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.

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.

AIM: To investigate the effect of autophagy on cell ferroptosis in intestinal ischemia-reperfusion injury. METHODS: Twenty-four SPF grade Wistar rats weighing 200-220 g were divided into 4 groups (n = 6): sham operation group (sham group), ischemia group (I group), ischemia-reperfusion group (I/R group),and ischemia-reperfusion + autophagy inhibitor group (I/R + 3-MA group). The ischemia model was established by clamping the superior mesenteric artery for 1 hour, and the intestinal ischemia-reperfusion injury model was established by reperfusion for 2 hours. HE staining was used to observe the pathological changes of intestinal mucosa and Chiu score under light microscope. Fe

Objective: To discuss the postoperative analgesia efficacy of multimodal analgesia of ropivacaine combined with dezocine, and to illuminate the feasibility of multimodal analgesia in the children undergoing cheiloplasty.Methods:In the randomized, controlled and double blind study, sixty children scheduled for cheiloplasty were randomly divided into ropivacaine group,dezocine group and multimodal analgesia group (n=20). The children in ropivacaine group and multimodal analgesia group were treated with infraobital nerve blockade (1.5 mL 0.25% ropivacaine)before skin incision.The children in dezocine group received the same volume of normal saline. The patients in dezocine group and the multimodal analgesia group received dezocine (0.15 mg·kg-1 )20 min before the end of operation, and the children in ropivacaine group received the same volume of normal saline.The children’s ages and weights,duration of anesthesia and operation, reviving and extubation time,agitation score and incidence,laryngospasm or bronchospasm,CRIES scores at 2,4,6,8,12, and 24 h after operation and adverse reactions were all recorded.Results:There were no significant differences in the age,weight,the duration of anesthesia and operation of the children between three groups (P >0.05).Compared with ropivacaine group,the reviving and extubation time of the children in dezocine group and multimodal analgesia group were increased (P <0.05).There were no significant differences in the scores and the incidence of agitation between three groups (P >0.05).There were no laryngospasm or bronchospasm occured in all groups.The CRIES score at 2 h after operation of the children in multimodal analgesia group was the lowest and there were significant differences compared with other two groups (P <0.05).The CRIES score at 4 h after operation of dezocine group was increased compared with 2 h after operation and was higher than other two groups (P < 0.05).The CRIES score at 6 h after operation of the children in multimodal analgesia group was yet the lowest, and there were significant differences compared with other two groups (P <0.05).The CRIES score at 6 h after operation of the children in ropivacaine group was also increased,but there was no significant difference compared with dezocine group (P >0.05).There were no significant differences in the CRIES scores at 8,12,and 24 h after operation between three groups (P > 0.05).Compared with other two groups,the incidence of tachycardia and the cases using analgesic in multimodal analgesia group were the lowest,and there were significant differences compared with other two groups (P < 0.05 ).There was no respiratory inhibition in all groups.Conclusion:The multimodal analgesia of ropivacaine combined with dezocine can effectively prolong the postoperative analgesia duration and reduce adverse reactions, and it can be safely used in the postoperative analgesia in the children undergoing cheiloplasty.