Design of remarkably simple, yet potent urea-based inhibitors of glutamate carboxypeptidase II (NAALADase).

  title={Design of remarkably simple, yet potent urea-based inhibitors of glutamate carboxypeptidase II (NAALADase).},
  author={A. Kozikowski and F. Nan and P. Conti and J. Zhang and E. Ramadan and T. Bzdȩga and B. Wr{\'o}blewska and J. Neale and S. Pshenichkin and J. Wroblewski},
  journal={Journal of medicinal chemistry},
  volume={44 3},
Imaging and therapeutic radiotracers for prostate cancer
Synthesis and evaluation of [64Cu]PSMA-617 targeted for prostate-specific membrane antigen in prostate cancer.
Although this radioligand shows slow clearance for kidney and high liver uptake, change of its chelator moiety and easy radiolabeling may enable development of new 64Cu or 67Cu-labeled PSMA ligands for imaging and radiotherapy. Expand
A targeted near-infrared nanoprobe for deep-tissue penetration and imaging of prostate cancer.
A deep-tissue imaging NIR nanoprobe targeting prostatic lesions that binds to PSMA+ tumour with sub-nanomolar affinity and high specificity, shows an excellent safety profile in primary cell lines in vitro and shows high penetrative capacity in a 3D prostate tumour model. Expand
Dipeptide Inhibitors of the Prostate Specific Membrane Antigen (PSMA): A Comparison of Urea and Thiourea Derivatives.
It is hypothesized that substituting the zinc-coordinating urea group for a thiourea group, thus incorporating a sulfur atom, could facilitate stronger binding to zinc(II) within the active site, and thus improve affinity for GCP(II)/PSMA. Expand
Inhibitors of prostate-specific membrane antigen in the diagnosis and therapy of metastatic prostate cancer – a review of patent literature
Most PSMA-targeted agents are based on the Lys-UREa-Glu or Glu-urea-glu structure, demonstrate strong PSMA -binding affinity in nanomolar range, and achieve diverse structural modifications in the non-pharmacophore pocket. Expand
PSMA-Targeting Radiopharmaceuticals for Prostate Cancer Therapy: Recent Developments and Future Perspectives
Simple Summary One of the most frequently diagnosed cancer in men is adenocarcinoma of the prostate. Once the disease is metastatic, only very limited treatment options are available, resulting in aExpand
Targeted delivery of cytotoxic proteins to prostate cancer via conjugation to small molecule urea-based PSMA inhibitors
It is demonstrated that urea-based PSMA inhibitors represent a simpler, less expensive alternative to antibodies as a means to deliver cytotoxic proteins to prostate cancer cells. Expand
The Role of Theranostics in Prostate Cancer.
The current status of theranostics in prostate cancer is reviewed, discussing the challenges and opportunities of combination therapies with more conventional agents such as androgen receptor inhibitors, cytotoxic chemotherapy, and immunotherapy. Expand
(S)-3-(Carboxyformamido)-2-(3-(carboxymethyl)ureido)propanoic Acid as A Novel PSMA Targeting Scaffold for Prostate Cancer Imaging.
(S)-3-(Carboxyformamido)-2-(3-(carboxymethyl)ureido) propanoic acids proved potent PSMA ligands with Ki values ranging from 0.08 nM - 8.98 nM, which are in the range of or are higher in potency compared to previously published Glu-Urea-based ligands. Expand
Bivalent Inhibitors of Prostate-Specific Membrane Antigen Conjugated to Desferrioxamine B Squaramide Labeled with Zirconium-89 or Gallium-68 for Diagnostic Imaging of Prostate Cancer.
The ligands presented here, which can be labeled with either gallium-68 or zirconium-89, have the potential to increase the number of clinical sites that can perform diagnostic PET imaging. Expand