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A multifunctional cross-validation high-throughput screening protocol enabling the discovery of new SHP2 inhibitors.
Song, Yihui; Zhao, Min; Wu, Yahong; Yu, Bin; Liu, Hong-Min.
Afiliação
  • Song Y; School of Pharmaceutical Sciences & Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education, Zhengzhou University, Zhengzhou 450001, China.
  • Zhao M; School of Pharmaceutical Sciences & Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education, Zhengzhou University, Zhengzhou 450001, China.
  • Wu Y; School of Life Sciences, Zhengzhou University, Zhengzhou 450001, China.
  • Yu B; School of Pharmaceutical Sciences & Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education, Zhengzhou University, Zhengzhou 450001, China.
  • Liu HM; School of Pharmaceutical Sciences & Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education, Zhengzhou University, Zhengzhou 450001, China.
Acta Pharm Sin B ; 11(3): 750-762, 2021 Mar.
Article em En | MEDLINE | ID: mdl-33777680
Palavras-chave
AKT, protein kinase B; ALK, anaplastic lymphoma kinase; AML, acute myelogenous leukemia; Allosteric inhibitors; BTLA, B and T lymphocyte attenuator; Bis-tris, bis-(2-hydroxyethyl)amino-tris(hydroxymethyl)methane; DTT, dithiothreitol; DiFMU, 6,8-difluoro-4-methylumbelliferyl hydroxid; DiFMUP, 6,8-difluoro-4-methylumbelliferyl phosphate; Enzyme assay; FI, fluorescence intensity; HEPES, 4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid; HTS, high-throughput screening; High-throughput screening; IC50, half maximal inhibitory concentration; JAK, janus kinase; JMML, juvenile myelomonocytic leukaemia; LB, lysogeny broth; LOC, ligand only control; LS, LEOPARD syndrome; MAPK, mitogen-activated protein kinase; MEK, extracellular regulated protein kinase kinases; NPC, no protein control; NS, Noonan syndrome; OD, optical density; PD-1, programmed death 1; PI3K, phosphatidylinositol 3 kinase; PMSF, phenylmethanesulfonyl fluoride; PTP, protein tyrosine phosphatase; R2, coefficient of determination; RAS, rat sarcoma; S/B, signal over background; SD, standard deviation; SDS-PAGE, sodium dodecyl sulphate polyacyrlamide gel electrophoresis; SH2, Src homology 2; SHP2; SHP2, Src homology phosphotyrosyl phosphatase 2; SHP2-PTP, protein tyrosine phosphatase domain of Src homology phosphotyrosyl phosphatase 2; SHP2-WT, wild type Src homology phosphotyrosyl phosphatase 2; STAT, signal transducer and activator of transcription; Thermal shift assay; Tm, melting temperature; p-IRS1, phosphorylated insulin receptor substrate 1; ΔTm, melting temperature change

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Tipo de estudo: Diagnostic_studies / Guideline / Screening_studies Idioma: En Ano de publicação: 2021 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Tipo de estudo: Diagnostic_studies / Guideline / Screening_studies Idioma: En Ano de publicação: 2021 Tipo de documento: Article