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1.发明公开NEUROPILIN-1 SPECIFIC BINDING PEPTIDE, FUSION PROTEIN FUSED WITH SAME, AND USE THEREOF 审中-公开神经纤维蛋白溶解蛋白-1特异性结合肽，与其融合的融合蛋白及其用途
公开(公告)号：EP3275895A1
公开(公告)日：2018-01-31
申请号：EP16769094.0
申请日：2016-03-23
发明人： KIM, Yong Sung , KIM, Ye Jin
IPC分类号： C07K14/705 , C07K19/00 , A61K9/127 , A61K47/48 , G01N33/53
CPC分类号： C07K14/705 , A61K9/127 , A61K38/00 , A61K47/50 , C07K19/00 , C07K2317/52 , C07K2317/522 , C07K2317/524 , C07K2317/526 , C07K2317/55 , C07K2317/56 , C07K2317/622 , C07K2319/30 , G01N33/53 , G01N33/57492 , G01N33/6845 , G01N33/6872 , G01N33/6893 , G01N2333/70596 , G01N2800/7014
摘要： The present invention relates to a peptide specifically binding only to neuropilin1 (NRP1), not binding to neuropilin2 (NRP2); a fusion protein, a small molecule drug, a nanoparticle, or a liposome fused with the peptide; and a pharmaceutical composition comprising the same for treating or preventing cancer or angiogenesis-related diseases and a composition comprising the same for diagnosing cancer or angiogenesis-related diseases. In addition, the present invention provides a polynucleotide for coding the peptide specifically binding to NRP1. Further, the present invention relates to a method for screening the peptide specifically binding to NRP1. An antibody heavy chain constant region fused with the peptide specifically binding to NRP1 according to the present invention has a characteristic of specifically binding to NRP1, and thus when being administered in vivo, selectively accumulates on tumor tissue, widens intercellular gaps between tumor vascular endothelial cells, promotes extravasation, and increases infiltration into tumor tissue. In addition, the antibody heavy chain constant region fused with the peptide specifically binding to NRP1 according to the present invention inhibits a vascular endothelial growth factor (VEGF) from binding to neurophilin1 and thereby has an ability of inhibiting angiogenesis in the tumor tissue. Therefore, the antibody heavy chain constant region fused with the peptide according to the present invention shows in vivo tumor-inhibiting activity.
摘要翻译： 本发明涉及仅与神经毡蛋白1（NRP1）特异性结合而不与神经毡蛋白2（NRP2）结合的肽; 融合蛋白，小分子药物，纳米颗粒或与肽融合的脂质体; 以及包含其的用于治疗或预防癌症或血管发生相关疾病的药物组合物以及包含其的用于诊断癌症或血管发生相关疾病的组合物。 另外，本发明提供了用于编码与NRP1特异性结合的肽的多核苷酸。 此外，本发明涉及用于筛选与NRP1特异性结合的肽的方法。 与根据本发明与NRP1特异性结合的肽融合的抗体重链恒定区具有与NRP1特异性结合的特征，因此当体内施用时，选择性地积聚在肿瘤组织上，扩大肿瘤血管内皮细胞之间的细胞间隙 ，促进外渗，并增加肿瘤组织的浸润。 此外，根据本发明与特异性结合NRP1的肽融合的抗体重链恒定区抑制血管内皮生长因子（VEGF）与神经炎蛋白1的结合，从而具有抑制肿瘤组织中血管生成的能力。 因此，与根据本发明的肽融合的抗体重链恒定区显示体内肿瘤抑制活性。
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2.发明公开
公开(公告)号：EP3511340A1
公开(公告)日：2019-07-17
申请号：EP17839824.4
申请日：2017-08-10
发明人： KIM, Yong Sung , JUNG, Keunok , HA, Ji Hee , KIM, Ye Jin , CHOI, Dong Ki , CHOI, Hye Ji
摘要： The present invention relates to a heterodimeric Fc-fused protein comprising a first Fc region and a second Fc region of an immunoglobulin Fc pair and a physiologically active protein composed of two or more different subunits, wherein one or more subunits of the physiologically active protein are linked separately to one or more ends of the N-terminus or C-terminus of the first Fc region and/or the second Fc region, and CH3 domains of the first Fc region and the second Fc region are mutated so as to promote the heterodimeric Fc formation. Moreover, the present invention relates to a pharmaceutical composition comprising the heterodimeric Fc-fused protein. The heterodimeric Fc-fused protein according to the present invention has an advantage in that it can retain the activity of a naturally occurring physiologically active protein whose two or more different subunits exhibit physiological activity by forming a protein complex, because the physiologically active protein can be linked to an immunoglobulin heterodimeric Fc such that the naturally occurring form and structure of the fused protein thereof can be maintained. When the heterodimeric Fc-fused protein according to the present invention is used, there is an advantage in that the in vivo half-life of the physiologically active protein contained in the heterodimeric Fc-fused protein can be significantly increased due to the Fc-mediated long half-life such that various physiological activities thereof in vivo can be long-lasting.
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3.发明公开
公开(公告)号：EP3680250A1
公开(公告)日：2020-07-15
申请号：EP18854495.1
申请日：2018-09-07
发明人： KIM, Yong Sung , KIM, Ye Jin , JUNG, Keunok , KIM, Jeong-Ah
摘要： The present invention relates to a composition for inhibiting regulatory T cell immunosuppression, containing a fusion protein comprising a peptide that binds specifically to neuropilin 1 (NRP1). The fusion protein comprising the peptide that binds specifically to neuropilin 1 according to the present invention can reduce the proportion of regulatory T cells among CD4+ T cells in tumor tissue and inhibit the activity of regulatory T cells that infiltrated into tumor tissue, thereby down-regulating immunosuppression in the tumor tissue without causing systemic toxicity. Thus, the fusion protein can exhibit a high effect on tumor treatment.
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公开(公告)号：EP3508495A1
公开(公告)日：2019-07-10
申请号：EP17847030.8
申请日：2017-08-31
申请人： Korea University Research and Business Foundation , Ajou University Industry-Academic Cooperation Foundation
发明人： LEE, Kyung-Mi , LIM, Seon Ah , KIM, Yong Sung , KIM, Ye Jin
摘要： A heterodimeric Fc-fused protein and a pharmaceutical composition comprising the heterodimeric Fc-fused protein are disclosed. The heterodimeric Fc-fused protein comprises first and second Fc regions of an immunoglobulin heavy chain constant region (Fc) pair and in which IL-21 is bound to at least one of the N-terminus or the C-terminus of the first Fc region and/or the second Fc region, wherein CH3 domains of the first Fc region and the second Fc region are mutated such that the formation of a heterodimer is promoted.
When the heterodimeric Fc-fused protein according to the present invention is used, an in vivo half-life of IL-21 included in the heterodimeric Fc-fused protein may be significantly increased.
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