Cancer biotherapy & radiopharmaceuticals最新文献_第7页

Biodistribution and dosimetry of free 211At, 125I- and 131I- in rats. 游离211At、125I-和131I-在大鼠体内的生物分布和剂量测定。

IF 3.4

Cancer biotherapy & radiopharmaceuticals Pub Date : 2013-11-01 Epub Date: 2013-06-22 DOI: 10.1089/cbr.2013.1483

Johan Spetz, Nils Rudqvist, Eva Forssell-Aronsson

{"title":"Biodistribution and dosimetry of free 211At, 125I- and 131I- in rats.","authors":"Johan Spetz, Nils Rudqvist, Eva Forssell-Aronsson","doi":"10.1089/cbr.2013.1483","DOIUrl":"https://doi.org/10.1089/cbr.2013.1483","url":null,"abstract":"131I is widely used for therapy in the clinic and 125I and 131I, and increasingly 211At, are often used in experimental studies. It is important to know the biodistribution and dosimetry for these radionuclides to determine potential risk organs when using radiopharmaceuticals containing these radionuclides. The purpose of this study was to investigate the biodistribution of 125I-, 131I-, and free 211At in rats and to determine absorbed doses to various organs and tissues. Male Sprague Dawley rats were injected simultaneously with 0.1-0.3 MBq 125I- and 0.1-0.3 MBq 131I-, or 0.05-0.2 MBq 211At and sacrificed 1 hour to 7 days after injection. The activities and activity concentrations in organs and tissues were determined and mean absorbed doses were calculated. The biodistribution of 125I- was similar to that of 131I- but the biodistribution of free 211At was different compared to 125I- and 131I-. The activity concentration of radioiodine was higher compared with 211At in the thyroid and lower in all extrathyroidal tissues. The mean absorbed dose per unit injected activity was highest to the thyroid. 131I gave the highest absorbed dose to the thyroid, and 211At gave the highest absorbed dose to all other tissues studied.","PeriodicalId":518937,"journal":{"name":"Cancer biotherapy & radiopharmaceuticals","volume":" ","pages":"657-64"},"PeriodicalIF":3.4,"publicationDate":"2013-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1089/cbr.2013.1483","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"31617169","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 68

Synthesis and biological evaluation of 90Y-labeled porphyrin-DOTA conjugate: a potential molecule for targeted tumor therapy. 90y标记卟啉- dota缀合物的合成及生物学评价:一种潜在的靶向肿瘤治疗分子。

IF 3.4

Cancer biotherapy & radiopharmaceuticals Pub Date : 2013-11-01 Epub Date: 2013-07-09 DOI: 10.1089/cbr.2013.1512

Sweety Mittal, Mohini Bhadwal, Tapas Das, Haladhar Dev Sarma, Rubel Chakravarty, Ashutosh Dash, Sharmila Banerjee, M R A Pillai

{"title":"Synthesis and biological evaluation of 90Y-labeled porphyrin-DOTA conjugate: a potential molecule for targeted tumor therapy.","authors":"Sweety Mittal, Mohini Bhadwal, Tapas Das, Haladhar Dev Sarma, Rubel Chakravarty, Ashutosh Dash, Sharmila Banerjee, M R A Pillai","doi":"10.1089/cbr.2013.1512","DOIUrl":"https://doi.org/10.1089/cbr.2013.1512","url":null,"abstract":"An unsymmetrically substituted porphyrin, 5-[4-(3-amino)-n-propyloxyphenyl]-10,15,20-tris-(4-carboxymethyleneoxyphenyl)porphyrin, was synthesized and coupled with p-NCS-benzyl-DOTA [p-isothiocyanato-benzyl-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid] for exploring its possible potential in targeted tumor therapy. The porphyrin-DOTA conjugate was radiolabeled with 90Y, obtained from a 90Sr/90Y electrochemical generator, developed in-house. Biodistribution studies performed in Swiss mice bearing fibrosarcoma tumor showed good tumor uptake (∼3.4% injected activity in per g of tumor) within 30 minutes postinjection. The tumor activity decreased with the progress of time, however, tumor to blood and tumor to muscle ratios considerably increased at 4 days postadministration owing to the clearance of the initially accumulated activities from the nontarget organs. The nonaccumulated activity exhibited major clearance through renal pathway.","PeriodicalId":518937,"journal":{"name":"Cancer biotherapy & radiopharmaceuticals","volume":" ","pages":"651-6"},"PeriodicalIF":3.4,"publicationDate":"2013-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1089/cbr.2013.1512","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"31208029","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 14

Associations between the four toll-like receptor polymorphisms and the risk of gastric cancer: a meta-analysis. 四种toll样受体多态性与胃癌风险之间的关系:一项荟萃分析。

IF 3.4

Cancer biotherapy & radiopharmaceuticals Pub Date : 2013-11-01 Epub Date: 2013-09-05 DOI: 10.1089/cbr.2012.1395

Jian Chen, Sheng Hu, Sanghua Liang, Qilong Chen, Qingqing Yang, Wenling Zheng, Wenli Ma

{"title":"Associations between the four toll-like receptor polymorphisms and the risk of gastric cancer: a meta-analysis.","authors":"Jian Chen, Sheng Hu, Sanghua Liang, Qilong Chen, Qingqing Yang, Wenling Zheng, Wenli Ma","doi":"10.1089/cbr.2012.1395","DOIUrl":"https://doi.org/10.1089/cbr.2012.1395","url":null,"abstract":"Purpose: The association between Toll-like receptor 2 (TLR2) -196 to -174del polymorphism and Toll-like receptor 4 (TLR4) polymorphisms (Asp299Gly, Thr399Ile, and 3725G>C) and gastric cancer risk are still conflicting. For better understanding of the effects of these four polymorphisms on gastric cancer risk, a meta-analysis was performed.Methods: An extensive search was performed to identify all case-control studies investigating such associations. Odds ratios (ORs) with 95% confidence intervals (CIs) were estimated to assess the relationship.Results: A total of 21 studies (3,436 cases and 4,239 controls) were found to be eligible for meta-analysis. In the overall analysis, a significantly increased risk was observed in TLR4 Asp299Gly polymorphism (G allele vs. A allele: OR=1.84, 95%CI: 1.41, 2.39; GA vs. AA: OR=1.89, 95%CI: 1.43, 2.48; Recessive model: OR=1.90, 95%CI: 1.44, 2.49) and TLR4 Thr399Ile polymorphism (T allele vs. C allele: OR=1.97, 95%CI: 1.22, 3.18; TC vs. CC: OR=1.94, 95%CI: 1.19, 3.15; Recessive model: OR=1.98, 95%CI: 1.21, 3.21), whereas no associations were found in any genetic models of TLR2 -196 to -174del and TLR4 3725G>C polymorphisms. Similar results were found in the subgroup analyses by ethnicity. However, we detected that A allele carriers of the TLR4 Asp299Gly polymorphism might have an increase risk of gastric cancer in the Helicobacter pylori-positive population (G allele vs. A allele: OR=2.01, 95%CI: 1.22, 3.31).Conclusion: The results of this meta-analysis indicate that the TLR4 Asp299Gly and Thr399Ile polymorphisms are risk factors for gastric cancer development.","PeriodicalId":518937,"journal":{"name":"Cancer biotherapy & radiopharmaceuticals","volume":" ","pages":"674-81"},"PeriodicalIF":3.4,"publicationDate":"2013-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1089/cbr.2012.1395","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"31709166","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 17

Penetratin-mediated delivery enhances the antitumor activity of the cationic antimicrobial peptide Magainin II. 穿透素介导的递送增强了阳离子抗菌肽Magainin II的抗肿瘤活性。

IF 3.4

Cancer biotherapy & radiopharmaceuticals Pub Date : 2013-05-01 Epub Date: 2013-01-03 DOI: 10.1089/cbr.2012.1328

Shan Liu, Hao Yang, Lin Wan, Jingqiu Cheng, Xiaofeng Lu

{"title":"Penetratin-mediated delivery enhances the antitumor activity of the cationic antimicrobial peptide Magainin II.","authors":"Shan Liu, Hao Yang, Lin Wan, Jingqiu Cheng, Xiaofeng Lu","doi":"10.1089/cbr.2012.1328","DOIUrl":"https://doi.org/10.1089/cbr.2012.1328","url":null,"abstract":"Cationic antimicrobial peptides (CAPs) with antitumor activity have potential for use as novel antitumor agents because of their lower risk for induction of resistance. Of these peptides, magainin II (MG2) exhibited cytotoxicity in tumor cells only at high concentrations, likely due to the inefficiency of MG2 in cell membrane binding and cell entry. Conjugation to a cell-penetrating peptide (CPP) might enhance the cytotoxicity of MG2 in tumor cells. Here, we constructed a fusion peptide MG2A by conjugating MG2 to the N-terminus of the CPP penetratin (Antp). It was found that the fusion peptide MG2A is more potent than unconjugated MG2 at tumor cell killing. The IC50s of MG2A for the tumor cells tested were at least 30 times lower than the IC50s of unconjugated MG2. These data indicate that conjugation to Antp significantly enhanced the cytotoxicity of MG2 in tumor cells. Moreover, the IC50s of MG2A for tumor cells are within 2 to 3 μM, which are about three to five times lower than the IC50 for normal cells. Furthermore, chondroitin sulfate (CS) was found to be overexpressed on the surface of the tested tumor cells, and the cytotoxicity of MG2A could be inhibited by the addition of exogenous CS. These results suggest that binding of Antp to CS on tumor cells might be one important cause for the selective cytotoxicity of MG2A in tumor cells. Taken together, conjugation of MG2 to Antp can significantly enhance its antitumor activity, and the fusion of CAP to Antp might be an alternative for cancer-targeted therapy.","PeriodicalId":518937,"journal":{"name":"Cancer biotherapy & radiopharmaceuticals","volume":" ","pages":"289-97"},"PeriodicalIF":3.4,"publicationDate":"2013-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1089/cbr.2012.1328","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40208393","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 43

Quantification of dose nonuniformities by voxel-based dosimetry in patients receiving 90Y-ibritumomab-tiuxetan. 90y -ibritumomab- tixetan患者剂量不均匀性的体素定量分析

IF 3.4

Cancer biotherapy & radiopharmaceuticals Pub Date : 2013-03-01 Epub Date: 2013-01-04 DOI: 10.1089/cbr.2012.1299

Francesco Cicone, Marco D'Arienzo, Andrea Carpaneto, Eleonora Russo, Angela Coniglio, Angelika Bischof Delaloye, Francesco Scopinaro

{"title":"Quantification of dose nonuniformities by voxel-based dosimetry in patients receiving 90Y-ibritumomab-tiuxetan.","authors":"Francesco Cicone, Marco D'Arienzo, Andrea Carpaneto, Eleonora Russo, Angela Coniglio, Angelika Bischof Delaloye, Francesco Scopinaro","doi":"10.1089/cbr.2012.1299","DOIUrl":"https://doi.org/10.1089/cbr.2012.1299","url":null,"abstract":"Unlabelled: Abstract Objective: To assess the impact of nonuniform dose distribution within lesions and tumor-involved organs of patients receiving Zevalin(®), and to discuss possible implications of equivalent uniform biological effective doses (EU-BED) on treatment efficacy and toxicity. MATLAB™ -based software for voxel-based dosimetry was adopted for this purpose.Methods: Eleven lesions from seven patients with either indolent or aggressive non-Hodgkin lymphoma were analyzed, along with four organs with disease. Absorbed doses were estimated by a direct integration of single-voxel kinetic data from serial tomographic images. After proper corrections, differential BED distributions and surviving cell fractions were estimated, allowing for the calculation of EU-BED. To quantify dose uniformity in each target area, a heterogeneity index was defined.Results: Average doses were below those prescribed by conventional radiotherapy to eradicate lymphoma lesions. Dose heterogeneity and effect on tumor control varied among lesions, with no apparent relation to tumor mass. Although radiation doses to involved organs were safe, unexpected liver toxicity occurred in one patient who presented with a pattern of diffuse infiltration.Conclusion: Voxel-based dosimetry and radiobiologic modeling can be successfully applied to lesions and tumor-involved organs, representing a methodological advance over estimation of mean absorbed doses. However, effects on tumor control and organ toxicity still cannot be easily predicted.","PeriodicalId":518937,"journal":{"name":"Cancer biotherapy & radiopharmaceuticals","volume":" ","pages":"98-107"},"PeriodicalIF":3.4,"publicationDate":"2013-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1089/cbr.2012.1299","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40212967","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 9

Indigenous (125)I brachytherapy source for the management of intraocular melanomas in India. 印度近距离治疗眼内黑色素瘤的来源

IF 3.4

Cancer biotherapy & radiopharmaceuticals Pub Date : 2013-02-01 DOI: 10.1089/cbr.2011.1123

Parag K Shah, Ulagiappa Selvaraj, Venkatapathy Narendran, Pandurangan Guhan, Sanjay Kumar Saxena, Ashutosh Dash

{"title":"Indigenous (125)I brachytherapy source for the management of intraocular melanomas in India.","authors":"Parag K Shah, Ulagiappa Selvaraj, Venkatapathy Narendran, Pandurangan Guhan, Sanjay Kumar Saxena, Ashutosh Dash","doi":"10.1089/cbr.2011.1123","DOIUrl":"https://doi.org/10.1089/cbr.2011.1123","url":null,"abstract":"Episcleral plaque brachytherapy using (125)I seed is a viable option for the management of intraocular cancer with minimal invasiveness and surgical complications. This article describes the fabrication of (125)I seeds and initial experience on their use for the management of intraocular choroidal melanomas. The process of (125)I seed fabrication includes immobilization of (125)I into palladium-coated silver wires, its encapsulation in titanium capsules using Nd: YAG laser and quality control to assure safety. Plaque preparation consists of the assignment of seeds to slots on the plaque to achieve a desired dose rate distribution. The clinical study reported here includes the retrospective review of 9 eyes of 9 patients who underwent ophthalmic brachytherapy between May 2008 and June 2011. The average apical diameter before brachytherapy was 7.6 mm and the average largest basal diameter was 12.1 mm, which reduced to 3.3 and 7.2 mm, respectively, after the procedure at an average follow-up of 24 months. Patients in our studies experienced good local tumor control. The results of this study represent a significant step forward in the management of intraocular tumors in India.","PeriodicalId":518937,"journal":{"name":"Cancer biotherapy & radiopharmaceuticals","volume":" ","pages":"21-8"},"PeriodicalIF":3.4,"publicationDate":"2013-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1089/cbr.2011.1123","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40222516","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 6

Recombinant hepatitis B virus surface antigen formulated with B-type CpG oligodeoxynucleotide induces therapeutic immunity against hepatitis B virus surface antigen-expressing liver cancer cells in mice. 用B型CpG低聚脱氧核苷酸配制的重组乙型肝炎病毒表面抗原可诱导对表达乙型肝炎病毒表面抗原的小鼠肝癌细胞的治疗性免疫。

IF 3.4

Cancer biotherapy & radiopharmaceuticals Pub Date : 2012-05-01 Epub Date: 2012-04-26 DOI: 10.1089/cbr.2011.1127

Xiaojing Zhou, Hongfei Wei, Peng Sun, Xiuli Wu, Min Wan, Peng Zhang, Sheng Guo, Tiesuo Zhao, Yongli Yu, Liying Wang

{"title":"Recombinant hepatitis B virus surface antigen formulated with B-type CpG oligodeoxynucleotide induces therapeutic immunity against hepatitis B virus surface antigen-expressing liver cancer cells in mice.","authors":"Xiaojing Zhou, Hongfei Wei, Peng Sun, Xiuli Wu, Min Wan, Peng Zhang, Sheng Guo, Tiesuo Zhao, Yongli Yu, Liying Wang","doi":"10.1089/cbr.2011.1127","DOIUrl":"https://doi.org/10.1089/cbr.2011.1127","url":null,"abstract":"To develop a therapeutic vaccine against hepatitis B virus surface antigen (HBsAg)-expressing liver cancer, we tried to prepare a vaccine by formulating recombinant HBsAg with BW006, a B type CpG oligodeoxynucleotide (ODN) with Th1-biasing activity, and examined its potency of inducing therapeutic immunity against HBsAg-expressing liver cancer cells in mice. When applied therapeutically, BW006 could assist HBsAg to induce vigorous immune responses capable of inhibiting the growth of HBsAg-expressing liver cancer cells and prolonging the survival of mice bearing HBsAg-expressing liver cancer cells. In vivo and in vitro experiments showed that the BW006-adjuvanted HBsAg enhanced the production of IgG2a antibodies, interferon-γ, and interleukin-12 and facilitated the generation of specific cytotoxic T lymphocyte that killed the HBsAg-expressing liver cancer cells. These results suggest that the BW006-adjuvanted HBsAg might be developed into a candidate tumor vaccine for the treatment of HBsAg-expressing liver cancer.","PeriodicalId":518937,"journal":{"name":"Cancer biotherapy & radiopharmaceuticals","volume":" ","pages":"234-42"},"PeriodicalIF":3.4,"publicationDate":"2012-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1089/cbr.2011.1127","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40187042","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 2

Treatment with unlabeled mAb BR96 after radioimmunotherapy with 177Lu-DOTA-BR96 in a syngeneic rat colon carcinoma model. 177Lu-DOTA-BR96放射免疫治疗后无标记单抗BR96治疗同基因大鼠结肠癌模型。

IF 3.4

Cancer biotherapy & radiopharmaceuticals Pub Date : 2012-04-01 Epub Date: 2012-03-14 DOI: 10.1089/cbr.2011.1132

Sophie E Eriksson, Tomas Ohlsson, Rune Nilsson, Jan Tennvall

{"title":"Treatment with unlabeled mAb BR96 after radioimmunotherapy with 177Lu-DOTA-BR96 in a syngeneic rat colon carcinoma model.","authors":"Sophie E Eriksson, Tomas Ohlsson, Rune Nilsson, Jan Tennvall","doi":"10.1089/cbr.2011.1132","DOIUrl":"https://doi.org/10.1089/cbr.2011.1132","url":null,"abstract":"Metastatic disease after successful treatment of the primary tumor continues to be a therapeutic challenge. Enhancement of therapeutic effects by the administration of unlabeled monoclonal antibodies (mAbs) after radioimmunotherapy (RIT) may provide a means of preventing or delaying the development of metastatic disease. In the present study, Brown Norway rats with syngeneic grafted colon carcinomas were administered the minimal effective therapeutic dose of 400 MBq/kg lutetium-177 ((177)Lu)-DOTA-BR96. After 2 weeks, half of the animals were given 15 mg/kg unlabeled mAb BR96 as consolidation therapy. Treatment response and toxicity were monitored 100 days after the treatment with unlabeled BR96. The treatment with unlabeled mAb after RIT resulted in a complete response (CR) in 19 of 19 animals, while RIT alone resulted in a CR in 17 of 19 animals. The additional treatment did not affect the number of animals with metastatic disease or the time to clinical symptoms of metastases. RIT resulted in reversible myelotoxicity. The unlabeled mAb BR96 did not cause any additional toxicity, making it possible to repeat the consolidation therapy.","PeriodicalId":518937,"journal":{"name":"Cancer biotherapy & radiopharmaceuticals","volume":" ","pages":"175-82"},"PeriodicalIF":3.4,"publicationDate":"2012-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1089/cbr.2011.1132","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40163519","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 9

Distribution, elimination, and renal handling of (99m)technetium-Demogastrin 1. (99m) techtium - demogastrin 1的分布、消除和肾脏处理。

IF 3.4

Cancer biotherapy & radiopharmaceuticals Pub Date : 2012-03-01 DOI: 10.1089/cbr.2011.1008

Frantisek Trejtnar, Alice Laznickova, Milan Laznicek, Zbynek Novy, Theodosia Maina, Berthold A Nock, Martin Behe

{"title":"Distribution, elimination, and renal handling of (99m)technetium-Demogastrin 1.","authors":"Frantisek Trejtnar, Alice Laznickova, Milan Laznicek, Zbynek Novy, Theodosia Maina, Berthold A Nock, Martin Behe","doi":"10.1089/cbr.2011.1008","DOIUrl":"https://doi.org/10.1089/cbr.2011.1008","url":null,"abstract":"Radiolabeled cholecystokinin/gastrin (CCK) receptor-targeting peptides are promising compounds for radiodiagnosis and radiotherapy of certain malignancies. This study evaluated the pharmacokinetic profile of a CCK-2 receptor-specific peptide, Demogastrin 1, labeled with technetium-99m ((99m)Tc-Demogastrin 1), in rats. To investigate the fate of (99m)Tc-Demogastrin 1 in the rat, biodistribution and elimination studies in vivo were performed, and elimination parameters in perfused rat liver and kidney were determined. Biodistribution studies showed that (99m)Tc-Demogastrin 1 was rapidly cleared from the blood and most organs. A significant amount of radioactivity was detected in the CCK-2 receptor-rich organs, such as the stomach. Low radioactivity was found in the CCK-1 receptor-rich organs. Radioactivity in bowels and stomach declined relatively slowly. High and long-term retention of radioactivity in the kidneys was observed. Elimination of (99m)Tc-Demogastrin 1 via the bile was negligible. A high and rapid renal excretion was observed in elimination experiments in vivo. In the perfused kidney, glomerular filtration was found to be the main renal excretion mechanism of (99m)Tc-Demogastrin 1. Demogastrin 1 was distributed preferentially to the organs expressing CCK-2 receptors. The decisive elimination route of (99m)Tc-Demogastrin 1 in rats was urinary excretion. A high and prolonged renal retention may limit potential clinical use of the compound.","PeriodicalId":518937,"journal":{"name":"Cancer biotherapy & radiopharmaceuticals","volume":" ","pages":"169-74"},"PeriodicalIF":3.4,"publicationDate":"2012-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1089/cbr.2011.1008","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40157647","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 2

Radiation induces up-regulation of somatostatin receptors 1, 2, and 5 in small cell lung cancer in vitro also at low absorbed doses. 在体外小细胞肺癌中，低吸收剂量的辐射诱导生长抑素受体1、2和5的上调。

IF 3.4

Cancer biotherapy & radiopharmaceuticals Pub Date : 2011-12-01 Epub Date: 2011-11-07 DOI: 10.1089/cbr.2010.0921

Jenny Oddstig, Peter Bernhardt, Ola Nilsson, Håkan Ahlman, Eva Forssell-Aronsson

{"title":"Radiation induces up-regulation of somatostatin receptors 1, 2, and 5 in small cell lung cancer in vitro also at low absorbed doses.","authors":"Jenny Oddstig, Peter Bernhardt, Ola Nilsson, Håkan Ahlman, Eva Forssell-Aronsson","doi":"10.1089/cbr.2010.0921","DOIUrl":"https://doi.org/10.1089/cbr.2010.0921","url":null,"abstract":"Background: Radiation can be used to up-regulate the expression of the somatostatin receptor (sstr) subtype 2 in small cell lung cancer (SCLC) cells at absorbed doses of 2-8 Gy. Increased sstr expression results in increased binding of radiolabeled somatostatin analogs to the tumor cell, which enhances the efficacy of systemic radionuclide therapy. The aim of this study was to determine if lower absorbed doses could up-regulate sstr2 expression, and possibly influence other sstr subtypes.Methods: Human H69 SCLC cells were irradiated with an absorbed dose of 0.12-6.0 Gy and the sstr mRNA expression 3 days after irradiation was measured by quantitative real-time polymerase chain reaction for sstr1-5. At the same time point was the binding of [(177)Lu]-DOTA(0)-Tyr(3)-octreotate to the cells measured after irradiation to an absorbed dose of 0.12-2.0 Gy and compared to the binding to nonirradiated cells.Results: mRNA expression of sstr1, sstr2, and sstr5 was increased by a factor of 1.5-2 in cells irradiated with absorbed doses≥4 Gy and the binding of [(177)Lu]-DOTA(0)-Tyr(3)-octreotate was, accordingly, 2-3 times higher to irradiated cells for all absorbed doses, except 0.25 Gy.Conclusion: The binding of [(177)Lu]-DOTA(0)-Tyr(3)-octreotate was increased after radiation exposure. This increase was observed at low absorbed doses in parallel with up-regulation of sstr1, sstr2, and sstr5 mRNA.","PeriodicalId":518937,"journal":{"name":"Cancer biotherapy & radiopharmaceuticals","volume":" ","pages":"759-65"},"PeriodicalIF":3.4,"publicationDate":"2011-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1089/cbr.2010.0921","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40133990","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 16