scholarly journals Optimizing the Performance of 68Ga Labeled FSHR Ligand in Prostate Cancer Model by Means of Aprotinin

2021 ◽  
Author(s):  
Donghui Pan ◽  
Lizhen Wang ◽  
Xinyu Wang ◽  
Junjie Yan ◽  
YuPing Xu ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Enzyme Inhibitors ◽  
Pharmacokinetic Profile ◽  
Cancer Model ◽  
Micropet Imaging ◽  
Average Percentage ◽  
Ic50 Value ◽  
Imaging Properties ◽  
Prostate Cancer Model

Abstract Purpose: Radiolabeled FSH1 peptides are potential specific probes for FSHR imaging. However, moderate uptakes and fast washout from the tumors may limit its widespread use. In this study, 68Ga labeled modified FSH1 analogs was prepared and the imaging properties were determined in the prostate cancer model with or without aprotinin.Methods: NOTA-MAL-FSH4 was synthesized and labeled with 68Ga. The pharmacokinetic profile of the peptide after co-administration with aprotinin was determined through metabolism analyses and microPET imaging.Results: 68Ga-NOTA-MAL-FSH4 was successfully prepared. The IC50 value of displacement 68Ga-NOTA-MAL-FSH4 with FSH1 was 139.4±1.16 nM. The PC-3 prostate tumor was visible after administration of the 68Ga labeled tracer. In vitro RP-HPLC analysis revealed that the average percentage of intact peptide in the plasma, liver and tumor was 8.30, 9.57 and 7.06 % respectively. In presence of aprotinin, the amounts of intact peptide increased to 34.32%, 20.63 % and 15.39 % in the counterparts respectively. MicroPET imaging showed that the uptakes of PC-3 tumors at 60mins after co-administration of 100μg, 200μg or 400μg enzyme inhibitors were 2.91±0.21%ID/g, 3.89±0.16%ID/g and 9.21±0.22%ID/g respectively.Conclusion: With the aid of a serine protease inhibitor, the performance of the 68Ga labeled peptide was optimized, which may benefit further clinical application.

scholarly journals Enhanced anti-tumor efficacy and mechanisms associated with docetaxel-piperine combination- in vitro and in vivo investigation using a taxane-resistant prostate cancer model

Oncotarget ◽  
2017 ◽  
Vol 9 (3) ◽  
pp. 3338-3352 ◽  
Author(s):  
Chenrui Li ◽  
Zhijun Wang ◽  
Qian Wang ◽  
Rebecca Lucinda Ka Yan Ho ◽  
Ying Huang ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Cancer Model ◽  
Prostate Cancer Model

scholarly journals Multiplex profiling identifies clinically relevant signalling proteins in an isogenic prostate cancer model of radioresistance

2019 ◽  
Vol 9 (1) ◽  
Author(s):  
S. Inder ◽  
M. Bates ◽  
N. Ni Labhrai ◽  
N. McDermott ◽  
J. Schneider ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Expression Profiles ◽  
Protein Profiling ◽  
Cancer Model ◽  
Protein Levels ◽  
Notch 3 ◽  
Molecular Radiation ◽  
Protein Expression Profiles ◽  
Prostate Cancer Model

AbstractThe exact biological mechanism governing the radioresistant phenotype of prostate tumours at a high risk of recurrence despite the delivery of advanced radiotherapy protocols remains unclear. This study analysed the protein expression profiles of a previously generated isogenic 22Rv1 prostate cancer model of radioresistance using DigiWest multiplex protein profiling for a selection of 90 signalling proteins. Comparative analysis of the profiles identified a substantial change in the expression of 43 proteins. Differential PARP-1, AR, p53, Notch-3 and YB-1 protein levels were independently validated using Western Blotting. Pharmacological targeting of these proteins was associated with a mild but significant radiosensitisation effect at 4Gy. This study supports the clinical relevance of isogenic in vitro models of radioresistance and clarifies the molecular radiation response of prostate cancer cells.

scholarly journals Influence of the Position and Composition of Radiometals and Radioiodine Labels on Imaging of Epcam Expression in Prostate Cancer Model Using the DARPin Ec1

Cancers ◽  
2021 ◽  
Vol 13 (14) ◽  
pp. 3589
Author(s):  
Sergey M. Deyev ◽  
Tianqi Xu ◽  
Yongsheng Liu ◽  
Alexey Schulga ◽  
Elena Konovalova ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Cell Adhesion Molecule ◽  
Early Stage ◽  
Cancer Model ◽  
C Terminus ◽  
Indium 111 ◽  
Gallium 68 ◽  
Imaging Properties ◽  
Selection Of ◽  
Prostate Cancer Model

The epithelial cell adhesion molecule (EpCAM) is intensively overexpressed in 40–60% of prostate cancer (PCa) cases and can be used as a target for the delivery of drugs and toxins. The designed ankyrin repeat protein (DARPin) Ec1 has a high affinity to EpCAM (68 pM) and a small size (18 kDa). Radiolabeled Ec1 might be used as a companion diagnostic for the selection of PCa patients for therapy. The study aimed to investigate the influence of radiolabel position (N- or C-terminal) and composition on the targeting and imaging properties of Ec1. Two variants, having an N- or C-terminal cysteine, were produced, site-specifically conjugated to a DOTA chelator and labeled with cobalt-57, gallium-68 or indium-111. Site-specific radioiodination was performed using ((4-hydroxyphenyl)-ethyl)maleimide (HPEM). Biodistribution of eight radiolabeled Ec1-probes was measured in nude mice bearing PCa DU145 xenografts. In all cases, positioning of a label at the C-terminus provided the best tumor-to-organ ratios. The non-residualizing [125I]I-HPEM label provided the highest tumor-to-muscle and tumor-to-bone ratios and is more suitable for EpCAM imaging in early-stage PCa. Among the radiometals, indium-111 provided the highest tumor-to-blood, tumor-to-lung and tumor-to-liver ratios and could be used at late-stage PCa. In conclusion, label position and composition are important for the DARPin Ec1.

NAD+ depletion by APO866 in combination with radiation in a prostate cancer model, results from an in vitro and in vivo study

2014 ◽  
Vol 110 (2) ◽  
pp. 348-354 ◽  
Author(s):  
Shuraila F. Zerp ◽  
Conchita Vens ◽  
Ben Floot ◽  
Marcel Verheij ◽  
Baukelien van Triest
Keyword(s):  
Prostate Cancer ◽  
In Vivo Study ◽  
Cancer Model ◽  
Nad Depletion ◽  
Prostate Cancer Model

Evaluation of Thermal Therapy in a Prostate Cancer Model Using a Wet Electrode Radiofrequency Probe

2001 ◽  
Vol 15 (6) ◽  
pp. 629-640 ◽  
Author(s):  
S. Bhowmick ◽  
D.J. Swanlund ◽  
J.E. Coad ◽  
L. Lulloff ◽  
M.F. Hoey ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Thermal Therapy ◽  
Cancer Model ◽  
Prostate Cancer Model
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