The present invention relates to a target-activated cell/tissue-penetrating peptide for delivery of impermeable compounds (Target Activated Cell/tissue Translocation peptide for Impermeable Compound Strategy (TACTICS)), and the use thereof, and more particularly to a target-activated cell/tissue-penetrating peptide, which comprises (a) a protein transduction domain (PTD), (b) a masking domain and (c) a spacer having a cleavage site specific for a target cell/tissue enzyme and is provided with target selectivity so as to penetrate specifically into a target tissue, and to a conjugate of the peptide with a drug or drug-containing particles for imaging or therapeutic applications. Because the target-activated cell/tissue-penetrating peptide has target selectivity, the peptide-drug conjugate exhibits maximized imaging and therapeutic effects, and the non-specific distribution of the conjugate in vivo is inhibited, so that the side effects of the conjugate are minimized, the diagnostic effects of the conjugate are maximized, and the conjugate is useful for the treatment of disease.
本发明涉及一种用于递送防渗化合物的靶向激活细胞/组织穿透肽(TACTICS)及其用途,特别是涉及一种靶向激活细胞/组织穿透肽、它包括(a)蛋白质转导结构域(
PTD)、(b)屏蔽结构域和(c)具有靶细胞/组织酶特异性裂解位点的间隔物,并具有靶选择性,可特异性地穿透到靶组织中,还包括该
多肽与药物或含药微粒的共轭物,用于成像或治疗应用。由于靶向激活的细胞/组织穿透肽具有靶向选择性,肽-药物共轭物显示出最大的成像和治疗效果,共轭物在体内的非特异性分布受到抑制,因此共轭物的副作用最小,共轭物的诊断效果最大,共轭物可用于治疗疾病。