Inhibitors of urokinase reduce size of prostate cancer xenografts in severe combined immunodeficient mice.
Cancer Res
; 57(4): 559-63, 1997 Feb 15.
Article
em En
| MEDLINE
| ID: mdl-9044824
ABSTRACT
Proteolytic enzymes are required to mediate tumor cell invasion and metastasis. The urokinase plasminogen activator (uPA) is commonly overexpressed by many human cancers. Therefore, uPA is a logical target to inhibit cancer invasion and metastasis. However, uPA inhibitors also reduce tumor growth. We used a mutated form of plasminogen activator inhibitor type 1 to conform a correlation between the inactivation of uPA and tumor size; we have compared these results with the action of p-aminobenzamidine and amiloride, known inhibitors of uPA. Our results show that blocking uPA by uPA inhibitors reduces tumor size in experimental animals. Our molecular simulation of docking inhibitors to the urokinase reveals that all tested small molecule inhibitors bind in proximity of uPA's specificity pocket, a critical site for future search of novel anticancer uPA inhibitors.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Benzamidinas
/
Ativadores de Plasminogênio
/
Ativador de Plasminogênio Tipo Uroquinase
/
Amilorida
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Antineoplásicos
Limite:
Animals
/
Humans
/
Male
Idioma:
En
Revista:
Cancer Res
Ano de publicação:
1997
Tipo de documento:
Article
País de afiliação:
Estados Unidos
País de publicação:
EEUU
/
ESTADOS UNIDOS
/
ESTADOS UNIDOS DA AMERICA
/
EUA
/
UNITED STATES
/
UNITED STATES OF AMERICA
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US
/
USA