Molecular determinants of drug-specific sensitivity for epidermal growth factor receptor (EGFR) exon 19 and 20 mutants in non-small cell lung cancer. [PDF]
We hypothesized that aberrations activating epidermal growth factor receptor (EGFR) via dimerization would be more sensitive to anti-dimerization agents (e.g., cetuximab).
Bazhenova, Lyudmila+6 more
core +3 more sources
The emerging roles and therapeutic potential of cyclin-dependent kinase 11 (CDK11) in human cancer. [PDF]
Overexpression and/or hyperactivation of cyclin-dependent kinases (CDKs) are common features of most cancer types. CDKs have been shown to play important roles in tumor cell proliferation and growth by controlling cell cycle, transcription, and RNA ...
Duan, Zhenfeng+4 more
core +1 more source
Overexpression of the protein kinase CK2 increases the survival and resistance to chemotherapy of acute myeloid leukemia cells [PDF]
Background: The critical role of protein kinase CK2 in the regulation of cellular apoptosis suggests its may be involvement in tumor cell resistance to both conventional and unconventional therapies.
PAVAN, LAURA
core +1 more source
Binimetinib inhibits MEK and is effective against neuroblastoma tumor cells with low NF1 expression. [PDF]
BackgroundNovel therapies are needed for children with high-risk and relapsed neuroblastoma. We hypothesized that MAPK/ERK kinase (MEK) inhibition with the novel MEK1/2 inhibitor binimetinib would be effective in neuroblastoma preclinical models ...
Liu, Yin+4 more
core +2 more sources
Proline-rich tyrosine kinase 2 mediates gonadotropin-releasing hormone signaling to a specific extracellularly regulated kinase-sensitive transcriptional locus in the luteinizing hormone beta-subunit gene [PDF]
G protein-coupled receptor regulation of gene transcription primarily occurs through the phosphorylation of transcription factors by MAPKs. This requires transduction of an activating signal via scaffold proteins that can ultimately determine the outcome
Adam J. Pawson+73 more
core +1 more source
DeepPurpose-based drug discovery in chondrosarcoma
Background: Chondrosarcoma (CS) is the second most common primary bone tumor, accounting for approximately 30% of all malignant bone tumors. Unfortunately, the efficacy of currently available drug therapies is limited.
Jianrui Li+3 more
doaj
Seminal plasma and prostaglandin E2 up-regulate fibroblast growth factor 2 expression in endometrial adenocarcinoma cells via E-series prostanoid-2 receptor-mediated transactivation of the epidermal growth factor receptor and extracellular signal-regulated kinase pathway [PDF]
BACKGROUND: Prostaglandin E(2) (PGE(2)) has been shown to modulate angiogenesis and tumour progression via the E-series prostanoid-2 (EP2) receptor. Endometrial adenocarcinomas may be exposed to endogenous PGE(2) and exogenous PGE(2), present at high ...
A.R. Williams+48 more
core +1 more source
A Stapled Peptide Mimic of the Pseudosubstrate Inhibitor PKI Inhibits Protein Kinase A
Kinases regulate multiple and diverse signaling pathways and misregulation is implicated in a multitude of diseases. Although significant efforts have been put forth to develop kinase-specific inhibitors, specificity remains a challenge.
Jascha T. Manschwetus+5 more
doaj +1 more source
Extracellular signal-regulated kinase 5 promotes acute cellular and systemic inflammation. [PDF]
Inflammatory critical illness is a syndrome that is characterized by acute inflammation and organ injury, and it is triggered by infections and noninfectious tissue injury, both of which activate innate immune receptors and pathways.
Farrar, Katherine+9 more
core +1 more source
Lessons from LIMK1 enzymology and their impact on inhibitor design [PDF]
LIM domain kinase 1 (LIMK1) is a key regulator of actin dynamics. It is thereby a potential therapeutic target for the prevention of fragile X syndrome and amyotrophic lateral sclerosis.
Beltrami, A+10 more
core +2 more sources