkA kinase inhibitors: oxindole and aza-oxindoles. Bioorg Med Chem Lett. 2004 Feb 23;14(4):953-7. | |||||
| REF 10 | Meriolins (3-(pyrimidin-4-yl)-7-azaindoles): synthesis, kinase inhibitory activity, cellular effects, and structure of a CDK2/cyclin A/meriolin com... J Med Chem. 2008 Feb 28;51(4):737-51. | |||||
| REF 11 | The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315. | |||||
| REF 12 | Design, synthesis, and biological evaluation of novel pyrimidine derivatives as CDK2 inhibitors. Eur J Med Chem. 2010 Mar;45(3):1158-66. | |||||
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