The invention belongs to the field of genetic engineering and biotechnology, and specifically discloses a design, preparation and pharmic application of a tumor-targeted TNF-related apoptosis-inducing ligand's variant. The tumor-targeted TNF-related apoptosis-inducing ligand's variant is generated by a fused protein which is consisted of the ligand of CD13, the connecting peptide and TNF-related apoptosis-inducing ligand's variant, and which is by the construction of coding gene of the variant according to the technology of genetic engineering and clone, soluble recombinant expression and ordinary separation and purification. The variant, produced by the method of preparation of the tumor-targeted TNF-related apoptosis-inducing ligand's variant, has favorable tumor-targeting characteristics and the significant enhancement of the anti-tumor effect. It is possible to reducing the required dosage of protein to the treatment effect, increasing the bioavailability, reducing the cost of treatment and overcome the potential toxic effects of the TNF-realated apoptosis-inducing ligand. Moreover, the preparation method of the tumor targeted TNF-related apoptosis-inducing ligand's variant of the present invention provides a method for producing the variant of soluble expression and high concern of polymer forms and a process of separation and purification thereof.本発明は、腫瘍ターゲティング腫瘍壊死因子関連アポトーシス誘導リガンド変異体の設計、調製方法及びその薬学的な応用を開示する。前記腫瘍ターゲティング腫瘍壊死因子関連アポトーシス誘導リガンド変異体は、ＣＤ１３のリガンドと、ジョイニングペプチドと、腫瘍壊死因子関連アポトーシス誘導リガンドと、によって融合蛋白質を形成し、前記変異体のコード遺伝子をクローン構築、可溶性型に組み換え・発現し、容易に分離・精製することで生産する。前記アポトーシス誘導リガンド変異体は、優れた腫瘍組織ターターゲティング能及び抗腫瘍増殖効果を有するので、治療投与量を下げ、生物学的利用能を向上させ、治療コストを削減し、さらに潜在的な毒性副作用を克服することができる。同時に、前記アポトーシス誘導リガンド変異体の生産方法は、可溶性型であり、重合体型高含有率で生産する発現方法と容易な分離精製プロセスを提供する。【選択図】 図８
