Gene/Protein
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Symptom
Drug
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Compound
Pivot Concepts:
Gene/Protein
Disease
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Target Concepts:
Gene/Protein
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Query: UMLS:C0267964 (
PAA
)
2,561
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
The in vitro cytotoxic activity profile of nine novel phenylarsonic acid (CAS 98-05-5,
PAA
) compounds against 17 human cancer cell lines including (a) ovarian cancer cell lines ES-2, PA-1, CAOV-3, OVCAR-3, (b) testicular cancer cell lines Ntera-2, Tera-2, N2NICP, 833K, and 64CP, (c) multiple myeloma cell lines ARH77, HS-Sultan, RPMI-8226, and U266, and (d) acute lymphoblastic leukemia (ALL) cell lines NALM-6, MOLT-3, ALL-1, and RS4; 11, was determined by the MTT assay. The lead compounds, 2-methylthio-4-[(4'-aminophenylazo)-phenylarsonic acid] pyrimidine (PHI-370) and 2-methylthio-4-(4'-phenylarsonic acid)-aminopyrimidine (PHI-380) caused apoptotic death in all 17 cancer cell lines at low micromolar concentrations, as documented by TUNEL assays and confocal laser scanning microscopy. PHI-380 was also tested and found to be very active against primary tumor cells isolated from surgical biopsy specimens of 14 patients with therapy-refractory non-small cell lung cancer, breast cancer, colon cancer,
lymphoma
, hepatoblastoma, or Wilm's tumor as well. Because of their broad-spectrum and potent anticancer activity and ability to induce apoptosis in primary tumor cells from therapy-refractory cancer patients,
PAA
compounds such as PHI-370 and PHI-380 may provide the basis for effective salvage regimens for patients with recurrent cancer.
...
PMID:Phenylarsonic acid compounds with broad-spectrum and potent cytotoxic activity against human cancer cells. 1287 14
Polyacrylamide glycoconjugates, Glyc-
PAA
, having various tags or labels are convenient tools for analysis of cellular lectins. Adaptation of such glycoprobes for flow cytometry allows us to reveal lectins expressed on cell surface and analyze their carbohydrate specificity as well as functionality. Localization of lectins is visualized by labeling of cells with fluorescein-tagged glycoprobes, Glyc-
PAA
-fluo, in combination with fluorescent microscopy techniques. Additionally, biotinylated glycoprobes can be immobilized on magnetic particles making it possible to separate a cell population according to its carbohydrate-binding profile. Here, we exemplify application of glycoprobes in the study of cellular siglecs and galectins, as well as lectin patterning of tumor cells. The specificity of sialic acid binding membrane-anchored lectins, siglecs-1, -5, -7, -8 and -9 was determined using this methodology. To study the carbohydrate-binding profile of soluble galactoside-binding lectins, galectins-1 or -3, these were loaded on (initially galectin free) Raji cells and probed using Glyc-
PAA
-fluo. Lessons learned from this model system allowed us to study the galectin distribution pattern of tumors: cells obtained from mice carrying mammary adenocarcinoma or
lymphoma
were probed with Glyc-
PAA
-fluo using flow cytometry. Disaccharide 6OSuLacdiNAc was shown to be the most potent probe for adenocarcinoma cells, demonstrating that 6OSuLacdiNAc-binding molecules accumulate on cell surface in a patch-wise distribution.
...
PMID:Glycoprobes as a tool for the study of lectins expressed on tumor cells. 1928 39