Substituted purine and 7-deazapurine compounds as modulators of epigenetic enzymes: a patent evaluation (WO2012075381).
Expert Opin Ther Pat
; 23(4): 537-43, 2013 Apr.
Article
em En
| MEDLINE
| ID: mdl-23448241
ABSTRACT
The patent presents 140 purine and 7-azapurine derivatives as potent inhibitors of DOT1L histone methyltransferase that might be useful in the treatment of leukemia with MLL rearrangements. It is becoming more and more evident that the deregulation of chromatin modifiers such as DOT1L plays a critical role in tumorigenesis. As yet, the number of pharmaceutical agents targeting chromatin modifiers is still limited. The market for such compounds has been estimated to be potentially as large as one third of all cancer patients. Overall, the prospective of a targeted product (i.e., a drug targeting a commonly affected chromatin modifier) is very promising, and exponentially growing investments into this market are anticipated.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Purinas
/
Leucemia
/
Epigênese Genética
/
Inibidores Enzimáticos
/
Terapia de Alvo Molecular
/
Metiltransferases
/
Antineoplásicos
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Expert Opin Ther Pat
Assunto da revista:
TERAPEUTICA
Ano de publicação:
2013
Tipo de documento:
Article
País de afiliação:
Alemanha