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J Recept Signal Transduct Res ; 25(4-6): 217-35, 2005.
Artigo em Inglês | MEDLINE | ID: mdl-16393913

RESUMO

TT-232 is a structural analogue of somatostatin exhibiting strong and selective growth-inhibitory effects, inhibition of neurogenic inflammation, as well as general anti-inflammatory and analgesic potential without the wide-ranging endocrine side effects of the parent hormone and its "traditional" analogues. The anti-inflammatory action of TT-232 is mediated through the SSTR4 receptor, and its antitumor activity is mediated through the SSTR1 receptor and by the tumor-specific isoform of pyruvate kinase. Its mechanism of action is in line with a new era of molecular medicine called signal transduction therapy, where "false" intracellular or intercellular communication is inhibited or corrected without interfering with basic cell functions and machinery. TT232 has passed phase I clinical trials without toxicity and significant side effects, and phase II studies are running for oncological and anti-inflammatory indications, respectively. This compound has the perspective to become the first drug in molecularly targeted therapy of inflammation where a combined effect of anti-inflammatory, analgesic, and neurogenic inflammation-inhibiting activity can be achieved.


Assuntos
Anti-Inflamatórios não Esteroides/uso terapêutico , Antineoplásicos/uso terapêutico , Inflamação/tratamento farmacológico , Neoplasias/tratamento farmacológico , Peptídeos Cíclicos/uso terapêutico , Transdução de Sinais/fisiologia , Sequência de Aminoácidos , Aminoácidos/química , Animais , Apoptose/fisiologia , Ciclo Celular/fisiologia , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Ativação Enzimática , Inibidores Enzimáticos/uso terapêutico , Humanos , Inflamação/metabolismo , Dados de Sequência Molecular , Estrutura Molecular , Neoplasias/metabolismo , Peptídeos Cíclicos/genética , Receptores de Somatostatina/metabolismo , Somatostatina/análogos & derivados
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