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PSMA ligands bind prostate-specific membrane antigen (PSMA), a cell-surface glutamate carboxypeptidase. A complementary DNA encoding PSMA was cloned in 1993 from a human prostate carcinoma cell line. In 1996 the protein was shown to act as a hydrolase with the substrate and inhibitor profile of a neuropeptidase that cleaves N-acetylaspartylglutamate. The enzyme is also known as glutamate carboxypeptidase II and folate hydrolase 1 (FOLH1). Many compounds here carry a urea-linked glutamate motif that fits the active site, coupled to a chelator or labeling group. PSMA-11 carries a chelator for gallium-68, while PSMA-1007 and piflufolastat are fluorinated ligands. tert-Butyl-DCL is a protected inhibitor intermediate, and PSMA-ALB-56 adds an albumin-binding group.
Synonyms: PSMA-617; PSMA617 TFA; PSMA617 triflouroacetic acid salt
PSMA-617, also know as vipivotide tetraxetan. It is a ligand used to make 177Lu-PSMA-617, which is a radioactive molecule to fight cancer.
PSMA-1007 is a high-affinity ligand for the prostate-specific membrane antigen (PSMA). Labeled with 18F, this compound serves as an effective PET tracer for imaging prostate cancer, facilitating the detection and monitoring of malignancies. Additionally, PSMA-1007 is applicable in the synthesis and research of radionuclide-drug conjugates (RDCs), enhancing therapeutic strategies in oncology.
Flotufolastat is a prostate-specific membrane antigen (PSMA) modulator that serves as a radiodiagnostic agent for imaging prostate cancer. This compound is instrumental in enhancing the detection and characterization of prostate cancer lesions. Flotufolastat is valuable for research applications focused on prostate cancer and other malignancies associated with PSMA expression.
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PSMA binder-1 is a potent ligand targeting Prostate-Specific Membrane Antigen (PSMA). It facilitates the synthesis of PSMA-targeting molecules, such as Ac-PSMA-trillium, providing a valuable tool for research in prostate cancer diagnosis and therapy. This compound is essential for studies focused on imaging and targeted treatment strategies aimed at PSMA-expressing tumors.
PSMA-azide is a ligand targeting prostate-specific membrane antigen (PSMA). It effectively inhibits PSMA-dependent hydrolysis of N-acetylaspartylglutamic acid (NAAG) with an IC50 of 9 nM and a Ki of 1 nM, making it a valuable tool for studying PSMA-related pathways. Additionally, PSMA-azide features an azide moiety, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition reactions (CuAAc) with alkynyl-containing molecules, facilitating various biochemical labeling and conjugation applications in research.
Prostate Specific Antigen Substrate is a fluorescent substrate utilized for the detection of enzymatic activity associated with prostate specific antigen (PSA). This reagent enables researchers to effectively measure PSA activity, aiding in the study of prostate cancer and other related conditions. Its application in various assays facilitates enhanced understanding of PSA's role in oncology research.
Synonyms: LY4181530; PSMA-62
PNT2001 is a potent prostate-specific membrane antigen (PSMA) ligand, exhibiting an IC50 of 3.1 nM. This compound enhances cellular internalization, making it a valuable tool for targeting PSMA in prostate cancer research. Additionally, PNT2001 can be labeled with 177Lu and 225Ac, facilitating the development of radiolabeled therapies for prostate cancer treatment and diagnostic applications.
PSMA binder-2 is a potent ligand targeting Prostate-Specific Membrane Antigen (PSMA), facilitating the synthesis of Ac-PSMA-trillium, which exhibits enhanced binding and pharmacokinetic properties. This versatile compound can be modified with various radioactive isotopes for different applications; when labeled with 111In, it serves effectively as a DOTA chelating and imaging agent. Alternatively, when conjugated with 225Ac, it acts as a Macropa chelator, proving valuable for targeted radionuclide therapy (TRT) in the research of metastatic castration-resistant prostate cancer (mCRPC).
PSMA Ligand 1 is a potent PSMA ligand that exhibits an IC50 of 26.74 nM. This compound has been radiolabeled with [18F], making it a suitable candidate for use as a PET tracer in imaging studies. Its primary applications include aiding in the diagnosis and monitoring of prostate cancer, facilitating innovative research in oncology and molecular imaging.
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Synonyms: PSMA-DOTA-PEI2
PDI2 (PSMA-DOTA-PEI2) is a prostate-specific membrane antigen (PSMA) ligand that functions as a tumor retention agent and imaging agent while reducing renal uptake. It selectively binds to PSMA on prostate cancer cells, facilitating entry through clathrin-dependent endocytosis, which results in increased tumor retention and decreased renal accumulation. PDI2 is valuable for research in prostate cancer and castration-resistant metastatic prostate cancer, particularly in the context of SPECT diagnostic imaging and radiotheranostics.
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PSMA Ligand 3 is a ligand specifically targeting Prostate-Specific Membrane Antigen (PSMA). Its primary function is to bind to PSMA, facilitating the detection and imaging of prostate cancer cells. This compound is valuable in cancer research, particularly in the study of prostate cancer diagnostics and therapy.
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PSMA binder-3 is a selective binder for Prostate-Specific Membrane Antigen (PSMA), a key target in prostate cancer research. This high-affinity ligand exhibits strong binding capabilities that facilitate the study of PSMA's role in tumor biology and therapeutic targeting. It is an essential tool for applications in imaging and drug development related to prostate cancer.
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Synonyms: Felivotide mopaxetan
PSMA-trillium is a PSMA-targeting compound that features a PSMA binder, a Macropa chelating molecule, and a pharmacokinetics modifier. This non-radioactive derivative of Actinium-225-PSMA-Trillium (BAY 3563254) offers enhanced PSMA targeting and optimized pharmacokinetic properties. PSMA-trillium effectively binds to Ac via the Macropa chelator and serves as a potent inhibitor of metastatic castration-resistant prostate cancer (mCRPC). It is a valuable tool for research into targeted therapies for prostate cancer.
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PSMA-N5 is a potent PSMA ligand, exhibiting a Ki value of 0.71 nM. This compound serves as a PET radiotracer specifically for imaging prostate cancer, facilitating the visualization of tumors. PSMA-N5 is valuable for research applications in prostate cancer and other malignancies associated with prostate-specific membrane antigen.
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PSMA-MAL-5 is a prostate-specific membrane antigen (PSMA) ligand that covalently binds to Cys466 of the PSMA protein. This compound demonstrates significant biological activity, including high radiostability and tumor uptake when labeled with 177Lu and 225Ac. PSMA-MAL-5 is also effective in inhibiting tumor growth, making it suitable for applications in SPECT/CT imaging and radionuclide therapy for prostate cancer.
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