An SAR study of hydroxy-trifluoromethylpyrazolines as inhibitors of Orai1-mediated store operated Ca<sup>2+</sup> entry in MDA-MB-231 breast cancer cells using a convenient Fluorescence Imaging Plate Reader assay.

Stevenson, Ralph J; Azimi, Iman; Flanagan, Jack U; Inserra, Marco; Vetter, Irina; Monteith, Gregory R; Denny, William A

An SAR study of hydroxy-trifluoromethylpyrazolines as inhibitors of Orai1-mediated store operated Ca²⁺ entry in MDA-MB-231 breast cancer cells using a convenient Fluorescence Imaging Plate Reader assay.

Stevenson, Ralph J; Azimi, Iman; Flanagan, Jack U; Inserra, Marco; Vetter, Irina; Monteith, Gregory R; Denny, William A.

Afiliação

Stevenson RJ; Auckland Cancer Society Research Centre, School of Medical Sciences, The University of Auckland, Private Bag 92019, Auckland 1142, New Zealand. Electronic address: r.stevenson@auckland.ac.nz.
Azimi I; The School of Pharmacy, The University of Queensland, Brisbane, Queensland, Australia; Mater Research Institute, The University of Queensland, Translational Research Institute, Brisbane, Queensland, Australia; Division of Pharmacy, College of Health and Medicine, University of Tasmania, Hobart, Tasm
Flanagan JU; Auckland Cancer Society Research Centre, School of Medical Sciences, The University of Auckland, Private Bag 92019, Auckland 1142, New Zealand; Maurice Wilkins Centre for Molecular Biodiscovery, The University of Auckland, Private Bag 92019, Auckland 1142, New Zealand.
Inserra M; Institute for Molecular Bioscience, The University of Queensland, St Lucia, Queensland 4072, Australia; School of Pharmacy, The University of Queensland, Woolloongabba, Queensland 4102, Australia.
Vetter I; Institute for Molecular Bioscience, The University of Queensland, St Lucia, Queensland 4072, Australia; School of Pharmacy, The University of Queensland, Woolloongabba, Queensland 4102, Australia.
Monteith GR; The School of Pharmacy, The University of Queensland, Brisbane, Queensland, Australia; Mater Research Institute, The University of Queensland, Translational Research Institute, Brisbane, Queensland, Australia.
Denny WA; Auckland Cancer Society Research Centre, School of Medical Sciences, The University of Auckland, Private Bag 92019, Auckland 1142, New Zealand; Maurice Wilkins Centre for Molecular Biodiscovery, The University of Auckland, Private Bag 92019, Auckland 1142, New Zealand. Electronic address: b.denny@au

Bioorg Med Chem ; 26(12): 3406-3413, 2018 07 23.

Article em En | MEDLINE | ID: mdl-29776832

Assuntos

Bloqueadores dos Canais de Cálcio/química; Proteína ORAI1/antagonistas & inibidores; Pirazóis/química; Neoplasias da Mama/metabolismo; Neoplasias da Mama/patologia; Cálcio/metabolismo; Bloqueadores dos Canais de Cálcio/metabolismo; Bloqueadores dos Canais de Cálcio/farmacologia; Sinalização do Cálcio/efeitos dos fármacos; Linhagem Celular Tumoral; Feminino; Humanos; Proteína ORAI1/metabolismo; Análise Serial de Proteínas; Pirazóis/metabolismo; Pirazóis/farmacologia; Espectrometria de Fluorescência; Relação Estrutura-Atividade

Palavras-chave

Ca(2+) release-activated Ca(2+) (CRAC) channel; Hydroxy-trifluoromethylpyrazoline; Inhibitor; Orai1; Store-operated Ca(2+)entry (SOCE); Structure-activity relationship (SAR); Triple negative breast cancer

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Pirazóis / Bloqueadores dos Canais de Cálcio / Proteína ORAI1 Limite: Female / Humans Idioma: En Revista: Bioorg Med Chem Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2018 Tipo de documento: Article País de publicação: Reino Unido

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