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.druglikeFilter 1.0: An AI powered filter for collectively measuring the drug-likeness of compounds.
Minjie MOU ; Yintao ZHANG ; Yuntao QIAN ; Zhimeng ZHOU ; Yang LIAO ; Tianle NIU ; Wei HU ; Yuanhao CHEN ; Ruoyu JIANG ; Hongping ZHAO ; Haibin DAI ; Yang ZHANG ; Tingting FU
Journal of Pharmaceutical Analysis 2025;15(6):101298-101298
Advancements in artificial intelligence (AI) and emerging technologies are rapidly expanding the exploration of chemical space, facilitating innovative drug discovery. However, the transformation of novel compounds into safe and effective drugs remains a lengthy, high-risk, and costly process. Comprehensive early-stage evaluation is essential for reducing costs and improving the success rate of drug development. Despite this need, no comprehensive tool currently supports systematic evaluation and efficient screening. Here, we present druglikeFilter, a deep learning-based framework designed to assess drug-likeness across four critical dimensions: 1) physicochemical rule evaluated by systematic determination, 2) toxicity alert investigated from multiple perspectives, 3) binding affinity measured by dual-path analysis, and 4) compound synthesizability assessed by retro-route prediction. By enabling automated, multidimensional filtering of compound libraries, druglikeFilter not only streamlines the drug development process but also plays a crucial role in advancing research efforts towards viable drug candidates, which can be freely accessed at https://idrblab.org/drugfilter/.
3.Risk factors of silicon oil dependent after pars plana vitrectomy in open globe injuries: Eye Injury Vitrectomy Study
Wan LU ; Kang FENG ; Qihua WANG ; Bingjie WANG ; Tong SUN ; Zhizhong MA ; Yuntao HU
Chinese Journal of Ocular Fundus Diseases 2025;41(4):277-281
Objective:To observe and preliminarily analyze the risk factors related to silicone oil dependence after pars plana vitrectomy (PPV) in open globe injuries (OGI) .Methods:A retrospective clinical study. This study included 211 patients with OGI who received PPV treatment from January 1, 2005 to December 31, 2016 in Eye Injury Vitrectomy Study database. Silicone oil dependence was defined as the intraocular pressure <10 mm Hg (1 mm Hg= 0.133 kPa) in silicone oil tamponade eye 6 months after PPV. The patient's age, intraocular pressure, type of injury, length of eyeball wound, as well as the presence of ciliary body injury, choroidal injury, and retinal resection and/or defect area were recorded in detail. Logistic multifactorial regression analyzed the correlation between age, eye wound length and ciliary body iinjury, choroidal injury and retinal resection and/or defect severity and silicone oil dependence.Results:211 OGI eyes underwent vitrectomy were included, the mean age of the study population was 32.93 years (range 1-73 years), and the median follow-up period was 20.06 months (range 5.85-90.58 months). Among the 211 eyes, 121 (57.3%, 121/211), 52 (24.6%, 52/211), 23 (10.9%, 23/211) and 15 (7.1%, 15/211) were rupture, perforation, intraocular foreign bodies and penetrating injury, respectively. 98 eyes (46.4%, 98/211) of silicone oil dependence in total, among them, 64 (65.3%, 64/98), 19 (19.4%, 19/98), 9 (9.2%, 9/98) and 6 (6.1%, 6/98) eyes were rupture, perforation, intraocular foreign body and penetrating injury, respectively. Correlation analysis revealed that silicone oil dependence was significantly associated with ciliary body injury [odds ratio ( OR) = 2.150, 95% confidence interval ( CI) 1.052-4.393], choroidal injury ( OR=3.233, 95% CI 1.454-7.191), and retinal injury ( OR=2.731, 95% CI 1.393-5.353). No correlation was found with age ( OR= 0.981, 95% CI 0.960-1.002) or ocular wound length ( OR=1.716, 95% CI 0.987-2.984) ( P> 0.05). Conclusion:Silicone oil dependency following PPV in OGIs are associated with ciliary body, choroidal, and retinal injuries, but no association with age or length of the ocular wound.
4.druglikeFilter 1.0:An AI powered filter for collectively measuring the drug-likeness of compounds
Minjie MOU ; Yintao ZHANG ; Yuntao QIAN ; Zhimeng ZHOU ; Yang LIAO ; Tianle NIU ; Wei HU ; Yuanhao CHEN ; Ruoyu JIANG ; Hongping ZHAO ; Haibin DAI ; Yang ZHANG ; Tingting FU
Journal of Pharmaceutical Analysis 2025;15(6):1370-1377
Advancements in artificial intelligence(AI)and emerging technologies are rapidly expanding the exploration of chemical space,facilitating innovative drug discovery.However,the transformation of novel compounds into safe and effective drugs remains a lengthy,high-risk,and costly process.Comprehensive early-stage evaluation is essential for reducing costs and improving the success rate of drug development.Despite this need,no comprehensive tool currently supports systematic evaluation and efficient screening.Here,we present druglikeFilter,a deep learning-based framework designed to assess drug-likeness across four critical dimensions:1)physicochemical rule evaluated by systematic determination,2)toxicity alert investigated from multiple perspectives,3)binding affinity measured by dual-path analysis,and 4)compound synthesizability assessed by retro-route prediction.By enabling automated,multidimensional filtering of compound libraries,druglikeFilter not only streamlines the drug development process but also plays a crucial role in advancing research efforts towards viable drug candidates,which can be freely accessed at https://idrblab.org/drugfilter/.
5.Clinicopathological Characteristics of HER2-Positive Breast Cancer Patients with BRCA1/2 Pathogenic Variants and Their Response to Neoadjuvant Targeted Therapy
Xingyu LIAO ; Huimin LIU ; Jie SUN ; Li HU ; Juan ZHANG ; Lu YAO ; Ye XU ; Yuntao XIE
Cancer Research on Prevention and Treatment 2025;52(6):491-495
Objective To analyze the proportion and clinicopathological characteristics of HER2-positive breast cancer patients with BRCA1/2 pathogenic variants, and their response to neoadjuvant anti-HER2 targeted therapy. Methods The clinicopathological data of 531 breast cancer patients with germline BRCA1/2 pathogenic variants (201 with BRCA1 variants and 330 with BRCA2 variants) were analyzed. Results Among the 201 BRCA1 and 330 BRCA2 variants, 17 (8.5%) and 42 (12.7%) HER2-positive breast cancer cases were identified, respectively, accounting for 11.1% of all BRCA1/2-mutated breast cancers. Compared with BRCA1/2-mutated HR-positive/HER2-negative patients, HER2-positive patients did not present any significant differences in clinicopathological features; however, compared with triple-negative breast cancer patients, HER2-positive patients had a later onset age and lower tumor grade. Among the 17 patients who received neoadjuvant anti-HER2 targeted therapy, 10 cases achieved pCR (58.8%), whereas 7 cases did not (41.2%). Conclusion HER2-positive breast cancer accounts for more than 10% of BRCA1/2-mutated patients. Approximately 40% of these patients fail to achieve pCR after neoadjuvant targeted therapy. This phenomenon highlights the possibility of combining anti-HER2 targeted agents with poly (adenosine diphosphate-ribose) polymerase inhibitors.
6.Impact of 5G remote robotic cholecystectomy on postoperative rehabilitation and quality of life in patients with gallstones
Yuqi MA ; Ming HU ; Yuan DENG ; Jing YANG ; Jin GUO ; Zeping ZHANG ; Wutang JING ; Weipeng ZHAN ; Hui CAI ; Yuntao MA
Chinese Journal of General Surgery 2025;40(7):528-532
Objective:To evaluate the effect of 5th generation mobile communication technology(5G) remote robot-assisted cholecystectomy on postoperative recovery and quality of life in patients with gallstones.Methods:Clinical data of patients who underwent 5G remote robotic cholecystectomy(20 cases) vs traditional robotic cholecystectomy(20 cases) at Gansu Provincial People's Hospital from May to September 2023 were retrospectively analyzed. Intraoperative and postoperative related indexes were compared between the two groups, and changes in pain analog scores before, 12 hours, and 24 hours after surgery, and global quality of life (GIQLI) scores before and 3 months after surgery were evaluated.Results:There was no significant difference between the two groups in terms of intraoperative and postoperative conditions (intraoperative blood loss, operative time, time to exhaustion, and length of hospital stay). Patients' pain analog scores at 12 and 24 hours postoperatively were lower than preoperatively, but the differences were not statistically significant( P>0.05). In addition, there was no significant difference in recovery indicators between the two groups compared to the control group ( P>0.05). Conclusion:The postoperative recovery metrics of 5G tele-robotic-assisted cholecystectomy were consistent with the results of conventional robotic surgery.
7.Risk factors of silicon oil dependent after pars plana vitrectomy in open globe injuries: Eye Injury Vitrectomy Study
Wan LU ; Kang FENG ; Qihua WANG ; Bingjie WANG ; Tong SUN ; Zhizhong MA ; Yuntao HU
Chinese Journal of Ocular Fundus Diseases 2025;41(4):277-281
Objective:To observe and preliminarily analyze the risk factors related to silicone oil dependence after pars plana vitrectomy (PPV) in open globe injuries (OGI) .Methods:A retrospective clinical study. This study included 211 patients with OGI who received PPV treatment from January 1, 2005 to December 31, 2016 in Eye Injury Vitrectomy Study database. Silicone oil dependence was defined as the intraocular pressure <10 mm Hg (1 mm Hg= 0.133 kPa) in silicone oil tamponade eye 6 months after PPV. The patient's age, intraocular pressure, type of injury, length of eyeball wound, as well as the presence of ciliary body injury, choroidal injury, and retinal resection and/or defect area were recorded in detail. Logistic multifactorial regression analyzed the correlation between age, eye wound length and ciliary body iinjury, choroidal injury and retinal resection and/or defect severity and silicone oil dependence.Results:211 OGI eyes underwent vitrectomy were included, the mean age of the study population was 32.93 years (range 1-73 years), and the median follow-up period was 20.06 months (range 5.85-90.58 months). Among the 211 eyes, 121 (57.3%, 121/211), 52 (24.6%, 52/211), 23 (10.9%, 23/211) and 15 (7.1%, 15/211) were rupture, perforation, intraocular foreign bodies and penetrating injury, respectively. 98 eyes (46.4%, 98/211) of silicone oil dependence in total, among them, 64 (65.3%, 64/98), 19 (19.4%, 19/98), 9 (9.2%, 9/98) and 6 (6.1%, 6/98) eyes were rupture, perforation, intraocular foreign body and penetrating injury, respectively. Correlation analysis revealed that silicone oil dependence was significantly associated with ciliary body injury [odds ratio ( OR) = 2.150, 95% confidence interval ( CI) 1.052-4.393], choroidal injury ( OR=3.233, 95% CI 1.454-7.191), and retinal injury ( OR=2.731, 95% CI 1.393-5.353). No correlation was found with age ( OR= 0.981, 95% CI 0.960-1.002) or ocular wound length ( OR=1.716, 95% CI 0.987-2.984) ( P> 0.05). Conclusion:Silicone oil dependency following PPV in OGIs are associated with ciliary body, choroidal, and retinal injuries, but no association with age or length of the ocular wound.
8.Impact of 5G remote robotic cholecystectomy on postoperative rehabilitation and quality of life in patients with gallstones
Yuqi MA ; Ming HU ; Yuan DENG ; Jing YANG ; Jin GUO ; Zeping ZHANG ; Wutang JING ; Weipeng ZHAN ; Hui CAI ; Yuntao MA
Chinese Journal of General Surgery 2025;40(7):528-532
Objective:To evaluate the effect of 5th generation mobile communication technology(5G) remote robot-assisted cholecystectomy on postoperative recovery and quality of life in patients with gallstones.Methods:Clinical data of patients who underwent 5G remote robotic cholecystectomy(20 cases) vs traditional robotic cholecystectomy(20 cases) at Gansu Provincial People's Hospital from May to September 2023 were retrospectively analyzed. Intraoperative and postoperative related indexes were compared between the two groups, and changes in pain analog scores before, 12 hours, and 24 hours after surgery, and global quality of life (GIQLI) scores before and 3 months after surgery were evaluated.Results:There was no significant difference between the two groups in terms of intraoperative and postoperative conditions (intraoperative blood loss, operative time, time to exhaustion, and length of hospital stay). Patients' pain analog scores at 12 and 24 hours postoperatively were lower than preoperatively, but the differences were not statistically significant( P>0.05). In addition, there was no significant difference in recovery indicators between the two groups compared to the control group ( P>0.05). Conclusion:The postoperative recovery metrics of 5G tele-robotic-assisted cholecystectomy were consistent with the results of conventional robotic surgery.
9.Robotic-assisted"3+1"Surgical Mode Strategy for 6 Cases of Median Arcuate Ligament Syndrome
Yuqi MA ; Yuntao MA ; Diaolong MA ; Qian YANG ; Weipeng ZHAI ; Hui CAI ; Ming HU
Chinese Journal of Minimally Invasive Surgery 2024;24(10):678-682
Objective To investigate the feasibility of robotic-assisted"3+1"surgical mode strategy for the treatment of median arcuate ligament syndrome(MALS).Methods Six patients diagnosed as MALS were enrolled between June 2019 and October 2023.The utilization of robotic-assisted"3+1"surgical mode(a 4-hole operation with 3 robot arms and 1 assistance hole)was carried out.Through a posterior splenic artery approach,the compression of the midline arcuate ligament on the abdominal trunk was relieved,which was an abdominal trunk vascularization.Results All the 6 patients underwent robotic-assisted"3+1"surgical mode successfully.The surgical duration(including the time for connecting and disconnecting the machine)was 38-52 min,with a mean of 43.2 min.The intraoperative bleeding volume was 5-25 ml,with a mean of 15 ml.The postoperative hospital stay was 6-9 d,with a mean of 7.5 d.All the 6 patients were followed up for 1-45 months after surgery(median,2.5 months).One patient remained unchanged in body weight,while 5 patients gained 1.0-2.0 kg in body weight,with a mean of 1.5 kg.The symptom of postprandial epigastric pain completely resolved in 5 patients,while the symptom was reduced but not completely alleviated in one patient.Conclusion Treatment of MALS with the robotic-assisted"3+1"surgical model involving abdominal trunk vascularization through a posterior splenic artery approach is safe and feasible.
10.An exploratory study of the domestic robotic surgical system for general surgery
Jing YANG ; Zeping ZHANG ; Guoyuan YANG ; Yiyun PENG ; Meijuan SONG ; Weipeng ZHAN ; Hongwei TIAN ; Ming HU ; Changfeng MIAO ; Dongdong CHEN ; Wei FANG ; Wutang JING ; Yuntao MA
Chinese Journal of General Surgery 2024;39(9):698-702
Objective:To evaluate the safety and efficacy of the domestic robotic surgical system for general surgery.Methods:A prospective single-center, single-arm exploratory study was conducted at Gansu Provincial People's Hospital from Jun 2022 to Oct 2023, enrolling 54 patients undergoing general surgery using domestically produced Toumai? Endoscopic Surgical Robotic System. The primary study endpoint was surgical success rate, and the secondary study endpoints were intraoperative bleeding, operative time, complications, system performance, hospitalization days.Results:In this study, robotic surgery was successfully completed in 52 patients, and in 2 patients undergoing thyroid operation it was converted to open surgery due to bleeding, with a success rate of 96%, no organ injury or death during surgery, and no system failure. The types of surgery included cholecystectomy, radical gastric cancer resection, radical colorectal cancer resection, inguinal hernia repair, partial hepatectomy, total thyroidectomy and choledocho-jejunal anastomosis.Conclusion:The study provides preliminary evidence of the safety and efficacy of the Toumai? Endoscopic Surgical Robotic System for the treatment of general surgical diseases.

Result Analysis
Print
Save
E-mail