HNF4-Α ANTAGONIST AND USE THEREOF

• Main Authors: KIM, YON HUI, NAM, SEUNG YOON, PARK, HEE SEO, CHANG, HAE RYUNG, JUNG, HAE RIM
• Format: Patent
• Language: English; French; Korean
• Published: 14.07.2016
• Subjects: HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The present invention relates to a Hepatocyte nuclear factor 4 alpha (HNF4-α) antagonist and a use thereof. It was found that the HNF4-α antagonist selected in the present invention specifically binds to a ligand binding domain of HNF4-α to inhibit the activity of HNF4-α. The HNF4-α antagonist of the present invention can not only be used as a pharmaceutical composition for preventing and treating cancers, or as a health functional food, but can also be applied to a composition for treating and preventing diseases caused by overexpression of HNF4-α since the HNF4-α antagonist of the present invention remarkably and specifically reduces expression of Wnt5a compared to known HNF4-α antagonists, and can inhibit the growth of stomach cancer cells. La présente invention concerne un antagoniste du facteur nucléaire hépatocytaire 4 alpha (HNF4-α) et une utilisation associée. Il a été découvert que l'antagoniste du HNF4-α sélectionné dans la présente invention se lie spécifiquement à un domaine de liaison du ligand de HNF4-α pour inhiber l'activité de HNF4-α. L'antagoniste de HNF4-α de la présente invention peut non seulement être utilisé en tant que composition pharmaceutique pour la prévention et le traitement de cancers, ou sous la forme d'un aliment fonctionnel de santé, mais aussi être appliqué à une composition pour le traitement et la prévention de maladies provoquées par la surexpression de HNF4-α étant donné que l'antagoniste de HNF4-α de la présente invention réduit de façon remarquable et spécifique l'expression de Wnt5a comparé aux antagonistes de HNF4-α connus, et peut inhiber la croissance de cellules du cancer de l'estomac. 본 발명은 HNF4-α(Hepatocyte nuclear factor 4 alpha) 길항제 및 이의 용도에 관한 것으로, 본 발명의 HNF4-α(Hepatocyte nuclear factor 4 alpha) 길항제 및 이의 용도에 관한 것으로, 본 발명에서 선별한 HNF4-α 길항제는 HNF4-α의 리간드 바인딩 도메인에 특이적으로 결합하여 HNF4-α의 활성을 억제시키는 것을 확인하였으며, 본 발명의 HNF4-α 길항제는 기존에 알려진 HNF4-α 길항제에 비해 현저하게 Wnt5a의 발현을 특이적으로 감소시키고, 위암세포의 성장을 억제할 수 있으므로, 암 예방 및 치료용 약학적 조성물 또는 건강기능식품으로 활용될 수 있을 뿐만 아니라, HNF4-α 과발현으로 인해 발생하는 질환의 치료 또는 예방용 조성물로 응용할 수 있다.