Bivalent Ligands for Protein Degradation in Drug Discovery.
Comput Struct Biotechnol J
; 17: 160-176, 2019.
Article
em En
| MEDLINE
| ID: mdl-30788082
ABCB1, ATP-binding cassette sub-family B member 1; AD, Alzheimer's disease; AHR, aryl hydrogen receptor; ALK, anaplastic lymphoma kinase; Aß, amyloid-ß; BET, bromodomain and extra-terminal; BTK, Bruton's tyrosine kinase; Bcl6, B-cell lymphoma 6; Bivalent ligand; Brd4, bromodomain 4; CDK9, cyclin dependent kinase 9; CK2, Casein kinase 2; CLIPTAC, click-formed proteolysis targeting chimera; CRBN, Cereblon; Chimera; DC50, the compound concentration that results in 50% target protein degradation; DHODH, Dihydroorotate dehydrogenase; Degrader; ERK1, extracellular signal-regulated kinase 1; ERRα, estrogen-related receptor alpha; ERα, estrogen receptor alpha; EZH2, enhancer of zeste homolog 2; FLT3, FMS-like tyrosine kinase-3; FRS2, fibroblast growth factor receptor substrate 2; GCN5, general control nonderepressible 5; GPCR, G-protein coupled receptor; GST, glutathione S-transferase; HDAC, histone deacetylase; HTS, high-throughput screening; MDM2, mouse double-minute 2 homolog; MetAP-2, methionine aminopeptidase-2; PCAF, P300/CBP-associated factor; PEG, polyethylene glycol; PI3K, phosphatidylinositol-3-kinase; PLK-1, polo-like kinase 1; POI, protein of interest; PROTAC; PROTAC, proteolysis targeting chimeras; Proteasome; Protein degradation; RAR, retinoic acid receptor; RIPK2, receptor-interacting serine/threonine-protein kinase 2; RTK, receptor tyrosine kinase; SARM, selective androgen receptor modulator; SNIPER, specific and non-genetic IAP-dependent protein eraser; TBK1, TANK-Binding kinase 1; TRIM24, tripartite motif-containing 24 (also known as TIF1α); VHL, Von Hippel-Lindau; cIAP1, cellular inhibitor of apoptosis protein
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MEDLINE
Tipo de estudo:
Prognostic_studies
Idioma:
En
Ano de publicação:
2019
Tipo de documento:
Article