1.Research progress on self-advocacy of cancer patients
Lanhui TAN ; Liping YU ; Huidan YU ; Ling FU
Chinese Journal of Modern Nursing 2022;28(32):4573-4576
This article reviews the concept, assessment tools, associated factors and intervention practice of cancer patients' self-advocacy. And this article puts forward the suggestion that current research should expand the research population, actively develop and refine self-advocacy scales, and gradually carry out cross-sectional, longitudinal and interventional research, so as to improve the awareness and attention of medical and nursing staff and provide a reference for improving patient-centered cancer care quality and cancer patients' quality of life.
2.Design, synthesis, and biological evaluation of quinazolin-4(3H)-one derivatives co-targeting poly(ADP-ribose) polymerase-1 and bromodomain containing protein 4 for breast cancer therapy
Xiaosa CHANG ; Dejuan SUN ; Danfeng SHI ; Guan WANG ; Yanmei CHEN ; Kai ZHANG ; Huidan TAN ; Jie LIU ; Bo LIU ; Liang OUYANG
Acta Pharmaceutica Sinica B 2021;11(1):156-180
This study was aimed to design the first dual-target small-molecule inhibitor co-targeting poly (ADP-ribose) polymerase-1 (PARP1) and bromodomain containing protein 4 (BRD4), which had important cross relation in the global network of breast cancer, reflecting the synthetic lethal effect. A series of new BRD4 and PARP1 dual-target inhibitors were discovered and synthesized by fragment-based combinatorial screening and activity assays that together led to the chemical optimization. Among these compounds, 19d was selected and exhibited micromole enzymatic potencies against BRD4 and PARP1, respectively. Compound 19d was further shown to efficiently modulate the expression of BRD4 and PARP1. Subsequently, compound 19d was found to induce breast cancer cell apoptosis and stimulate cell cycle arrest at G1 phase. Following pharmacokinetic studies, compound 19d showed its antitumor activity in breast cancer susceptibility gene 1/2 (BRCA1/2) wild-type MDA-MB-468 and MCF-7 xenograft models without apparent toxicity and loss of body weight. These results together demonstrated that a highly potent dual-targeted inhibitor was successfully synthesized and indicated that co-targeting of BRD4 and PARP1 based on the concept of synthetic lethality would be a promising therapeutic strategy for breast cancer.