1.Enhanced radiotheranostic targeting of integrin α5β1 with PEGylation-enabled peptide multidisplay platform (PEGibody): A strategy for prolonged tumor retention with fast blood clearance.
Siqi ZHANG ; Xiaohui MA ; Jiang WU ; Jieting SHEN ; Yuntao SHI ; Xingkai WANG ; Lin XIE ; Xiaona SUN ; Yuxuan WU ; Hao TIAN ; Xin GAO ; Xueyao CHEN ; Hongyi HUANG ; Lu CHEN ; Xuekai SONG ; Qichen HU ; Hailong ZHANG ; Feng WANG ; Zhao-Hui JIN ; Ming-Rong ZHANG ; Rui WANG ; Kuan HU
Acta Pharmaceutica Sinica B 2025;15(2):692-706
Peptide-based radiopharmaceuticals targeting integrin α5β1 show promise for precise tumor diagnosis and treatment. However, current peptide-based radioligands that target α5β1 demonstrate inadequate in vivo performance owing to limited tumor retention. The use of PEGylation to enhance the tumor retention of radiopharmaceuticals by prolonging blood circulation time poses a risk of increased blood toxicity. Therefore, a PEGylation strategy that boosts tumor retention while minimizing blood circulation time is urgently needed. Here, we developed a PEGylation-enabled peptide multidisplay platform (PEGibody) for PR_b, an α5β1 targeting peptide. PEGibody generation involved PEGylation and self-assembly. [64Cu]QM-2303 PEGibodies displayed spherical nanoparticles ranging from 100 to 200 nm in diameter. Compared with non-PEGylated radioligands, [64Cu]QM-2303 demonstrated enhanced tumor retention time due to increased binding affinity and stability. Importantly, the biodistribution analysis confirmed rapid clearance of [64Cu]QM-2303 from the bloodstream. Administration of a single dose of [177Lu]QM-2303 led to robust antitumor efficacy. Furthermore, [64Cu]/[177Lu]QM-2303 exhibited low hematological and organ toxicity in both healthy and tumor-bearing mice. Therefore, this study presents a PEGibody-based radiotheranostic approach that enhances tumor retention time and provides long-lasting antitumor effects without prolonging blood circulation lifetime. The PEGibody-based radiopharmaceutical [64Cu]/[177Lu]QM-2303 shows great potential for positron emission tomography imaging-guided targeted radionuclide therapy for α5β1-overexpressing tumors.
2.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.
3.Construction of nursing quality sensitive indicator system for ovarian neoplasms patients
Guofang KUANG ; Shihui LYU ; Peng YU ; Jieting YANG ; Jun LIU ; Xiaoli HUANG ; Shuai SUN ; Huimin GAO ; Xinzhi SHAN
Chinese Journal of Modern Nursing 2020;26(26):3634-3638
Objective:To construct a scientific and practical ovarian tumor nursing quality sensitive indicator system so as to provide a reference for evaluating the quality of nursing care for patients with ovarian tumors.Methods:Based on Donabedian's three-dimensional theoretical model of structure-process-outcome quality management, we used literature review and Delphi expert correspondence consultation to construct a nursing quality sensitive indicator system for ovarian tumor patients. From February to April 2019, we selected 20 experts from 16 ClassⅢ Grade A general hospitals and 2 higher nursing institutions from 7 provinces/municipalities in Shandong Province, Jiangsu Province, Beijing, Jilin Province, Shanghai, Guangdong Province and Sichuan Province for consultation.Results:Among two rounds of consultation, valid recovery rates were 90.00% and 94.44% respectively; authority coefficients were all 0.92; familiarity coefficients were 0.89 and 0.91 respectively; judgment coefficients were 0.94 and 0.92 respectively; Kendall harmony coefficients were 0.204 and 0.426 respectively; the differences were all statistically significant ( P<0.05) . The final nursing quality sensitive indicator system for ovarian tumor patients included 3 first-level indicators, 12 second-level indicators and 23 third-level indicators. Conclusions:The nursing quality sensitive indicator system for ovarian tumor patients is highly scientific and practical which can be used to standardize clinical nursing care for patients with ovarian tumors by gynecological nurses and improve the nursing quality.
4.Effect of different types of nutrient solution on preoperative fasting time
Weiji QIU ; Shitong LI ; Tianfang HUA ; Gang BAI ; Yu LU ; Jieting GAO ; Ning KONG
Chinese Journal of Clinical Nutrition 2015;23(2):73-76
Objective To discuss the feasibility of preoperative diet by measuring gastric emptying time of carbohydrate and protein nutrient solutions in healthy volunteers.Methods A total of 20 healthy volunteers were collected from August 2013 to May 2014.On the morning of the trial,baseline gastric residual volume of each volunteer was measured with magnetic resonance imaging at 8 a.m.,then each of the 20 healthy volunteers took 12.5% carbohydrate solution 400 ml (containing 40 g of maltodextrin and 10 g of sucrose) or 12.5% whey protein solution (containing 50 g whey protein) in 5 minutes.Magnetic resonance imaging was conducted to measure the gastric residual volume every 25 minutes.The volunteers were shifted to the other nutrient solution after a 1-week interval.The gastric emptying time of both nutrient solutions was calculated to generate the curves illustrating the process of gastric emptying.Results The baseline gastric residual volume of the volunteers was (14.90 ± 9.39) ml.The total gastric emptying time of carbohydrate solution was (104.90 ± 27.98) min (95 % CI 98.64-111.16 min),while that of whey protein solution was (199.6 ± 34.17) min (95% CI 184.47-214.73 min).There was a significant difference between these two types of nutrient solution in terms of gastric emptying time (P < 0.000 1).Conclusions The induction of anesthesia could be performed 2 hours after carbohydrate administration,and at least 4 hours after whey protein administration.

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