Alvocidib

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Alvocidib
Flavopiridol.svg
Identifiers
CAS number 146426-40-6 N
PubChem 5287969
ChemSpider 4450222 YesY
DrugBank DB03496
MeSH Flavopiridol
ChEMBL CHEMBL428690 N
Jmol-3D images Image 1
Properties
Molecular formula C21H20ClNO5
Molar mass 401.8402
Except where noted otherwise, data are given for materials in their standard state (at 25 °C (77 °F), 100 kPa)
 N (verify) (what is: YesY/N?)
Infobox references

Alvocidib (INN; also known as Flavopiridol or HMR-1275) is a flavonoid alkaloid CDK9 kinase inhibitor under clinical development for the treatment of chronic lymphocytic leukemia, by Sanofi. 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]

  1. ^ Sekine C, Sugihara T, Miyake S, Hirai H, Yoshida M, Miyasaka N, Kohsaka H (2008). "Successful treatment of animal models of rheumatoid arthritis with small-molecule cyclin-dependent kinase inhibitors". J. Immunol. 180 (3): 1954–61. doi:10.4049/jimmunol.180.3.1954. PMID 18209094. 
  2. ^ Ruef J, Meshel AS, Hu Z, Horaist C, Ballinger CA, Thompson LJ, Subbarao VD, Dumont JA, Patterson C (1999). "Flavopiridol inhibits smooth muscle cell proliferation in vitro and neointimal formation In vivo after carotid injury in the rat". Circulation 100 (6): 659–65. doi:10.1161/01.cir.100.6.659. PMID 10441105. 
  3. ^ Chao SH, Fujinaga K, Marion JE, Taube R, Sausville 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. 
  4. ^ Chao SH, 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. 
  5. ^ Cheng B, Li T, Rahl PB, Adamson TE, Loudas NB, Guo J, Varzavand K, Cooper JJ, Hu X, Gnatt A, Young RA, Price DH (2012). "Functional association of Gdown1 with RNA polymerase II poised on human genes". Mol. Cell 45 (1): 38–50. doi:10.1016/j.molcel.2011.10.022. PMC 3259526. PMID 22244331. 
  6. ^ Rahl PB, Lin CY, Seila AC, Flynn RA, McCuine S, Burge CB, Sharp PA, Young RA (2010). "c-Myc regulates transcriptional pause release". Cell 141 (3): 432–45. doi:10.1016/j.cell.2010.03.030. PMC 2864022. PMID 20434984.