The Experts below are selected from a list of 10311 Experts worldwide ranked by ideXlab platform
Seyed Jalal Hosseinimehr - One of the best experts on this subject based on the ideXlab platform.
-
99mTc-(Tricine)-HYNIC-Lys-FROP Peptide for Breast Tumor Targeting.
Anti-cancer Agents in Medicinal Chemistry, 2019Co-Authors: Sajjad Ahmadpour, Seyed Mohammad Abedi, Zohreh Noaparast, Seyed Jalal HosseinimehrAbstract:BACKGROUND Breast cancer is a malignant disease with high mortality rate among women in the world. It is necessary to diagnose breast cancer at the early stage before it metastasizes in patients. OBJECTIVE The aim of this study is the evaluation of 99mTc-(Tricine)-HYNIC-Lys-FROP for breast tumor imaging. METHOD Lys-FROP peptide was labeled with 99mTc using HYNIC as chelator and Tricine as co-ligand. Specific binding of this radiolabeled peptide on breast cancerous cell was assessed in different cell lines as well as in tumor-bearing mice. RESULTS HYNIC-Lys-FROP peptide was labeled with 99mTc at radiochemical purity more than 99%. It was observed high stability in normal saline and serum about 95%. The highest cellular uptake was observed in MCF-7 breast tumor cells treated with 99mTc-(Tricine)-HYNIC-Lys-FROP as compared to other cell lines (lung, ovarian, T47D breast cancer cell lines). Biodistribution results in female MCF-7 tumor-bearing mice showed the relatively high tumor uptake and tumor-muscle ratio as 3.82 ± 0.66 after 15 min post-injection of 99mTc-(Tricine)- HYNIC-Lys-FROP. Tumor uptake was reduced in mice that were co-injected with excess of unlabeled peptide to be 0.91 ± 0.08. CONCLUSION Findings showed this radiolabeled peptide is a promising candidate for tumor targeting and molecular imaging of breast cancer.
-
99mTc-HYNIC-(Ser)3-LTVPWY peptide bearing Tricine as co-ligand for targeting and imaging of HER2 overexpression tumor
Radiochimica Acta, 2018Co-Authors: Nazan Aligholikhamseh, Seyed Mohammad Abedi, Sajjad Ahmadpour, Fatemeh Khodadust, Seyed Jalal HosseinimehrAbstract:Abstract Human epidermal growth factor receptor 2 (HER2) is overexpressed in several cancers. Today’s tumor targeting is receiving more attention due to its specificity to target receptor-dependent cancers. The aim of this study was to evaluate the 99mTc-HYNIC-(Tricine)-(Ser)3-LTVPWY peptide for tumor targeting and imaging with overexpression of HER2. HYNIC-(Ser)3-LTVPWY peptide was labeled with 99mTc using Tricine as a co-ligand at room temperature. Specific binding of this radiolabeled peptide was assessed on four cancer cell lines with different levels of HER2 receptor expression. Also the affinity of 99mTc-HYNIC-(Tricine)-(Ser)3-LTVPWY peptide to the HER2 receptor was evaluated in the SKOV-3 cell line. Biodistribution study of this radiolabeled peptide was performed in SKOV-3 tumor bearing nude mice. The HYNIC conjugated peptide was simply labeled with 99mTc radionuclide with high labeling efficiency about 98±1% showing favorable stability in normal saline and human serum. In the presence of unlabeled peptide as competitor, the HER2 binding capacity of the radiolabeled peptide reduced (approximately five-fold). The KD and Bmax values were found 2.6±0.5 nM and (2.6±0.1)×106, respectively. The tumor/muscle ratios for this radiotracer were determined 1.17±0.77, 1.15±0.32 and 2.65±0.32 at 1, 2 and 4 h after injection, respectively. Presaturation of HER2 receptors in SKOV-3 xenografted nude mice showed a reduction in the tumor/muscle ratio confirming in vivo specificity of the peptide. According to SPECT imaging, the tumor was visualized in mouse after 4 h postinjection of radiolabeled peptide. 99mTc-HYNIC-(Tricine)-(Ser)3-LTVPWY peptide exhibited overexpressed HER2 tumor targeting.
-
Tricine co-ligand improved the efficacy of 99mTc-HYNIC-(Ser)3-J18 peptide for targeting and imaging of non-small-cell lung cancer.
Biomedicine & Pharmacotherapy, 2018Co-Authors: Zahra Shaghaghi, Seyed Mohammad Abedi, Seyed Jalal HosseinimehrAbstract:Abstract The early diagnosis of non-small cell lung cancer (NSCLC) is important for increasing survival rate and improving quality life of patients. The aim of this study was to investigate 99m Tc-(Tricine)-HYNIC-(Ser)3-J18 for targeting and imaging of NSCLC in A-549 xenografted nude mice. The (Ser)3-J18 peptide was conjugated with HYNIC and labeled with 99m Tc using Tricine as a co-ligand. The radiolabeled peptide was evaluated for its radiochemical purity, stability, receptor binding and internalization in vitro. The future experiments were performed for tumor targeting and imaging in A-549 tumor-bearing mice. 99m Tc-(Tricine)-HYNIC-(Ser)3-J18 was obtained at high labeling efficiency at room temperature and favorable stability in saline and human plasma. At the cellular level, the radiolabeled peptide specifically bond to A-549 cells with a KD 4.1 ± 1.3 nM. Biodistribution study revealed tumor to blood and tumor to muscle ratios were about 3.12 and 5.63 respectively after 2 h injection of radiolabeled peptide. These ratios were significantly decreased by co-injection of excess non-labeled peptide in mice. This radiolabeled peptide selectively targeted to NSCLC tumor and exhibited a high target uptake combined with acceptable low background activity for tumor imaging in mice. The results of this study and its comparison with another study showed that 99m Tc-(Tricine)-HYNIC-(Ser)3-J18 is better than previously reported radiolabeled peptide as 99m Tc-(EDDA/Tricine)-HYNIC-(Ser)3-J18 for NSCLC targeting and imaging.
-
99m Tc-HYNIC-(Tricine/EDDA)-FROP peptide for MCF-7 breast tumor targeting and imaging
Journal of Biomedical Science, 2018Co-Authors: Sajjad Ahmadpour, Seyed Mohammad Abedi, Zohreh Noaparast, Seyed Jalal HosseinimehrAbstract:Breast cancer is the most common malignancy among women in the world. Development of novel tumor-specific radiopharmaceuticals for early breast tumor diagnosis is highly desirable. In this study we developed 99mTc-HYNIC-(Tricine/EDDA)-Lys-FROP peptide with the ability of specific binding to MCF-7 breast tumor. The FROP-1 peptide was conjugated with the bifunctional chelator hydrazinonicotinamide (HYNIC) and labeled with 99mTc using Tricine/EDDA co-ligand. The cellular specific binding of 99mTc-HYNIC-FROP was evaluated on different cell lines as well as with blocking experiment on MCF-7 (human breast adenocarcinoma). The tumor targeting and imaging of this labeled peptide were performed on MCF-7 tumor bearing mice. Radiochemical purity for 99mTc-HYNIC-(Tricine/EDDA)-FROP was 99% which was determined with ITLC method. This radiolabeled peptide showed high stability in normal saline and serum about 98% which was monitored with HPLC method. In saturation binding experiments, the binding constant (Kd) to MCF-7 cells was determined to be 158 nM. Biodistribution results revealed that the 99mTc-HYNIC-FROP was mainly exerted from urinary route. The maximum tumor uptake was found after 30 min post injection (p.i.); however maximum tumor/muscle ratio was seen at 15 min p.i. The tumor uptake of this labeled peptide was specific and blocked by co-injection of excess FROP. According to the planar gamma imaging result, tumor was clearly visible due to the tumor uptake of 99mTc-HYNIC-(Tricine/EDDA)-FROP in mouse after 15 min p.i. The 99mTc-HYNIC-(Tricine/EDDA)-FROP is considered a promising probe with high specific binding to MCF-7 breast cancer cells.
-
99m tc hynic Tricine edda frop peptide for mcf 7 breast tumor targeting and imaging
Journal of Biomedical Science, 2018Co-Authors: Sajjad Ahmadpour, Seyed Mohammad Abedi, Zohreh Noaparast, Seyed Jalal HosseinimehrAbstract:Breast cancer is the most common malignancy among women in the world. Development of novel tumor-specific radiopharmaceuticals for early breast tumor diagnosis is highly desirable. In this study we developed 99mTc-HYNIC-(Tricine/EDDA)-Lys-FROP peptide with the ability of specific binding to MCF-7 breast tumor. The FROP-1 peptide was conjugated with the bifunctional chelator hydrazinonicotinamide (HYNIC) and labeled with 99mTc using Tricine/EDDA co-ligand. The cellular specific binding of 99mTc-HYNIC-FROP was evaluated on different cell lines as well as with blocking experiment on MCF-7 (human breast adenocarcinoma). The tumor targeting and imaging of this labeled peptide were performed on MCF-7 tumor bearing mice. Radiochemical purity for 99mTc-HYNIC-(Tricine/EDDA)-FROP was 99% which was determined with ITLC method. This radiolabeled peptide showed high stability in normal saline and serum about 98% which was monitored with HPLC method. In saturation binding experiments, the binding constant (Kd) to MCF-7 cells was determined to be 158 nM. Biodistribution results revealed that the 99mTc-HYNIC-FROP was mainly exerted from urinary route. The maximum tumor uptake was found after 30 min post injection (p.i.); however maximum tumor/muscle ratio was seen at 15 min p.i. The tumor uptake of this labeled peptide was specific and blocked by co-injection of excess FROP. According to the planar gamma imaging result, tumor was clearly visible due to the tumor uptake of 99mTc-HYNIC-(Tricine/EDDA)-FROP in mouse after 15 min p.i. The 99mTc-HYNIC-(Tricine/EDDA)-FROP is considered a promising probe with high specific binding to MCF-7 breast cancer cells.
Seyed Mohammad Abedi - One of the best experts on this subject based on the ideXlab platform.
-
99m tc edda Tricine hynic gnrh analogue as a potential imaging probe for diagnosis of prostate cancer
Chemical Biology & Drug Design, 2020Co-Authors: Arezou Masteri Farahani, Seyed Mohammad Abedi, Fariba Maleki, Nourollah Sadeghzadeh, Saeid Abediankenari, Mostafa ErfaniAbstract:Prostate cancer is a serious threat to men's health, so it is necessary to develop the techniques for early detection of this malignancy. Radiolabeled peptides are the useful tools for diagnosis of prostate cancer. In this research, we designed a new HYNIC-conjugated GnRH analogue and labeled it by 99m Tc with Tricine/EDDA as coligands. We used aminohexanoic acid (Ahx) as a hydrocarbon linker to generate 99m Tc-(Tricine/EDDA)-HYNIC-Ahx-[DLys6 ]GnRH. The radiopeptide exhibited high radiochemical purity and stability in solution and serum. Two human prostate cancer cell lines LN-CaP and DU-145 were used for cellular experiments. The binding specificity and affinity of radiopeptide for LN-CaP were superior to DU-145 cells. The Kd values for LN-CaP and DU-145 cells were 41.91 ± 7.03 nM and 55.96 ± 10.56 nM, respectively. High kidney uptake proved that the main excretion route of radiopeptide was through the urinary system. The tumor/muscle ratio of 99m Tc-HYNIC-Ahx-[DLys6 ]GnRH was 4.14 at 1 hr p.i. that decreased to 2.41 at 4 hr p.i. in LN-CaP tumor-xenografted nude mice. The blocking experiment revealed that the tumor uptake was receptor-mediated. The lesion was visualized clearly using 99m Tc-[DLys6 ]GnRH at 1 hr p.i. Accordingly, this research highlights the capability of 99m Tc-(Tricine/EDDA)-HYNIC-Ahx-[DLys6 ]GnRH peptide as a promising agent for GnRHR-expressing tumor imaging.
-
99m Tc-(EDDA/Tricine)-HYNIC-GnRH analogue as a potential imaging probe for diagnosis of prostate cancer.
Chemical Biology & Drug Design, 2020Co-Authors: Arezou Masteri Farahani, Seyed Mohammad Abedi, Fariba Maleki, Nourollah Sadeghzadeh, Saeid Abediankenari, Mostafa ErfaniAbstract:Prostate cancer is a serious threat to men's health, so it is necessary to develop the techniques for early detection of this malignancy. Radiolabeled peptides are the useful tools for diagnosis of prostate cancer. In this research, we designed a new HYNIC-conjugated GnRH analogue and labeled it by 99m Tc with Tricine/EDDA as coligands. We used aminohexanoic acid (Ahx) as a hydrocarbon linker to generate 99m Tc-(Tricine/EDDA)-HYNIC-Ahx-[DLys6 ]GnRH. The radiopeptide exhibited high radiochemical purity and stability in solution and serum. Two human prostate cancer cell lines LN-CaP and DU-145 were used for cellular experiments. The binding specificity and affinity of radiopeptide for LN-CaP were superior to DU-145 cells. The Kd values for LN-CaP and DU-145 cells were 41.91 ± 7.03 nM and 55.96 ± 10.56 nM, respectively. High kidney uptake proved that the main excretion route of radiopeptide was through the urinary system. The tumor/muscle ratio of 99m Tc-HYNIC-Ahx-[DLys6 ]GnRH was 4.14 at 1 hr p.i. that decreased to 2.41 at 4 hr p.i. in LN-CaP tumor-xenografted nude mice. The blocking experiment revealed that the tumor uptake was receptor-mediated. The lesion was visualized clearly using 99m Tc-[DLys6 ]GnRH at 1 hr p.i. Accordingly, this research highlights the capability of 99m Tc-(Tricine/EDDA)-HYNIC-Ahx-[DLys6 ]GnRH peptide as a promising agent for GnRHR-expressing tumor imaging.
-
99mTc-(Tricine)-HYNIC-Lys-FROP Peptide for Breast Tumor Targeting.
Anti-cancer Agents in Medicinal Chemistry, 2019Co-Authors: Sajjad Ahmadpour, Seyed Mohammad Abedi, Zohreh Noaparast, Seyed Jalal HosseinimehrAbstract:BACKGROUND Breast cancer is a malignant disease with high mortality rate among women in the world. It is necessary to diagnose breast cancer at the early stage before it metastasizes in patients. OBJECTIVE The aim of this study is the evaluation of 99mTc-(Tricine)-HYNIC-Lys-FROP for breast tumor imaging. METHOD Lys-FROP peptide was labeled with 99mTc using HYNIC as chelator and Tricine as co-ligand. Specific binding of this radiolabeled peptide on breast cancerous cell was assessed in different cell lines as well as in tumor-bearing mice. RESULTS HYNIC-Lys-FROP peptide was labeled with 99mTc at radiochemical purity more than 99%. It was observed high stability in normal saline and serum about 95%. The highest cellular uptake was observed in MCF-7 breast tumor cells treated with 99mTc-(Tricine)-HYNIC-Lys-FROP as compared to other cell lines (lung, ovarian, T47D breast cancer cell lines). Biodistribution results in female MCF-7 tumor-bearing mice showed the relatively high tumor uptake and tumor-muscle ratio as 3.82 ± 0.66 after 15 min post-injection of 99mTc-(Tricine)- HYNIC-Lys-FROP. Tumor uptake was reduced in mice that were co-injected with excess of unlabeled peptide to be 0.91 ± 0.08. CONCLUSION Findings showed this radiolabeled peptide is a promising candidate for tumor targeting and molecular imaging of breast cancer.
-
99mTc-HYNIC-(Ser)3-LTVPWY peptide bearing Tricine as co-ligand for targeting and imaging of HER2 overexpression tumor
Radiochimica Acta, 2018Co-Authors: Nazan Aligholikhamseh, Seyed Mohammad Abedi, Sajjad Ahmadpour, Fatemeh Khodadust, Seyed Jalal HosseinimehrAbstract:Abstract Human epidermal growth factor receptor 2 (HER2) is overexpressed in several cancers. Today’s tumor targeting is receiving more attention due to its specificity to target receptor-dependent cancers. The aim of this study was to evaluate the 99mTc-HYNIC-(Tricine)-(Ser)3-LTVPWY peptide for tumor targeting and imaging with overexpression of HER2. HYNIC-(Ser)3-LTVPWY peptide was labeled with 99mTc using Tricine as a co-ligand at room temperature. Specific binding of this radiolabeled peptide was assessed on four cancer cell lines with different levels of HER2 receptor expression. Also the affinity of 99mTc-HYNIC-(Tricine)-(Ser)3-LTVPWY peptide to the HER2 receptor was evaluated in the SKOV-3 cell line. Biodistribution study of this radiolabeled peptide was performed in SKOV-3 tumor bearing nude mice. The HYNIC conjugated peptide was simply labeled with 99mTc radionuclide with high labeling efficiency about 98±1% showing favorable stability in normal saline and human serum. In the presence of unlabeled peptide as competitor, the HER2 binding capacity of the radiolabeled peptide reduced (approximately five-fold). The KD and Bmax values were found 2.6±0.5 nM and (2.6±0.1)×106, respectively. The tumor/muscle ratios for this radiotracer were determined 1.17±0.77, 1.15±0.32 and 2.65±0.32 at 1, 2 and 4 h after injection, respectively. Presaturation of HER2 receptors in SKOV-3 xenografted nude mice showed a reduction in the tumor/muscle ratio confirming in vivo specificity of the peptide. According to SPECT imaging, the tumor was visualized in mouse after 4 h postinjection of radiolabeled peptide. 99mTc-HYNIC-(Tricine)-(Ser)3-LTVPWY peptide exhibited overexpressed HER2 tumor targeting.
-
Tricine co-ligand improved the efficacy of 99mTc-HYNIC-(Ser)3-J18 peptide for targeting and imaging of non-small-cell lung cancer.
Biomedicine & Pharmacotherapy, 2018Co-Authors: Zahra Shaghaghi, Seyed Mohammad Abedi, Seyed Jalal HosseinimehrAbstract:Abstract The early diagnosis of non-small cell lung cancer (NSCLC) is important for increasing survival rate and improving quality life of patients. The aim of this study was to investigate 99m Tc-(Tricine)-HYNIC-(Ser)3-J18 for targeting and imaging of NSCLC in A-549 xenografted nude mice. The (Ser)3-J18 peptide was conjugated with HYNIC and labeled with 99m Tc using Tricine as a co-ligand. The radiolabeled peptide was evaluated for its radiochemical purity, stability, receptor binding and internalization in vitro. The future experiments were performed for tumor targeting and imaging in A-549 tumor-bearing mice. 99m Tc-(Tricine)-HYNIC-(Ser)3-J18 was obtained at high labeling efficiency at room temperature and favorable stability in saline and human plasma. At the cellular level, the radiolabeled peptide specifically bond to A-549 cells with a KD 4.1 ± 1.3 nM. Biodistribution study revealed tumor to blood and tumor to muscle ratios were about 3.12 and 5.63 respectively after 2 h injection of radiolabeled peptide. These ratios were significantly decreased by co-injection of excess non-labeled peptide in mice. This radiolabeled peptide selectively targeted to NSCLC tumor and exhibited a high target uptake combined with acceptable low background activity for tumor imaging in mice. The results of this study and its comparison with another study showed that 99m Tc-(Tricine)-HYNIC-(Ser)3-J18 is better than previously reported radiolabeled peptide as 99m Tc-(EDDA/Tricine)-HYNIC-(Ser)3-J18 for NSCLC targeting and imaging.
Sajjad Ahmadpour - One of the best experts on this subject based on the ideXlab platform.
-
99mTc-(Tricine)-HYNIC-Lys-FROP Peptide for Breast Tumor Targeting.
Anti-cancer Agents in Medicinal Chemistry, 2019Co-Authors: Sajjad Ahmadpour, Seyed Mohammad Abedi, Zohreh Noaparast, Seyed Jalal HosseinimehrAbstract:BACKGROUND Breast cancer is a malignant disease with high mortality rate among women in the world. It is necessary to diagnose breast cancer at the early stage before it metastasizes in patients. OBJECTIVE The aim of this study is the evaluation of 99mTc-(Tricine)-HYNIC-Lys-FROP for breast tumor imaging. METHOD Lys-FROP peptide was labeled with 99mTc using HYNIC as chelator and Tricine as co-ligand. Specific binding of this radiolabeled peptide on breast cancerous cell was assessed in different cell lines as well as in tumor-bearing mice. RESULTS HYNIC-Lys-FROP peptide was labeled with 99mTc at radiochemical purity more than 99%. It was observed high stability in normal saline and serum about 95%. The highest cellular uptake was observed in MCF-7 breast tumor cells treated with 99mTc-(Tricine)-HYNIC-Lys-FROP as compared to other cell lines (lung, ovarian, T47D breast cancer cell lines). Biodistribution results in female MCF-7 tumor-bearing mice showed the relatively high tumor uptake and tumor-muscle ratio as 3.82 ± 0.66 after 15 min post-injection of 99mTc-(Tricine)- HYNIC-Lys-FROP. Tumor uptake was reduced in mice that were co-injected with excess of unlabeled peptide to be 0.91 ± 0.08. CONCLUSION Findings showed this radiolabeled peptide is a promising candidate for tumor targeting and molecular imaging of breast cancer.
-
99mTc-HYNIC-(Ser)3-LTVPWY peptide bearing Tricine as co-ligand for targeting and imaging of HER2 overexpression tumor
Radiochimica Acta, 2018Co-Authors: Nazan Aligholikhamseh, Seyed Mohammad Abedi, Sajjad Ahmadpour, Fatemeh Khodadust, Seyed Jalal HosseinimehrAbstract:Abstract Human epidermal growth factor receptor 2 (HER2) is overexpressed in several cancers. Today’s tumor targeting is receiving more attention due to its specificity to target receptor-dependent cancers. The aim of this study was to evaluate the 99mTc-HYNIC-(Tricine)-(Ser)3-LTVPWY peptide for tumor targeting and imaging with overexpression of HER2. HYNIC-(Ser)3-LTVPWY peptide was labeled with 99mTc using Tricine as a co-ligand at room temperature. Specific binding of this radiolabeled peptide was assessed on four cancer cell lines with different levels of HER2 receptor expression. Also the affinity of 99mTc-HYNIC-(Tricine)-(Ser)3-LTVPWY peptide to the HER2 receptor was evaluated in the SKOV-3 cell line. Biodistribution study of this radiolabeled peptide was performed in SKOV-3 tumor bearing nude mice. The HYNIC conjugated peptide was simply labeled with 99mTc radionuclide with high labeling efficiency about 98±1% showing favorable stability in normal saline and human serum. In the presence of unlabeled peptide as competitor, the HER2 binding capacity of the radiolabeled peptide reduced (approximately five-fold). The KD and Bmax values were found 2.6±0.5 nM and (2.6±0.1)×106, respectively. The tumor/muscle ratios for this radiotracer were determined 1.17±0.77, 1.15±0.32 and 2.65±0.32 at 1, 2 and 4 h after injection, respectively. Presaturation of HER2 receptors in SKOV-3 xenografted nude mice showed a reduction in the tumor/muscle ratio confirming in vivo specificity of the peptide. According to SPECT imaging, the tumor was visualized in mouse after 4 h postinjection of radiolabeled peptide. 99mTc-HYNIC-(Tricine)-(Ser)3-LTVPWY peptide exhibited overexpressed HER2 tumor targeting.
-
99m Tc-HYNIC-(Tricine/EDDA)-FROP peptide for MCF-7 breast tumor targeting and imaging
Journal of Biomedical Science, 2018Co-Authors: Sajjad Ahmadpour, Seyed Mohammad Abedi, Zohreh Noaparast, Seyed Jalal HosseinimehrAbstract:Breast cancer is the most common malignancy among women in the world. Development of novel tumor-specific radiopharmaceuticals for early breast tumor diagnosis is highly desirable. In this study we developed 99mTc-HYNIC-(Tricine/EDDA)-Lys-FROP peptide with the ability of specific binding to MCF-7 breast tumor. The FROP-1 peptide was conjugated with the bifunctional chelator hydrazinonicotinamide (HYNIC) and labeled with 99mTc using Tricine/EDDA co-ligand. The cellular specific binding of 99mTc-HYNIC-FROP was evaluated on different cell lines as well as with blocking experiment on MCF-7 (human breast adenocarcinoma). The tumor targeting and imaging of this labeled peptide were performed on MCF-7 tumor bearing mice. Radiochemical purity for 99mTc-HYNIC-(Tricine/EDDA)-FROP was 99% which was determined with ITLC method. This radiolabeled peptide showed high stability in normal saline and serum about 98% which was monitored with HPLC method. In saturation binding experiments, the binding constant (Kd) to MCF-7 cells was determined to be 158 nM. Biodistribution results revealed that the 99mTc-HYNIC-FROP was mainly exerted from urinary route. The maximum tumor uptake was found after 30 min post injection (p.i.); however maximum tumor/muscle ratio was seen at 15 min p.i. The tumor uptake of this labeled peptide was specific and blocked by co-injection of excess FROP. According to the planar gamma imaging result, tumor was clearly visible due to the tumor uptake of 99mTc-HYNIC-(Tricine/EDDA)-FROP in mouse after 15 min p.i. The 99mTc-HYNIC-(Tricine/EDDA)-FROP is considered a promising probe with high specific binding to MCF-7 breast cancer cells.
-
99m tc hynic Tricine edda frop peptide for mcf 7 breast tumor targeting and imaging
Journal of Biomedical Science, 2018Co-Authors: Sajjad Ahmadpour, Seyed Mohammad Abedi, Zohreh Noaparast, Seyed Jalal HosseinimehrAbstract:Breast cancer is the most common malignancy among women in the world. Development of novel tumor-specific radiopharmaceuticals for early breast tumor diagnosis is highly desirable. In this study we developed 99mTc-HYNIC-(Tricine/EDDA)-Lys-FROP peptide with the ability of specific binding to MCF-7 breast tumor. The FROP-1 peptide was conjugated with the bifunctional chelator hydrazinonicotinamide (HYNIC) and labeled with 99mTc using Tricine/EDDA co-ligand. The cellular specific binding of 99mTc-HYNIC-FROP was evaluated on different cell lines as well as with blocking experiment on MCF-7 (human breast adenocarcinoma). The tumor targeting and imaging of this labeled peptide were performed on MCF-7 tumor bearing mice. Radiochemical purity for 99mTc-HYNIC-(Tricine/EDDA)-FROP was 99% which was determined with ITLC method. This radiolabeled peptide showed high stability in normal saline and serum about 98% which was monitored with HPLC method. In saturation binding experiments, the binding constant (Kd) to MCF-7 cells was determined to be 158 nM. Biodistribution results revealed that the 99mTc-HYNIC-FROP was mainly exerted from urinary route. The maximum tumor uptake was found after 30 min post injection (p.i.); however maximum tumor/muscle ratio was seen at 15 min p.i. The tumor uptake of this labeled peptide was specific and blocked by co-injection of excess FROP. According to the planar gamma imaging result, tumor was clearly visible due to the tumor uptake of 99mTc-HYNIC-(Tricine/EDDA)-FROP in mouse after 15 min p.i. The 99mTc-HYNIC-(Tricine/EDDA)-FROP is considered a promising probe with high specific binding to MCF-7 breast cancer cells.
-
an improved 99mtc hynic ser 3 ltvspwy peptide with edda Tricine as co ligands for targeting and imaging of her2 overexpression tumor
European Journal of Medicinal Chemistry, 2018Co-Authors: Fatemeh Khodadust, Seyed Mohammad Abedi, Sajjad Ahmadpour, Nazan Aligholikhamseh, Seyed Jalal HosseinimehrAbstract:Abstract Overexpression of human epidermal receptor 2 (HER2) has given the opportunity for targeting and delivering of imaging radiotracers. The aim of this study was to evaluate the 99mTc-HYNIC-(EDDA/Tricine)-(Ser)3-LTVSPWY peptide for tumor targeting and imaging of tumor with overexpression of HER2. The HYNIC-(Ser)3-LTVSPWY was labeled with 99mTc in presence of EDDA/Tricine mixture as co-ligands. The in vitro and in vivo studies of this radiolabeled peptide were performed for cellular specific binding and tumor targeting. The high radiochemical purity of 99mTc-HYNIC (EDDA/Tricine)-(Ser)3-LTVSPWY was obtained to be 99%. It exhibited high stability in normal saline and human serum. In HER2 binding affinity study, a significant reduction in uptake of radiolabeled peptide (7.7 fold) was observed by blocking SKOV-3 cells receptors with unlabeled peptide. The KD and Bmax values for this radiolabeled peptide were determined as 3.3 ± 1.0 nM and 2.9 ± 0.3 × 106 CPM/pMol, respectively. Biodistribution study revealed tumor to blood and tumor to muscle ratios about 6.9 and 4 respectively after 4 h. Tumor imaging by gamma camera demonstrated considerable high contrast tumor uptake. This developed 99mTc-HYNIC-(Ser)3-LTVSPWY peptide selectively targeted on HER2 tumor and exhibited a high target uptake combined with acceptable low background activity for tumor imaging in mice. The results of this study and its comparison with another study showed that 99mTc-HYNIC-(EDDA/Tricine)-(Ser)3-LTVSPWY is much better than previously reported radiolabeled peptide as 99mTc-CSSS-LTVSPWY for HER2 overexpression tumor targeting and imaging.
Yumin Zheng - One of the best experts on this subject based on the ideXlab platform.
-
Protease activated receptor-1 targeted 99Tcm-(HYNIC-BMS-200261)(Tricine)(TPPTS) imaging on nude mice bearing human breast cancer
Chinese Journal of Nuclear Medicine and Molecular Imaging, 2018Co-Authors: Jie Liu, Xiaojian Liu, Chaoling Jin, Meng Wang, Wei Fang, Haojie Dai, Jue Yan, Yumin ZhengAbstract:Objective To study the reliability of 99Tcm-(hydrazinonicotinamide (HYNIC)-BMS-200261)(Tricine)(trisodium triphenylphosphine-3, 3′, 3″-trisulfonate (TPPTS)) as a radiotracer for protease activated receptor-1 (PAR-1) expression in breast cancer. Methods Fifteen nude mice bearing MDA-MB-435, MDA-MB-231 and MCF-7 human breast cancer xenografts (5 mice for each cell line) with different PAR-1 expression were used for 99Tcm-(HYNIC-BMS-200261)(Tricine)(TPPTS) γ imaging, and tumor/non-tumor (T/NT) ratios were obtained with region of interest (ROI) technique. Afterwards, the biodistribution of 99Tcm-(HYNIC-BMS-200261)(Tricine)(TPPTS) was analyzed in tumor-bearing nude mice, and the radioactivity in tumor (percentage activity of injection dose per gram of tissue, %ID/g) was calculated. The immunostaining was performed to examine PAR-1 expression in tumor tissue and semi-quantitative analysis was used. One-way analysis of variance and Pearson correlation analysis were used to analyze data. Results At 2 h postinjection, the T/NT ratios were 3.03±0.32, 2.27±0.25 and 1.51±0.13 respectively in nude mice bearing MDA-MB-435, MDA-MB-231 and MCF-7 xenografts; the tumor uptakes of 99Tcm-(HYNIC-BMS-200261)(Tricine)(TPPTS) were (1.03±0.15), (0.56±0.14) and (0.30±0.06) %ID/g; PAR-1 expression levels were (17.22±2.71)%, (10.78±1.95)% and (2.80±1.18)%, respectively (F values: 47.66, 46.36, 62.35, all P
-
protease activated receptor 1 targeted 99tcm hynic bms 200261 Tricine tppts imaging on nude mice bearing human breast cancer
Chinese Journal of Nuclear Medicine and Molecular Imaging, 2018Co-Authors: Jie Liu, Xiaojian Liu, Chaoling Jin, Meng Wang, Wei Fang, Haojie Dai, Jue Yan, Yumin ZhengAbstract:Objective To study the reliability of 99Tcm-(hydrazinonicotinamide (HYNIC)-BMS-200261)(Tricine)(trisodium triphenylphosphine-3, 3′, 3″-trisulfonate (TPPTS)) as a radiotracer for protease activated receptor-1 (PAR-1) expression in breast cancer. Methods Fifteen nude mice bearing MDA-MB-435, MDA-MB-231 and MCF-7 human breast cancer xenografts (5 mice for each cell line) with different PAR-1 expression were used for 99Tcm-(HYNIC-BMS-200261)(Tricine)(TPPTS) γ imaging, and tumor/non-tumor (T/NT) ratios were obtained with region of interest (ROI) technique. Afterwards, the biodistribution of 99Tcm-(HYNIC-BMS-200261)(Tricine)(TPPTS) was analyzed in tumor-bearing nude mice, and the radioactivity in tumor (percentage activity of injection dose per gram of tissue, %ID/g) was calculated. The immunostaining was performed to examine PAR-1 expression in tumor tissue and semi-quantitative analysis was used. One-way analysis of variance and Pearson correlation analysis were used to analyze data. Results At 2 h postinjection, the T/NT ratios were 3.03±0.32, 2.27±0.25 and 1.51±0.13 respectively in nude mice bearing MDA-MB-435, MDA-MB-231 and MCF-7 xenografts; the tumor uptakes of 99Tcm-(HYNIC-BMS-200261)(Tricine)(TPPTS) were (1.03±0.15), (0.56±0.14) and (0.30±0.06) %ID/g; PAR-1 expression levels were (17.22±2.71)%, (10.78±1.95)% and (2.80±1.18)%, respectively (F values: 47.66, 46.36, 62.35, all P<0.05). The T/NT ratios and tumor uptake of 99Tcm-(HYNIC-BMS-200261)(Tricine)(TPPTS) at 2 h post-injection were correlated with PAR-1 expression (r values: 0.934 and 0.929, both P<0.05). Conclusions 99Tcm-(HYNIC-BMS-200261)(Tricine)(TPPTS) imaging could be a noninvasive and effective method for monitoring PAR-1 expression in human breast cancer. Key words: Breast neoplasms; Receptors, proteinase-activated; Antistatic agents; Radionuclide imaging; Tumor cells, cultured; Mice, nude
-
Preparation of 99Tcm-(HYNIC-BMS-200261)(Tricine)(TPPTS) and its biodistribution and preliminary imaging study in nude mice bearing human breast cancer
Chinese Journal of Nuclear Medicine and Molecular Imaging, 2016Co-Authors: Xiaojian Liu, Jie Liu, Chaoling Jin, Meng Wang, Wei Fang, Haojie Dai, Jue Yan, Yumin ZhengAbstract:Objective To synthesize 99Tcm-(HYNIC-BMS-200261)(Tricine)(trisodium triphenylphosphine-3, 3', 3″-trisulfonate)(99Tcm-(HYNIC-BMS-200261)(Tricine)(TPPTS)) and evaluate its biodistribution and feasibility of imaging in nude mice bearing human breast cancer xenografts. Methods HYNIC was conjugated to BMS-200261, then Tricine and TPPTS were used as coligands for 99Tcm-labeling. The radiochemical purity and stability of 99Tcm-(HYNIC-BMS-200261) (Tricine) (TPPTS) were measured with HPLC. Biodistribution in normal mice and imaging in nude mice bearing MDA-MB-435 breast cancer xenografts were performed respectively. Results The radiochemical purity of 99Tcm-(HYNIC-BMS-200261)(Tricine)(TPPTS) was over 90%, and remained over 85% after 4 h at room temperature. The biodistribution data in normal mice showed a rapid clearance from blood. The tracer uptake of blood was (0.08±0.02) %ID/g at 2 h postinjection. 99Tcm-(HYNIC-BMS-200261)(Tricine)(TPPTS) was excreted mainly via the liver and kidneys. There was little radioactivity accumulation in gastrointestinal tract. The tracer uptake of spleen, stomach and small intestine were (0.35±0.13), (0.27±0.11) and (0.25±0.07) %ID/g at 2 h postinjection. Gamma imaging showed the tumor tissue uptake was remarkable at 30 min postinjection, with the maximum T/NT ratio of 3.40±0.30 at 1 h postinjection. Conclusions 99Tcm-(HYNIC-BMS-200261)(Tricine) (TPPTS) may be easily prepared with high radiochemical purity and stability. The imaging results and biodistribution characteristics suggest it may be promising for the detection of breast cancer. Key words: (HYNIC-BMS-200261)(Tricine)-(TPPTS); Istope labeling; Technetium; Radionuclide imaging; Breast neoplasms; Mice
Fatemeh Khodadust - One of the best experts on this subject based on the ideXlab platform.
-
99mTc-HYNIC-(Ser)3-LTVPWY peptide bearing Tricine as co-ligand for targeting and imaging of HER2 overexpression tumor
Radiochimica Acta, 2018Co-Authors: Nazan Aligholikhamseh, Seyed Mohammad Abedi, Sajjad Ahmadpour, Fatemeh Khodadust, Seyed Jalal HosseinimehrAbstract:Abstract Human epidermal growth factor receptor 2 (HER2) is overexpressed in several cancers. Today’s tumor targeting is receiving more attention due to its specificity to target receptor-dependent cancers. The aim of this study was to evaluate the 99mTc-HYNIC-(Tricine)-(Ser)3-LTVPWY peptide for tumor targeting and imaging with overexpression of HER2. HYNIC-(Ser)3-LTVPWY peptide was labeled with 99mTc using Tricine as a co-ligand at room temperature. Specific binding of this radiolabeled peptide was assessed on four cancer cell lines with different levels of HER2 receptor expression. Also the affinity of 99mTc-HYNIC-(Tricine)-(Ser)3-LTVPWY peptide to the HER2 receptor was evaluated in the SKOV-3 cell line. Biodistribution study of this radiolabeled peptide was performed in SKOV-3 tumor bearing nude mice. The HYNIC conjugated peptide was simply labeled with 99mTc radionuclide with high labeling efficiency about 98±1% showing favorable stability in normal saline and human serum. In the presence of unlabeled peptide as competitor, the HER2 binding capacity of the radiolabeled peptide reduced (approximately five-fold). The KD and Bmax values were found 2.6±0.5 nM and (2.6±0.1)×106, respectively. The tumor/muscle ratios for this radiotracer were determined 1.17±0.77, 1.15±0.32 and 2.65±0.32 at 1, 2 and 4 h after injection, respectively. Presaturation of HER2 receptors in SKOV-3 xenografted nude mice showed a reduction in the tumor/muscle ratio confirming in vivo specificity of the peptide. According to SPECT imaging, the tumor was visualized in mouse after 4 h postinjection of radiolabeled peptide. 99mTc-HYNIC-(Tricine)-(Ser)3-LTVPWY peptide exhibited overexpressed HER2 tumor targeting.
-
an improved 99mtc hynic ser 3 ltvspwy peptide with edda Tricine as co ligands for targeting and imaging of her2 overexpression tumor
European Journal of Medicinal Chemistry, 2018Co-Authors: Fatemeh Khodadust, Seyed Mohammad Abedi, Sajjad Ahmadpour, Nazan Aligholikhamseh, Seyed Jalal HosseinimehrAbstract:Abstract Overexpression of human epidermal receptor 2 (HER2) has given the opportunity for targeting and delivering of imaging radiotracers. The aim of this study was to evaluate the 99mTc-HYNIC-(EDDA/Tricine)-(Ser)3-LTVSPWY peptide for tumor targeting and imaging of tumor with overexpression of HER2. The HYNIC-(Ser)3-LTVSPWY was labeled with 99mTc in presence of EDDA/Tricine mixture as co-ligands. The in vitro and in vivo studies of this radiolabeled peptide were performed for cellular specific binding and tumor targeting. The high radiochemical purity of 99mTc-HYNIC (EDDA/Tricine)-(Ser)3-LTVSPWY was obtained to be 99%. It exhibited high stability in normal saline and human serum. In HER2 binding affinity study, a significant reduction in uptake of radiolabeled peptide (7.7 fold) was observed by blocking SKOV-3 cells receptors with unlabeled peptide. The KD and Bmax values for this radiolabeled peptide were determined as 3.3 ± 1.0 nM and 2.9 ± 0.3 × 106 CPM/pMol, respectively. Biodistribution study revealed tumor to blood and tumor to muscle ratios about 6.9 and 4 respectively after 4 h. Tumor imaging by gamma camera demonstrated considerable high contrast tumor uptake. This developed 99mTc-HYNIC-(Ser)3-LTVSPWY peptide selectively targeted on HER2 tumor and exhibited a high target uptake combined with acceptable low background activity for tumor imaging in mice. The results of this study and its comparison with another study showed that 99mTc-HYNIC-(EDDA/Tricine)-(Ser)3-LTVSPWY is much better than previously reported radiolabeled peptide as 99mTc-CSSS-LTVSPWY for HER2 overexpression tumor targeting and imaging.
-
An improved 99mTc-HYNIC-(Ser)3-LTVSPWY peptide with EDDA/Tricine as co-ligands for targeting and imaging of HER2 overexpression tumor.
European Journal of Medicinal Chemistry, 2017Co-Authors: Fatemeh Khodadust, Seyed Mohammad Abedi, Sajjad Ahmadpour, Nazan Aligholikhamseh, Seyed Jalal HosseinimehrAbstract:Abstract Overexpression of human epidermal receptor 2 (HER2) has given the opportunity for targeting and delivering of imaging radiotracers. The aim of this study was to evaluate the 99mTc-HYNIC-(EDDA/Tricine)-(Ser)3-LTVSPWY peptide for tumor targeting and imaging of tumor with overexpression of HER2. The HYNIC-(Ser)3-LTVSPWY was labeled with 99mTc in presence of EDDA/Tricine mixture as co-ligands. The in vitro and in vivo studies of this radiolabeled peptide were performed for cellular specific binding and tumor targeting. The high radiochemical purity of 99mTc-HYNIC (EDDA/Tricine)-(Ser)3-LTVSPWY was obtained to be 99%. It exhibited high stability in normal saline and human serum. In HER2 binding affinity study, a significant reduction in uptake of radiolabeled peptide (7.7 fold) was observed by blocking SKOV-3 cells receptors with unlabeled peptide. The KD and Bmax values for this radiolabeled peptide were determined as 3.3 ± 1.0 nM and 2.9 ± 0.3 × 106 CPM/pMol, respectively. Biodistribution study revealed tumor to blood and tumor to muscle ratios about 6.9 and 4 respectively after 4 h. Tumor imaging by gamma camera demonstrated considerable high contrast tumor uptake. This developed 99mTc-HYNIC-(Ser)3-LTVSPWY peptide selectively targeted on HER2 tumor and exhibited a high target uptake combined with acceptable low background activity for tumor imaging in mice. The results of this study and its comparison with another study showed that 99mTc-HYNIC-(EDDA/Tricine)-(Ser)3-LTVSPWY is much better than previously reported radiolabeled peptide as 99mTc-CSSS-LTVSPWY for HER2 overexpression tumor targeting and imaging.
