HNF4-alpha ANTAGONIST AND USE THEREOF

Abstract

Provided is a hepatocyte nuclear factor 4 alpha (HNF4-α) antagonist and a use thereof. The HNF4-α antagonist selected in the present invention was confirmed to specifically bind to the ligand binding domain of HNF4-α, thereby inhibiting the activity of HNF4-α. The HNF4-α antagonist of the present invention can significantly reduce the expression of Wnt5a in a specific manner compared to that of the conventional known HNF4-α antagonists, and can also inhibit the growth of gastric cancer cells. Therefore, the HNF4-α antagonist of the present invention can not only be used as a pharmaceutical composition or a health functional food for preventing and treating cancer but can also be applied to a composition for treating or preventing diseases occurring due to the overexpression of HNF4-α.

What is claimed is: 
     
         1 . A hepatocyte nuclear factor 4 alpha (HNF4-α) antagonist comprising at least one selected from the group consisting of at least one type of a compound selected from the group consisting of the following Formula 1 and Formula 2; and salts thereof: 
       
         
           
           
               
               
           
         
         wherein R 1  to R 5  are each independently a hydrogen atom (H), an oxygen atom (O), a nitro group (NO 2 ), a halogen atom, a C 1-6  alkyl group substituted with one to six identical or different halogen atoms, or a C 1-6  alkyl group. 
       
     
     
         2 . The HNF4-α antagonist of  claim 1 , wherein Formula 1 is expressed by the following Formula 3: 
       
         
           
           
               
               
           
         
       
     
     
         3 . The HNF4-α antagonist of  claim 1 , wherein Formula 2 is expressed by the following Formula 4: 
       
         
           
           
               
               
           
         
       
     
     
         4 . The HNF4-α antagonist of  claim 1 , wherein Formula 1 and Formula 2 specifically bind to the ligand binding domain of HNF4-α. 
     
     
         5 . A hepatocyte nuclear factor 4 alpha (HNF4-α) antagonist comprising at least one type selected from the group consisting of at least one type of a compound selected from the group consisting of the following Formula 5 and Formulas 5-1 to 5-7, which are derivatives of Formula 5; and salts thereof: 
       
         
           
           
               
               
           
         
         
           
           
               
               
           
         
       
     
     
         6 . A hepatocyte nuclear factor 4 alpha (HNF4-α) antagonist comprising at least one type selected from the group consisting of at least one type of a compound selected from the group consisting of the following Formula 6 and Formulas 6-1 to 6-10, which are derivatives of Formula 6; and salts thereof: 
       
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
       
     
     
         7 . A hepatocyte nuclear factor 4 alpha (HNF4-α) antagonist comprising at least one type selected from the group consisting of at least one type of a compound selected from the group consisting of the following Formula 7 and Formulas 7-1 to 7-5, which are derivatives of Formula 7; and salts thereof: 
       
         
           
           
               
               
           
         
       
     
     
         8 . A hepatocyte nuclear factor 4 alpha (HNF4-α) antagonist comprising at least one type selected from the group consisting of at least one type of a compound selected from the group consisting of the following Formula 8 and Formula 8-1, which is a derivative of Formula 8; and salts thereof: 
       
         
           
           
               
               
           
         
       
     
     
         9 . A method for treating cancer comprising administering an effective amount of the HNF4-α antagonist of  claim 1  to a subject in need thereof. 
     
     
         10 . The method of  claim 9 , wherein the HNF4-α antagonist expresses wingless-type MMTV integration site family, member 5A (Wnt5a) by inhibiting the activity of HNF4-α. 
     
     
         11 . The method of  claim 9 , wherein the cancer is at least one type selected from the group consisting of gastric cancer, colorectal cancer, breast cancer, cervical cancer, and liver cancer. 
     
     
         12 . A method for treating cancer comprising administering an effective amount of the HNF4-α antagonist of  claim 2  to a subject in need thereof. 
     
     
         13 . The method of  claim 12 , wherein the HNF4-α antagonist expresses wingless-type MMTV integration site family, member 5A (Wnt5a) by inhibiting the activity of HNF4-α. 
     
     
         14 . The method of  claim 12 , wherein the cancer is at least one type selected from the group consisting of gastric cancer, colorectal cancer, breast cancer, cervical cancer, and liver cancer.