Alvocidib
| Alvocidib | |
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2-(2-chlorophenyl)-5,7-dihydroxy-8-[(3S,4R)-3-hydroxy-1-methyl-4-piperidinyl]-4-chromenone |
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| Identifiers | |
| CAS number | 146426-40-6  |
| PubChem | 5287969 |
| ChemSpider | 4450222  |
| DrugBank | DB03496 |
| MeSH | Flavopiridol |
| ChEMBL | CHEMBL428690 |
| Jmol-3D images | Image 1 |
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| Properties | |
| Molecular formula | C21H20ClNO5 |
| Molar mass | 401.8402 |
 (verify) (what is:  / ?)Except where noted otherwise, data are given for materials in their standard state (at 25 °C, 100 kPa) |
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| Infobox references | |
Alvocidib (INN; also known as Flavopiridol or HMR-1275) is a cyclin-dependent kinase inhibitor under clinical development for the treatment of chronic lymphocytic leukemia. It has been studied also for the treatment of arthritis[1] and atherosclerotic plaque formation [2] The target of Flavopiridol is the positive transcription elongation factor P-TEFb.[3][4] Treatment of cells with Flavopiridol leads to inhibition of P-TEFb and the loss of mRNA production.[5][6]
References [edit]
- ^ Sekine C, Sugihara T, Miyake S, et al. (February 2008). "Successful treatment of animal models of rheumatoid arthritis with small-molecule cyclin-dependent kinase inhibitors". J. Immunol. 180 (3): 1954–61. PMID 18209094.
- ^ Meshel AS, Ruef J, Hu Z, Horaist C, Ballinger CA, Thompson LJ, Subbarao VD, Dumont JA, Patterson C. (August 1999). "Flavopiridol inhibits smooth muscle cell proliferation in vitro and neointimal formation In vivo after carotid injury in the rat.". Circulation 10 (100): 659–65. PMID 10441105.
- ^ Chao, S.H.; Fujinaga K, Marion JE, Taube R, Sauseville EA, Senderowicz AM, Peterlin, BM, Price DH (2000). "Flavopiridol inhibits P-TEFb and blocks HIV-1 replication.". J. Biol. Chem 275 (37): 28345–8. doi:10.1074/jbc.C000446200. PMID 10906320.
- ^ Chao, S.H.; Price DH (2001). "Flavopiridol inactivates P-TEFb and blocks most RNA polymerase II transcription in vivo.". J. Biol. Chem 276 (34): 31793–9. doi:10.1074/jbc.M102306200. PMID 11431468.
- ^ Cheng, Bo; Li T, Rahl PB, Adamson TE, Loudas NB, Guo J, Varzavand K, Cooper JJ, Hu X, Gnatt A, Young RA, Price DH. "Functional association of Gdown1 with RNA polymerase II poised on human genes.". Molecular Cell 45: 38–50. doi:10.1016/j.molcel.2011.10.022. PMID 22244331.
- ^ Rahl, PB; Lin CY, Seila AC, Flynn RA, McCuine S, Burge CB, Sharp PA, Young RA. "c-Myc regulates transcriptional pause release". Cell 141: 432–45. doi:10.1016/j.cell.2010.03.030. PMC 2864022. PMID 20434984.
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