酪氨酸激酶抑制剂抗肿瘤活性评价方法研究进展

Advance of antitumor activity research in tyrosine kinase inhibitors

目的酪氨酸激酶的突变和过表达在肿瘤无限制生长、抗凋亡、侵袭和转移中具有重要作用。筛选和评估酪氨酸激酶抑制剂抗肿瘤活性已经成为靶向抗肿瘤药物研究的热点和关键点,多种评价酪氨酸激酶抑制剂抗肿瘤活性的方法在抗肿瘤药物研究中各有优势,自动化、规模化的高通量靶向酪氨酸激酶抑制剂抗肿瘤活性评价方法将可为恶性肿瘤的治疗筛选出大量候选化合物,而分子影像学的应用将有助于尽早提供大量更有效、经济和安全的肿瘤靶向治疗武器。

Mutations and overexpression of tyrosine kinase are critical in malignant tumor cell＇s survival, proliferation, invasion, and metastasis. Screening and research antitumor activity of tyrosine kinase inhibitors have been the key point in development of target antitumor drugs. Several methods of research antitumor activity of tyrosine kinase inhibitors have their own merits. Lots of candidate compounds will be screened by autonomous and large scale high through target research methods of antitumor activity of tyrosine kinase inhibitors. In addition, molecular imaging will lastly promote the appearance of more effective, economical and safe target arms for tumor treatment.