FCX-146, a potent allosteric inhibitor of Akt kinase in cancer cells: Lead optimization of the second-generation arylidene indanone scaffold.

Balasubramaniam, Meenakshisundaram; Lakkaniga, Naga Rajiv; Dera, Ayed A; Fayi, Majed Al; Abohashrh, Mohammed; Ahmad, Irfan; Chandramoorthy, Harish C; Nalini, Ganesan; Rajagopalan, Prasanna

Balasubramaniam, Meenakshisundaram; Lakkaniga, Naga Rajiv; Dera, Ayed A; Fayi, Majed Al; Abohashrh, Mohammed; Ahmad, Irfan; Chandramoorthy, Harish C; Nalini, Ganesan; Rajagopalan, Prasanna.

Afiliação

Balasubramaniam M; Department of Geriatrics, College of Medicine, University of Arkansas for Medical Sciences, Little Rock, AR, USA.
Lakkaniga NR; Department of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, Little Rock, AR, USA.
Dera AA; Department of Clinical Laboratory Sciences, College of Applied Medical Sciences, King Khalid University, Abha, Saudi Arabia.
Fayi MA; Central Research Laboratory, College of Applied Medical Sciences, King Khalid University, Abha, Saudi Arabia.
Abohashrh M; Department of Clinical Laboratory Sciences, College of Applied Medical Sciences, King Khalid University, Abha, Saudi Arabia.
Ahmad I; Central Research Laboratory, College of Applied Medical Sciences, King Khalid University, Abha, Saudi Arabia.
Chandramoorthy HC; Department of Basic Medical Sciences, College of Applied Medical Sciences, King Khalid University, Abha, Saudi Arabia.
Nalini G; Department of Clinical Laboratory Sciences, College of Applied Medical Sciences, King Khalid University, Abha, Saudi Arabia.
Rajagopalan P; Central Research Laboratory, College of Applied Medical Sciences, King Khalid University, Abha, Saudi Arabia.

Biotechnol Appl Biochem ; 68(1): 82-91, 2021 Feb.

Article em En | MEDLINE | ID: mdl-32067263

Assuntos

Indanos; Simulação de Dinâmica Molecular; Neoplasias; Inibidores de Proteínas Quinases; Proteínas Proto-Oncogênicas c-akt; Transdução de Sinais/efeitos dos fármacos; Regulação Alostérica/efeitos dos fármacos; Proteínas Reguladoras de Apoptose/biossíntese; Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos; Células HL-60; Humanos; Indanos/química; Indanos/farmacologia; Neoplasias/tratamento farmacológico; Neoplasias/metabolismo; Neoplasias/patologia; Inibidores de Proteínas Quinases/química; Inibidores de Proteínas Quinases/farmacologia; Proteínas Proto-Oncogênicas c-akt/antagonistas & inibidores; Proteínas Proto-Oncogênicas c-akt/química; Proteínas Proto-Oncogênicas c-akt/metabolismo

Palavras-chave

Akt kinase; PI3K-signalling; allosteric inhibition; cell proliferation; docking; enzyme inhibition; lead optimization; molecular-dynamic (MD) simulation

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Tipo de estudo: Prognostic_studies Limite: Humans Idioma: En Ano de publicação: 2021 Tipo de documento: Article

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