scholarly journals Structure–Activity Relationship of18F-Labeled Phosphoramidate Peptidomimetic Prostate-Specific Membrane Antigen (PSMA)-Targeted Inhibitor Analogues for PET Imaging of Prostate Cancer

2016 ◽  
Vol 59 (12) ◽  
pp. 5684-5694 ◽  
Author(s):  
Shorouk Dannoon ◽  
Tanushree Ganguly ◽  
Hendry Cahaya ◽  
Jonathan J. Geruntho ◽  
Matthew S. Galliher ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Pet Imaging ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Prostate Specific Membrane Antigen ◽  
Structure Activity ◽  
Specific Membrane

scholarly journals Prostate-specific membrane antigen and fibroblast activation protein distribution in prostate cancer: preliminary data on immunohistochemistry and PET imaging

2021 ◽  
Author(s):  
Katharina Kessel ◽  
Robert Seifert ◽  
Matthias Weckesser ◽  
Martin Boegemann ◽  
Sebastian Huss ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Lymph Node ◽  
Pet Imaging ◽  
Fibroblast Activation Protein ◽  
Prostate Specific Membrane Antigen ◽  
Psma Pet ◽  
Node Metastases ◽  
Small Patient ◽  
Specific Membrane ◽  
Psma Expression

Abstract Introduction Fibroblast activation protein (FAP) has been recently presented as new imaging target for malignant diseases and offers high contrast to surrounding normal tissue. FAP tracer uptake has been reported in various tumor entities. The aim of this study was to compare FAP and Prostate-specific membrane antigen (PSMA) expression in primary prostate cancer employing histological analyses and PET imaging in two small patient collectives. Methods Two independent small patient collectives were included in this study. For cohort A, data of 5 prostate cancer patients and 3 patients with benign prostate hyperplasia were included. Patients with prostate cancer were initially referred for PSMA PET staging. Radical prostatectomy was performed in all patients and prostate specimen of patients and biopsies of healthy controls were available for further evaluation. Histological workup included HE and immunohistochemistry using PSMA Ab, FAP Ab. Cohort B consists of 6 Patients with diagnosed mCRPC and available PSMA as well as FAP PET. Results Patients with proven prostate cancer infiltration exhibited strong positivity for PSMA in both primary tumors and lymph node metastases while stainings for FAP were found positive in some cases, but not all (2/5). Controls with BPH presented moderate PSMA staining and in one case also with a positive FAP staining (1/3). PET imaging with FAP seemed to result in more precise results in case of low PSMA expression than PSMA-PET. Conclusions While PSMA staining intensity is a valid indicator of prostate cancer in both primary tumor and lymph node metastases, the expression of FAP seems to be heterogeneous but not necessarily linked to cancer-associated fibroblasts. It is also present in inflammation-associated myofibroblasts. Therefore, its ultimate role in prostate cancer diagnosis remains a subject of discussion.

3D-QSAR and Molecular Docking Studies on Design Anti-Prostate Cancer Curcumin Analogues

2020 ◽  
Vol 16 (3) ◽  
pp. 245-256 ◽  
Author(s):  
Xi Meng ◽  
Lianhua Cui ◽  
Fucheng Song ◽  
Mingyuan Luan ◽  
Junjie Ji ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Biological Activity ◽  
Molecular Docking ◽  
Correlation Coefficient ◽  
Structure Activity Relationship ◽  
Docking Studies ◽  
Activity Relationship ◽  
Molecular Docking Studies ◽  
Curcumin Analogs ◽  
Structure Activity

Background: Prostate cancer is one of the most common tumors in the world and the fifth leading cause of male cancer death. Although the treatment of localized androgen-dependent prostate cancer has been successful, the efficacy of androgen-independent metastatic disease is limited. Curcumin, a natural product, has been found to inhibit the proliferation of prostate cancer cells. Objective: To design curcumin analogs with higher biological activity and lower toxicity and side effects for the treatment of prostate cancer. Methods: In this study, the three dimensional-quantitative structure activity relationship (3DQSAR) and molecular docking studies were performed on 34 curcumin analogs as anti-prostate cancer compounds. We introduced OSIRIS Property Explorer to predict drug-related properties of newly designed compounds. Results: The optimum CoMSIA model exhibited statistically significant results: the cross-validated correlation coefficient q2 is 0.540 and non-cross-validated R2 value is 0.984. The external predictive correlation coefficient Rext 2 is 0.792. The information of structure-activity relationship can be obtained from the CoMSIA contour maps. In addition, the molecular docking study of the compounds for 3ZK6 as the protein target revealed important interactions between active compounds and amino acids. Conclusion: Compound 28i may be a new type of anti-prostate cancer drug with higher biological activity and more promising development.

scholarly journals Initial Evaluation of [18F]DCFPyL for Prostate-Specific Membrane Antigen (PSMA)-Targeted PET Imaging of Prostate Cancer

2015 ◽  
Vol 17 (4) ◽  
pp. 565-574 ◽  
Author(s):  
Zsolt Szabo ◽  
Esther Mena ◽  
Steven P. Rowe ◽  
Donika Plyku ◽  
Rosa Nidal ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Pet Imaging ◽  
Initial Evaluation ◽  
Prostate Specific Membrane Antigen ◽  
Specific Membrane

scholarly journals Imaging standardization systems for hybrid PET imaging of prostate cancer with radiolabeled prostate-specific membrane antigen ligands: comparative review of PROMISE and PSMA-RADS version 1.0

2019 ◽  
pp. 90-99
Author(s):  
A. V. Leontyev ◽  
N. A. Rubtsova ◽  
A. I. Khalimon ◽  
M. T. Kuliev ◽  
I. V. Pylova ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Pet Imaging ◽  
Prostate Specific Membrane Antigen ◽  
Advantages And Disadvantages ◽  
Comparative Review ◽  
Two Systems ◽  
Specific Membrane

This article provides a comparative review of two systems for standardized evaluation of the results of hybrid PET imaging with radiolabeled PSMA ligands – PROMISE and PSMA-RADS version 1.0. The principles of classification, nomenclature and evaluation algorithms, as well as recommendations for structuring research and conclusion protocols, highlighting the advantages and disadvantages of the proposed systems, are considered in detail.

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