Idioma:

Anticancer Therapeutics That Target Selenoenzymes: Synthesis, Characterization, in vitro Cytotoxicity, and Thioredoxin Reductase Inhibition of a Series of Gold(I) Complexes Containing Hydrophilic Phosphine Ligands

Vergara, Elena ; Casini, Angela ; Sorrentino, Francesca ; Zava, Olivier ; Cerrada, Elena ; Rigobello, Maria Pia ; Bindoli, Alberto ; Laguna, Mariano ; Dyson, Paul J.

ChemMedChem, 2010-01, Vol.5 (1), p.96-102 [Periódico revisado por pares]

Weinheim: WILEY-VCH Verlag

Texto completo disponível

Citações Citado por

Enviar para

Título:
Anticancer Therapeutics That Target Selenoenzymes: Synthesis, Characterization, in vitro Cytotoxicity, and Thioredoxin Reductase Inhibition of a Series of Gold(I) Complexes Containing Hydrophilic Phosphine Ligands
Autor: Vergara, Elena ; Casini, Angela ; Sorrentino, Francesca ; Zava, Olivier ; Cerrada, Elena ; Rigobello, Maria Pia ; Bindoli, Alberto ; Laguna, Mariano ; Dyson, Paul J.
Assuntos: Adamantane - analogs & derivatives ; Adamantane - chemistry ; Antineoplastic Agents - chemistry ; Antineoplastic Agents - toxicity ; antitumor agents ; Bridged Bicyclo Compounds - chemistry ; Cell Line, Tumor ; Coordination Complexes - chemistry ; Coordination Complexes - toxicity ; enzyme inhibitors ; Glutathione Reductase - antagonists & inhibitors ; Glutathione Reductase - metabolism ; Gold - chemistry ; gold complexes ; Humans ; Ligands ; medicinal chemistry ; Organophosphorus Compounds - chemistry ; Phosphines - chemistry ; Sulfonic Acids - chemistry ; thioredoxin reductases ; Thioredoxin-Disulfide Reductase - antagonists & inhibitors ; Thioredoxin-Disulfide Reductase - metabolism
É parte de: ChemMedChem, 2010-01, Vol.5 (1), p.96-102
Notas: ArticleID:CMDC200900370
istex:21EBFFFEF7F2FEF93B96BEC68655409EF4384FDE
National Science Foundation
ark:/67375/WNG-VFJW8K4K-S
ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
Descrição: Gold(I) complexes bearing water‐soluble phosphine ligands, including 1,3,5‐triaza‐7‐phosphaadamantane (PTA), 3,7‐diacetyl‐1,3,7‐triaza‐5‐phosphabicyclo[3.3.1]nonane (DAPTA), and sodium triphenylphosphine trisulfonate (TPPTS), in combination with thionate ligands, were screened for their antiproliferative activities against human ovarian cancer cell lines A2780 either sensitive or resistant to cisplatin. In addition, the compounds were screened for their inhibition of mammalian thioredoxin reductases (TrxR), enzymes that are overexpressed in many tumor cells and contribute to drug resistance. The gold(I)–phosphine complexes efficiently inhibited cytosolic and mitochondrial TrxRs at concentrations that did not affect the related oxidoreductase glutathione reductase (GR). Additional complementary information on the enzyme metallation process and potential gold binding sites was obtained through the application of a specific biochemical assay using a thiol‐tagging reagent, BIAM (biotin‐conjugated iodoacetamide). Several studies indicate that thioredoxin reductases represent effective druggable targets for the development of new anticancer drugs. We report herein the inhibitory properties of gold(I) complexes with water‐soluble phosphine ligands. Biochemical studies suggest binding of gold atoms to both cysteine and selenocysteine residues that are catalytically essential.
Editor: Weinheim: WILEY-VCH Verlag
Idioma: Inglês;Alemão

Links

View this record in MEDLINE/PubMed

Voltar para lista de resultados

Anterior Resultado 10 Avançar Ir para próxima página

Realização: Logos de Redes Sociais:

Anticancer Therapeutics That Target Selenoenzymes: Synthesis, Characterization, in vitro Cytotoxicity, and Thioredoxin Reductase Inhibition of a Series of Gold(I) Complexes Containing Hydrophilic Phosphine Ligands

Vergara, Elena ; Casini, Angela ; Sorrentino, Francesca ; Zava, Olivier ; Cerrada, Elena ; Rigobello, Maria Pia ; Bindoli, Alberto ; Laguna, Mariano ; Dyson, Paul J.

Weinheim: WILEY-VCH Verlag

Buscando em bases de dados remotas. Favor aguardar.