KIM, Joong Kyu,김중규,PARK, Tae Kyo,박태교,WOO, Sung Ho,우성호,KIM, Hak-Sung,김학성,LEE, Joong-jae,이중재,JO, Seong-Min,조성민,RYOU, Jeong-Hyun,유정현,KIM, Tae Yoon,김태윤,PARK, Yun-Hee,박윤희,CHOI, Hyo Jung,최효정,JUNG, Ji Eun,정지
申请号：
KRKR2015/014423
公开号：
WO2016/108587A1
申请日:
2015.12.29
申请国别(地区):
WO
年份:
2016
代理人:
摘要：
The present invention relates to a drug conjugate using a repebody derivative, and a preparation method thereof and, more specifically, to a repebody derivative drug conjugate (RDC) in which a drug, a toxin, a ligand, and a substance having activity such as detection marking are conjugated to repebody, which exhibits substrate specificity by connecting a leucine-rich repeat (LRR) structure originated from a variable lymphocyte receptor (VLR) as a variable region on the N-terminus of an LRR family protein having an alpha helical capping motif, and a preparation method thereof. The RDC according to the present invention is a conjugate which is combined with a compound having high substrate specificity and excellent tissue and tumor penetration that repebody provides, and biological activity. As such, the RDC has the advantages of having superior efficacy compared to the case of using repebody alone, and having specific selectivity compared to the case of using the compound alone. Due to these features, the RDC is expected to be utilized in the treatment of tumors by combining, with repebody, which specifically binds to a protein overexpressed on cancer cells, a toxin that kills cells, to thereby selectively kill only the cancer cells.La présente invention concerne un conjugué de médicament utilisant un dérivé de repebody, et un procédé pour le préparer, et, plus spécifiquement, un conjugué de dérivé de repebody et de médicament (CRM) dans lequel un médicament, une toxine, un ligand, et une substance ayant une activité comme la détection de marquage sont conjugués à un repebody, qui présente une spécificité de substrat par connexion dune structure répétée riche en leucine (RRL) provenant dun récepteur variable de lymphocyte (RLV) comme une région variable sur lextrémité N-terminale dune protéine de la famille des RRL comprenant un motif de coiffage en hélice alpha, et un procédé pour le préparer. Le CRM selon la présente invention est un conjugué qui est combiné à un c
