Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T04820
|
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| Former ID |
TTDR00301
|
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| Target Name |
Cyclin-dependent protein kinase Pfmrk
|
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| Gene Name |
Pfmrk
|
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| Synonyms |
MO15-related protein kinase Pfmrk; Pfmrk
|
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| Target Type |
Research
|
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| Disease | Malaria [ICD10: B54] | ||||
| BioChemical Class |
Kinase
|
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| Target Validation |
T04820
|
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| UniProt ID | |||||
| EC Number |
EC 2.7.1.37
|
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| Sequence |
MENNSTERYIFKPNFLGEGSYGKVYKAYDTILKKEVAIKKMKLNEISNYIDDCGINFVLL
REIKIMKEIKHKNIMSALDLYCEKDYINLVMEIMDYDLSKIINRKIFLTDSQKKCILLQI LNGLNVLHKYYFMHRDLSPANIFINKKGEVKLADFGLCTKYGYDMYSDKLFRDKYKKNLN LTSKVVTLWYRAPELLLGSNKYNSSIDMWSFGCIFAELLLQKALFPGENEIDQLGKIFFL LGTPNENNWPEALCLPLYTEFTKATKKDFKTYFKIDDDDCIDLLTSFLKLNAHERISAED AMKHRYFFNDPLPCDISQLPFNDL |
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| Inhibitor | (E)-1-(4-Nitro-phenyl)-3-pyridin-2-yl-propenone | Drug Info | [1] | ||
| 2,5-dichloro-N-p-tolylthiophene-3-sulfonamide | Drug Info | [2] | |||
| 2,5-dichloro-N-phenylthiophene-3-sulfonamide | Drug Info | [2] | |||
| 2-chloro-N-(o-tolylcarbamoyl)benzamide | Drug Info | [2] | |||
| 3-[3-(2-Hydroxy-ethoxy)-phenyl]-1H-quinolin-2-one | Drug Info | [1] | |||
| 5-chloro-4-nitrothiophene-2-sulfonamide | Drug Info | [2] | |||
| 5-Nitro-1H-indole-2,3-dione | Drug Info | [1] | |||
| APIGENIN | Drug Info | [1] | |||
| KENPAULLONE | Drug Info | [1] | |||
| N'-(2-fluorobenzoyl)-2-naphthohydrazide | Drug Info | [2] | |||
| N-(2-aminoethyl)isoquinoline-5-sulfonamide | Drug Info | [3] | |||
| Oxindole derivative | Drug Info | [4] | |||
| Thiophene sulfonamide | Drug Info | [5] | |||
| WR-080539 | Drug Info | [6] | |||
| WR-089120 | Drug Info | [6] | |||
| WR-190706 | Drug Info | [6] | |||
| WR-203581 | Drug Info | [6] | |||
| WR-289009 | Drug Info | [6] | |||
| WR-289010 | Drug Info | [6] | |||
| WR-289012 | Drug Info | [6] | |||
| WR-289016 | Drug Info | [6] | |||
| References | |||||
| REF 1 | J Med Chem. 2004 Oct 21;47(22):5418-26.A three-dimensional in silico pharmacophore model for inhibition of Plasmodium falciparum cyclin-dependent kinases and discovery of different classes of novel Pfmrk specific inhibitors. | ||||
| REF 2 | Activity of substituted thiophene sulfonamides against malarial and mammalian cyclin dependent protein kinases, Bioorg. Med. Chem. Lett. 20(13):3863-3867 (2010). | ||||
| REF 3 | Bioorg Med Chem Lett. 2007 Sep 1;17(17):4961-6. Epub 2007 Jun 12.Evaluation of broad spectrum protein kinase inhibitors to probe the architecture of the malarial cyclin dependent protein kinase Pfmrk. | ||||
| REF 4 | Novel molecular targets for antimalarial chemotherapy. Int J Antimicrob Agents. 2007 Jul;30(1):4-10. Epub 2007 Mar 6. | ||||
| REF 5 | Novel molecular targets for antimalarial drug development. Chem Biol Drug Des. 2008 Apr;71(4):287-97. Epub 2008 Feb 22. | ||||
| REF 6 | Bioorg Med Chem Lett. 2009 Apr 1;19(7):1982-5. Epub 2009 Feb 13.Selective inhibition of Pfmrk, a Plasmodium falciparum CDK, by antimalarial 1,3-diaryl-2-propenones. | ||||
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