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In an effort to seek novel agents targeting prostate-specific membrane antigen (PSMA), sixteen ligands (L1-L16) with structural modifications in S1' binding pocket were synthesized and evaluated for PSMA inhibition. (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. Computational docking was performed to study the binding mode of the two most potent ligands discovered. FITC-conjugated L14 could selectively stain PSMA+ LNCaP cells over PSMA- PC3 cells. IRDye800CW conjugated L16 can effectively image tumors in a murine xenograft model of prostate cancer.
This article was published in the following journal.
Name: Journal of medicinal chemistry
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Diagnostic study which evaluates the level of PSMA expression in patients with locally advanced, recurrent and/or metastatic ACC/SDC of ≥18 years old with 68Ga-PSMA-PET/CT imaging in ord...
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A polyester used for absorbable sutures & surgical mesh, especially in ophthalmic surgery. 2-Hydroxy-propanoic acid polymer with polymerized hydroxyacetic acid, which forms 3,6-dimethyl-1,4-dioxane-dione polymer with 1,4-dioxane-2,5-dione copolymer of molecular weight about 80,000 daltons.
A cytoplasmic receptor and peroxin that contains a series of TETRACOTIPEPTIDE REPEATS and binds to PEROXISOME TARGETING SIGNAL 1 (SKL-type). It is essential for protein import into PEROXISOMES; mutations in the PEX5 gene are associated with PEROXISOMAL DISORDERS such as ZELLWEGER SYNDROME.
A cytoplasmic receptor and peroxin that contains a series of WD40 REPEATS and binds to PEROXISOME TARGETING SIGNAL 2. It is essential for protein import into PEROXISOMES; mutations in the human PEX7 gene are associated with PEROXISOMAL DISORDERS such as Type 1 CHONDRODYSPLASIA PUNCTATA, RHIZOMELIC.
A dioxygenase and alkylation repair homolog that catalyzes the methylation of 5-carboxymethyl URIDINE to 5-methylcarboxymethyl uridine at the wobble position of the ANTICODON loop in TRANSFER RNA (tRNA) via its methyltransferase domain. It has a preference for tRNA (ARGININE) and tRNA (GLUTAMATE), and does not bind tRNA (LYSINE).
Endogenously produced lipid-soluble gaseous molecules which function as neurotransmitters and signal mediators targeting ION CHANNELS and transporters.
Bladder Cancer Brain Cancer Breast Cancer Cancer Cervical Cancer Colorectal Head & Neck Cancers Hodgkin Lymphoma Leukemia Lung Cancer Melanoma Myeloma Ovarian Cancer Pancreatic Cancer ...
Benign Prostatic Hyperplasia (BPH)
An enlarged prostate (benign prostatic enlargement (BPE) or benign prostatic hyperplasia (BPH)) is common in men after the age of about 50. Having an enlarged prostate does not mean you have cancer. In some cases, an enlarged prostate can cause the ...
Prostate cancer (cancer de prostata) Prostate cancer (cancer de prostata) is a form of cancer that develops in the prostate, a gland in the male reproductive system. Most prostate cancers are slow growing; however, there are cases of aggressive prostat...