Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: EC:3.4.17.21 (prostate-specific membrane antigen)
 1,761 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Animal toxicology and clinical phase I trial data have documented that the PSMA-activated thapsigargin drug, G202 is non-myelosuppressive. This lack of myelosuppression facilitates G202 combination with a variety of additional clinically approved drugs. For example, thapsigargin's ability to induce ER stress raises its potential for synergy when combined with radiation and cytotoxic chemotherapies. Finally, G202-based delivery of the thapsigargin analog causes marked reduction of expression of the androgen receptor (AR) in prostate cancer cells and the estrogen receptor (ER) protein in breast cancer. These results suggest that combination therapy with anti-androgen/estrogens and G202 could be synergistic against prostate and/or breast cancer. These combinatorial approaches are currently under pre-clinical evaluation in our laboratories.
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PMID:Engineering enzymatically activated "molecular grenades" for cancer. 2283 32

The immunophenotype of a normal testis and the excretory duct system has not been studied comprehensively in fetal and adult patients without testicular disease or hormonal manipulation so far. In addition, testicular (TA) and epididymal (EA) appendages are frequent paratesticular structures without previously reported comprehensive immunophenotypic studies. Immunohistochemistry for multiple markers, including the androgen receptor (AR), the estrogen receptor (ER), the progesterone receptor (PR), the prostate-specific antigen, the prostate-specific membrane antigen, PAX8, WT1, calretinin, CK7, CK20, OCT4, SALL4, and CD117, was performed on full sections of testicular/paratesticular tissue from a large cohort of adult and fetal autopsy patients. In contrast to adult germ cells (GC), fetal GC strongly express OCT4 and CD117, although the expression of these proteins is lost in the early postnatal period; SALL4, in contrast, is expressed in both fetal and adult GC, with only weak and focal expression in adult patients. Fetal Sertoli cells (SC) express WT1 and calretinin strongly and diffusely, in contrast to adult SC. Both fetal and adult excretory duct systems express CK7 and PAX8 with frequent AR coexpression, and all 3 main segments of the excretory duct system (ductuli efferentes, epididymis, and vas deferens) have unique immunophenotypes. The rete testis also has a unique immunohistochemical expression pattern, which includes strong expression of CK7, PAX8, WT1, calretinin, and AR. Finally, of the adult autopsy patients examined, 80% had a TA, and 60% had an EA; these paratesticular structures occurred at stereotypical locations, demonstrated reproducible morphologic features, and had a unique immunophenotype relative to other studied structures, with strong CK7, PAX8, WT1, AR, ER, and PR coexpression. The testis and the paratestis may be involved by diverse neoplastic and non-neoplastic processes, and knowledge of the immunophenotypic expression spectrum of these tissues may aid in clinical diagnosis and advance our understanding of the pathogenesis of both oncologic and nononcologic disease processes.
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PMID:Comprehensive Immunophenotypic Characterization of Adult and Fetal Testes, the Excretory Duct System, and Testicular and Epididymal Appendages. 2686 15

Noninvasive molecular imaging of cancer by means of the scintigraphic imaging modalities PET, PET/CT, and PET/MRI represents a powerful diagnostic tool in modern nuclear medicine. Radiotracers labeled with the prominent positron emitter fluorine-18 are routinely used to target and visualize discrete biological structures dysregulated in the progression of cancer. Such tracers are therefore capable of detecting oncological pathologies in vivo at the cellular and subcellular level in a timely manner and are thereby used for early detection of cancer as well as monitoring for treatment response. This chapter describes a variety of important 18F-labeled radiopharmaceuticals that are frequently used in oncological PET imaging. Small-molecule and low-molecular-weight radiotracers for the detection of glucose utilization, amino acid transport, protein synthesis, membrane lipid synthesis, cell proliferation, cell death, hypoxia, estrogen receptor status, prostate-specific membrane antigen (PSMA) expression, and bone mineralization of tumors are introduced. The structural properties, common radiochemical synthesis approaches as well as in vivo metabolism and accumulation mechanisms of the clinically most important 18F-labeled radiotracers are described.
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PMID:18F-Labeled Small-Molecule and Low-Molecular-Weight PET Tracers for the Noninvasive Detection of Cancer. 3259 90