A multifunctional cross-validation high-throughput screening protocol enabling the discovery of new SHP2 inhibitors.
Acta Pharm Sin B
; 11(3): 750-762, 2021 Mar.
Article
em En
| MEDLINE
| ID: mdl-33777680
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