Acid-mediated Lipinski's second rule: application to drug design and targeting in cancer.
Eur Biophys J
; 43(4-5): 199-206, 2014 May.
Article
em En
| MEDLINE
| ID: mdl-24687685
ABSTRACT
With a predicted 382.4 per 100,000 people expected to suffer from some form of malignant neoplasm by 2015, and a current death toll of 1 out of 8 deaths worldwide, improving treatment and/or drug design is an essential focus of cancer research. Multi-drug resistance is the leading cause of chemotherapeutic failure, and delivery of anticancer drugs to the inside of cancerous cells is another major challenge. Fifteen years ago, in a completely different field in which improving drug delivery is the objective, the bioavailability of oral compounds, Christopher Lipinski formulated some rules that are still used by the pharmaceutical industry as rules of thumb to improve drug delivery to their target. Although Lipinski's rules were not formulated to improve delivery of antineoplastic drugs to the inside of cancer cells, it is interesting to note that the problems are similar. On the basis of the strong similarity between the fields, we discuss how they can be connected and how new drug targets can be defined in cancer.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Desenho de Fármacos
/
Terapia de Alvo Molecular
/
Neoplasias
Tipo de estudo:
Prognostic_studies
Idioma:
En
Revista:
Eur Biophys J
Assunto da revista:
BIOFISICA
Ano de publicação:
2014
Tipo de documento:
Article