State Key Laboratory of Pharmaceutical Biotechnology, Affiliated Drum Tower Hospital, Medical School of Nanjing University, School of Life Sciences, Nanjing University, Nanjing, 210023P. R. China.
Central Laboratory, Nanjing Integrated Traditional Chinese & Western Medicine Hospital Affiliated with Nanjing University of Chinese Medicine, Nanjing, 210014P. R. China.
Future Med Chem. 2024 Jul 2;16(13):1287-1298. doi: 10.1080/17568919.2024.2347072. Epub 2024 May 22.
Lysosomal pH changes are associated with drug resistance, cell growth and invasion of tumors, but effective and specific real-time monitoring of lysosomal pH compounds for cancer therapy is lacking. Here, based on the covalent linkage of the anticancer drug palbociclib and fluorescent dye fluorescein isothiocyanate (FITC), we designed and developed a novel palbociclib-derived multifunctional molecule (Pal-FITC) for lysosomal targeting and diagnostic therapeutic integration. Pal-FITC fluoresces is 20-fold stronger than that of FITC and shows a linear response in the pH range of 4.0-8.2 (R = 0.9901). Pal-FITC blocks cells in G1 phase via . Our study provides new strategies for tumor-targeted imaging and personalized therapy.
溶酶体 pH 值变化与肿瘤耐药性、细胞生长和侵袭有关，但缺乏有效的、针对溶酶体 pH 值化合物的实时监测用于癌症治疗。在这里，基于抗癌药物帕博西尼与荧光染料异硫氰酸荧光素（FITC）的共价连接，我们设计并开发了一种新型的帕博西尼衍生的多功能分子（Pal-FITC）用于溶酶体靶向和诊断治疗一体化。Pal-FITC 的荧光强度比 FITC 强 20 倍，在 pH 值为 4.0-8.2 的范围内呈线性响应（R=0.9901）。Pal-FITC 通过阻断细胞周期在 G1 期。我们的研究为肿瘤靶向成像和个性化治疗提供了新的策略。
