上海医药
上海醫藥
상해의약
SHANGHAI MEDICAL & PHARMACEUTICAL JOURNAL
2015年
1期
69-74
,共6页
受体%多肽载体%肿瘤%靶向治疗%丙戊酸
受體%多肽載體%腫瘤%靶嚮治療%丙戊痠
수체%다태재체%종류%파향치료%병무산
receptor-targeted%peptide-drug conjugate%tumor%VPA
常规化疗药物对癌细胞没有选择性,常常会导致严重的副作用。提高这些药物的靶向特异性已成为药物开发的热点方向之一。一些小分子多肽能够靶向作用于特定的受体,因而被用作癌症化疗药物的载体。化疗药物与多肽载体偶联构成新的多肽载体抗肿瘤药物。这些药物具有高特异性、高亲和力和肿瘤渗透力等优点,能够通过细胞表面的特定受体将药物送到靶向癌细胞内,提高抗癌效果、减少副作用和癌细胞的耐药性。多肽载体靶向药物被誉为新一代的靶向特异性的抗肿瘤药物之一。
常規化療藥物對癌細胞沒有選擇性,常常會導緻嚴重的副作用。提高這些藥物的靶嚮特異性已成為藥物開髮的熱點方嚮之一。一些小分子多肽能夠靶嚮作用于特定的受體,因而被用作癌癥化療藥物的載體。化療藥物與多肽載體偶聯構成新的多肽載體抗腫瘤藥物。這些藥物具有高特異性、高親和力和腫瘤滲透力等優點,能夠通過細胞錶麵的特定受體將藥物送到靶嚮癌細胞內,提高抗癌效果、減少副作用和癌細胞的耐藥性。多肽載體靶嚮藥物被譽為新一代的靶嚮特異性的抗腫瘤藥物之一。
상규화료약물대암세포몰유선택성,상상회도치엄중적부작용。제고저사약물적파향특이성이성위약물개발적열점방향지일。일사소분자다태능구파향작용우특정적수체,인이피용작암증화료약물적재체。화료약물여다태재체우련구성신적다태재체항종류약물。저사약물구유고특이성、고친화력화종류삼투력등우점,능구통과세포표면적특정수체장약물송도파향암세포내,제고항암효과、감소부작용화암세포적내약성。다태재체파향약물피예위신일대적파향특이성적항종류약물지일。
Conventional cancer chemotherapy has very limited effects due to lacking speciifcity resulting in severe toxic side effects. Certain G protein-coupled receptors (GPCRs) are highly expressed in many tumor cells and tumoral blood veins, with their cognate ligands being peptides. Therefore, these peptides, especially their long-acting analogs, can be applied as drug-delivery vehicles by coupling with cytotoxic agents. These novel cytotoxic peptide-drug conjugates display more potent anti-tumor efifcacy by targeting the cognate receptors while reducing toxic side effects and overcoming multiple drug resistance. This new receptor-targeted approach may provide a promising opportunity for the improvement of cancer treatments.