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1.
Bioorg Med Chem Lett ; 20(16): 4945-50, 2010 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-20621472

RESUMO

The search for small molecules that preferentially target the functionally important surfaces of estrogen receptor and disrupt the transcriptional activity in the cell has emerged as a promising area towards rationale based drug design. Herein, we report substituted styryl chromones as a new class of compounds that exhibit selectivity for ERbeta binding at the second binding site of HT and antiproliferative activity in human breast cancer cell line.


Assuntos
Antineoplásicos/síntese química , Benzopiranos/síntese química , Cromonas/química , Estirenos/síntese química , Antineoplásicos/uso terapêutico , Antineoplásicos/toxicidade , Benzopiranos/farmacologia , Benzopiranos/uso terapêutico , Sítios de Ligação , Neoplasias da Mama/tratamento farmacológico , Linhagem Celular Tumoral , Cromonas/uso terapêutico , Cromonas/toxicidade , Simulação por Computador , Desenho de Fármacos , Receptor beta de Estrogênio/química , Feminino , Humanos , Estirenos/farmacologia , Estirenos/uso terapêutico , Termodinâmica
2.
Mod Pathol ; 17(4): 482-8, 2004 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-14976536

RESUMO

The distribution of proteoglycans in 21 temporal and two ulnar artery pseudoaneurysms was studied immunohistochemically. A history of trauma was elicited in six cases, and 16 of the lesions were pulsatile. The clinical diagnosis was aneurysm or cyst in 18 patients, possible arteritis in two patients, tumor in one patient, and unknown in the remaining patient. Histologically, there was a prominent myxoid neointimal response in the walls of each interrupted artery. The remnant arterial segment was often inconspicuous. Prominent smooth muscle cell proliferation and granulation tissue response with inflammation led to misdiagnosis of tumor or vasculitis, respectively, in 11 cases. Immunohistochemical staining for proteoglycans demonstrated abundant, diffuse versican in interrupted wall segments. Biglycan was confined to collagenized and vascularized areas. In some portions of medial disruption, in which angiogenesis was prominent, decorin was expressed within endothelial cells of neocapillaries. These findings demonstrate that superficial pseudoaneurysms may be mistaken clinically and pathologically for unrelated entities. The immunohistochemical studies confirm that versican is upregulated in areas of tensile stress. In addition, the presence of endothelial expression of decorin supports the concept of decorin's involvement in angiogenesis.


Assuntos
Falso Aneurisma/patologia , Matriz Extracelular/metabolismo , Proteoglicanas/metabolismo , Artérias Temporais/patologia , Adolescente , Adulto , Idoso , Falso Aneurisma/etiologia , Falso Aneurisma/metabolismo , Biglicano , Biomarcadores/análise , Criança , Proteoglicanas de Sulfatos de Condroitina/análise , Proteoglicanas de Sulfatos de Condroitina/metabolismo , Decorina , Matriz Extracelular/química , Proteínas da Matriz Extracelular , Feminino , Humanos , Técnicas Imunoenzimáticas , Lectinas Tipo C , Masculino , Pessoa de Meia-Idade , Proteoglicanas/análise , Artérias Temporais/metabolismo , Artéria Ulnar/metabolismo , Artéria Ulnar/patologia , Versicanas
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