1.Fibroblast activation protein targeting radiopharmaceuticals: From drug design to clinical translation.
Yuxuan WU ; Xingkai WANG ; Xiaona SUN ; Xin GAO ; Siqi ZHANG ; Jieting SHEN ; Hao TIAN ; Xueyao CHEN ; Hongyi HUANG ; Shuo JIANG ; Boyang ZHANG ; Yingzi ZHANG ; Minzi LU ; Hailong ZHANG ; Zhicheng SUN ; Ruping LIU ; Hong ZHANG ; Ming-Rong ZHANG ; Kuan HU ; Rui WANG
Acta Pharmaceutica Sinica B 2025;15(9):4511-4542
The activation proteins released by fibroblasts in the tumor microenvironment regulate tumor growth, migration, and treatment response, thereby influencing tumor progression and therapeutic outcomes. Owing to the proliferation and metastasis of tumors, fibroblast activation protein (FAP) is typically highly expressed in the tumor stroma, whereas it is nearly absent in adult normal tissues and benign lesions, making it an attractive target for precision medicine. Radiolabeled agents targeting FAP have the potential for targeted cancer diagnosis and therapy. This comprehensive review aims to describe the evolution of FAPI-based radiopharmaceuticals and their structural optimization. Within its scope, this review summarizes the advances in the use of radiolabeled small molecule inhibitors for tumor imaging and therapy as well as the modification strategies for FAPIs, combined with insights from structure-activity relationships and clinical studies, providing a valuable perspective for radiopharmaceutical clinical development and application.
2.Effect of mannitol combined with psychological intervention on post-operative swelling of extremities fractures
Chinese Journal of Biochemical Pharmaceutics 2017;37(6):33-34,37
Objective To observe the influence mannitol combined with psychological intervention on post-operative swelling of extremities fractures.Methods96 patients from January 2013 to March 2015, were randomly divided into observation group and control group of 48 cases.In the control group were treated with mannitol treatment, observation group were treated with mannitol combined with psychological intervention, the two groups were recorded cases of fracture after swelling sweling.Results①After treatment, patients swelling time was (7.02+1.02) d, than the control group (9.87±1.23) d, and the difference was statistically significant (P<0.05).②The observation group were 6 days and 9 days after treatment forearm limb circumference, respectively (25.76±1.06) cm, (23.15±0.76) cm, were lower than in the control group (27.12±1.10) cm, (24.20±0.79) cm, and the difference was significant sex (P<0.05).The observation group were 6 days and 9 days after treatment were leg limb circumference (35.18±0.74) cm, (32.04±0.31) cm, were lower than in the control group (36.76±0.78) cm, (33.17±0.37) cm, and the difference was significant sex (P<0.05).③ Observation group patients after the treatment of anxiety and depression were on average lower than the control group, and the difference was statistically significant (P<0.05).ConclusionMannitol combined with psychological intervention effect fracture surgery swelling of extremities significant, can significantly reduce the postoperative pain is worthy of further research and application.
3.Interaction between methylenetetrahydrofolate reductase C677T gene polymorphism and sleep duration on risk of stroke pathogenesis
Yan ZHANG ; Ruping XIE ; Yang SHEN ; Dongsheng FAN
Journal of Peking University(Health Sciences) 2008;40(3):262-269
Objective: To investigate the interaction between methylenetetrahydrofolate reductase (MTHFR) C677T polymorphism and sleeping duration on risk of stroke in a Chinese Han ethnic population. Methods: In the case-control study and epidemiological investigation, the self-reported sleep duration and MTHFR C677T polymorphism of 245 patients with cerebral infarction, 222 patients with cerebral hemorrhage and 282 controls were collected. Multiple logistic regression was performed to analyze the interaction between MTHFR C677T polymorphism and sleeping duration on risk of stroke. Results: After adjustment for major confounding variables, multiple logistic regression analysis showed that: (1) There was significant association between long sleep duration (>8 hours of sleep per night) and cerebral infarction (OR=3.90; 95% CI:2.43-6.26), but not for cerebral hemorrhage (OR=1.16, 95% CI: 0.71-1.92). On the other hand, insomnia (sleep duration less than 6 hours) was neither associated with cerebral infarction nor hemorrhage. (2) MTHFR TT genotype increased the risk of cerebral infarction significantly (OR=2.01; 95% CI:1.12-3.61), but not for cerebral hemorrhage (OR=1.16,95% CI:0.71-1.92). (3) There was a significant synergistic effect of interaction between MTHFR TT677 genotype and long sleep duration on risk of cerebral infarction (OR=6.22; 95% CI:2.44-15.83). Conclusion: MTHFR TT677 genotype and long sleep duration increase the risk of cerebral infarction independent of confounding factors, respectively. Furthermore, there is a significant synergistic effect between MTHFR TT677 genotype and long sleep duration on risk of cerebral infarction in the Chinese Han ethnic population.

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