about
Kinase-dead BRAF and oncogenic RAS cooperate to drive tumor progression through CRAFNovel inhibitors of B-RAF based on a disubstituted pyrazine scaffold. Generation of a nanomolar lead.Novel inhibitors of the v-raf murine sarcoma viral oncogene homologue B1 (BRAF) based on a 2,6-disubstituted pyrazine scaffold.Novel tricyclic pyrazole BRAF inhibitors with imidazole or furan central scaffolds.A novel, selective, and efficacious nanomolar pyridopyrazinone inhibitor of V600EBRAF.Paradox-breaking RAF inhibitors that also target SRC are effective in drug-resistant BRAF mutant melanoma.Combined Pan-RAF and MEK Inhibition Overcomes Multiple Resistance Mechanisms to Selective RAF Inhibitors.The genetic landscape of clinical resistance to RAF inhibition in metastatic melanoma.The role of signaling pathways in the development and treatment of hepatocellular carcinoma.Potent BRAF kinase inhibitors based on 2,4,5-trisubstituted imidazole with naphthyl and benzothiophene 4-substituents.Gatekeeper mutations mediate resistance to BRAF-targeted therapies.Development of novel, highly potent inhibitors of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF): increasing cellular potency through optimization of a distal heteroaromatic group.BRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring.Pyridoimidazolones as novel potent inhibitors of v-Raf murine sarcoma viral oncogene homologue B1 (BRAF).Identification of inhibitors of the kinase activity of oncogenic V600E BRAF in an enzyme cascade high-throughput screen.In vitro and in vivo pharmacokinetic-pharmacodynamic relationships for the trisubstituted aminopurine cyclin-dependent kinase inhibitors olomoucine, bohemine and CYC202.The Cyclin-dependent kinase inhibitor CYC202 (R-roscovitine) inhibits retinoblastoma protein phosphorylation, causes loss of Cyclin D1, and activates the mitogen-activated protein kinase pathway.Novel hinge binder improves activity and pharmacokinetic properties of BRAF inhibitors.Novel potent BRAF inhibitors: toward 1 nM compounds through optimization of the central phenyl ring.The cyclin-dependent kinase inhibitor seliciclib (R-roscovitine; CYC202) decreases the expression of mitotic control genes and prevents entry into mitosis.Molecular profiling and combinatorial activity of CCT068127: a potent CDK2 and CDK9 inhibitor.Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitors.Suppression of interferon gene expression overcomes resistance to MEK inhibition in KRAS-mutant colorectal cancerAll Roads Lead to the RibosomeThe EGF Receptor Hokey-CokeyInactivation of NF1 Promotes Resistance to EGFR Inhibition in KRAS/NRAS/BRAFV600-Wild-Type Colorectal CancerCombined targeting of MEK and the glucocorticoid receptor for the treatment of RAS-mutant multiple myelomaIncreased inflammatory lipid metabolism and anaplerotic mitochondrial activation follow acquired resistance to vemurafenib in BRAF-mutant melanoma cellsCorrection: Suppression of interferon gene expression overcomes resistance to MEK inhibition in KRAS-mutant colorectal cancerA genome-scale CRISPR screen identifies the ERBB and mTOR signalling networks as key determinants of response to PI3K inhibition in pancreatic cancer
P50
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P50
description
hulumtues
@sq
researcher
@en
wetenschapper
@nl
հետազոտող
@hy
name
Steven Whittaker
@ast
Steven Whittaker
@en
Steven Whittaker
@es
Steven Whittaker
@nl
Steven Whittaker
@sl
type
label
Steven Whittaker
@ast
Steven Whittaker
@en
Steven Whittaker
@es
Steven Whittaker
@nl
Steven Whittaker
@sl
prefLabel
Steven Whittaker
@ast
Steven Whittaker
@en
Steven Whittaker
@es
Steven Whittaker
@nl
Steven Whittaker
@sl
P106
P21
P31
P496
0000-0001-9062-7947