Abexinostat

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Psoraleno
Abexinostat.svg
General
Fórmula molecular ?H23N3O5 
Identificadores
Número CAS 783355-60-2[1]
ChemSpider 9924562
PubChem 11749858
KEGG D10060
[editar datos en Wikidata]

Abexinostat (INN,[2] anteriormente PCI-24781 o CRA-024781) con fórmula C21H23N3O5, es un candidato a fármaco experimental para el tratamiento del cáncer.[3] Actualmente se encuentra en desarrollo por Pharmacyclics y se encuentra en ensayos clínicos de fase II para el linfoma de células B.[4] Los estudios pre-clínicos sugieren también el potencial para el tratamiento de otros diferentes tipos de cáncer.[5] [6] [7] [8]

Abexinostat ejerce su efecto como un inhibidor de la Histona deacetilasa.[9] [10]

Referencias[editar]

  1. Número CAS
  2. WHO Drug Information, Vol. 25, No. 2, 2011
  3. Abexinostat, NCI Cancer Dictionary
  4. Abexinostat HCl (PCI-24781), PanHDAC-inhibitor, Pharmacyclics
  5. Bhalla, S; Balasubramanian, S; David, K; Sirisawad, M; Buggy, J; Mauro, L; Prachand, S; Miller, R; Gordon, LI; Evens, AM (2009). «PCI-24781 induces caspase and reactive oxygen species-dependent apoptosis through NF-kappaB mechanisms and is synergistic with bortezomib in lymphoma cells». Clinical cancer research : an official journal of the American Association for Cancer Research 15 (10): 3354–65. doi:10.1158/1078-0432.CCR-08-2365. PMC 2704489. PMID 19417023. 
  6. Lopez, G; Liu, J; Ren, W; Wei, W; Wang, S; Lahat, G; Zhu, QS; Bornmann, WG; McConkey, DJ; Pollock, RE; Lev, DC (2009). «Combining PCI-24781, a novel histone deacetylase inhibitor, with chemotherapy for the treatment of soft tissue sarcoma». Clinical cancer research : an official journal of the American Association for Cancer Research 15 (10): 3472–83. doi:10.1158/1078-0432.CCR-08-2714. PMID 19417021. 
  7. Rivera-Del Valle, N; Gao, S; Miller, CP; Fulbright, J; Gonzales, C; Sirisawad, M; Steggerda, S; Wheler, J; Balasubramanian, S; Chandra, J (2010). «PCI-24781, a Novel Hydroxamic Acid HDAC Inhibitor, Exerts Cytotoxicity and Histone Alterations via Caspase-8 and FADD in Leukemia Cells». International journal of cell biology 2010: 207420. doi:10.1155/2010/207420. PMC 2817379. PMID 20145726. 
  8. Yang, C; Choy, E; Hornicek, FJ; Wood, KB; Schwab, JH; Liu, X; Mankin, H; Duan, Z (2011). «Histone deacetylase inhibitor (HDACI) PCI-24781 potentiates cytotoxic effects of doxorubicin in bone sarcoma cells». Cancer chemotherapy and pharmacology 67 (2): 439–46. doi:10.1007/s00280-010-1344-7. PMID 20461381. 
  9. Buggy, JJ; Cao, ZA; Bass, KE; Verner, E; Balasubramanian, S; Liu, L; Schultz, BE; Young, PR; Dalrymple, SA (2006). «CRA-024781: A novel synthetic inhibitor of histone deacetylase enzymes with antitumor activity in vitro and in vivo». Molecular cancer therapeutics 5 (5): 1309–17. doi:10.1158/1535-7163.MCT-05-0442. PMID 16731764. 
  10. Adimoolam, S; Sirisawad, M; Chen, J; Thiemann, P; Ford, JM; Buggy, JJ (2007). «HDAC inhibitor PCI-24781 decreases RAD51 expression and inhibits homologous recombination». Proceedings of the National Academy of Sciences of the United States of America 104 (49): 19482–7. doi:10.1073/pnas.0707828104. PMC 2148315. PMID 18042714. 

Bibliografía[editar]