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Alvocidib

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Alvocidib

Alvocidib
Identifiers
CAS number  N
PubChem
ChemSpider  YesY
DrugBank
MeSH
ChEMBL  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   YesY/N?)

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

  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.  
  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.  
  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.  
  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.  
  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.  
  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.  
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