Following epigenetic STING (stimulator of interferon genes) derepression, inhibition of the MPS1 kinase strongly reactivated cGAS-STING signaling in mutations in both the oncogene KRAS and the tumor suppressor kinase LKB/STK11. Exploiting these findings could lead to a new therapeutic strategy to target treatment-refractory tumors with mutations in KL tumors, which have mutations in both KRAS and LKB1/STK11.
The coagulation factor XI (FXI) from the liver acts as an endocrine molecule in the heart, protecting it from heart failure. Scientists at the University of California, Los Angeles (UCLA) found that this communication between the two organs is mediated by the interaction between FXI and a heart protein. This interaction activated genes in cardiomyocytes that reduced inflammation, fibrosis and diastolic dysfunction, protecting the heart from a heart attack. That FXI participates in preventing heart failure suggests the possibility of using it as a therapeutic target.
The University of Antwerp has identified new quinazolin-4-one and thieno[2,3-d]pyrimidin-4-one HER4 (ERBB4) inhibitors reported to be useful for the treatment of heart failure, cancer, fibrosis, and metabolic and inflammatory disorders.
Genfleet Therapeutics (Shanghai) Inc. has synthesized new mitogen-activated protein kinase kinase kinase kinase 1 (MAP4K1; HPK1; MEKKK1) inhibitors reported to be useful for the treatment of cancer.
Convalife (Shanghai) Health Technology Co. Ltd. has presented new thyroid hormone receptor α (TR-α) and (TR-β) agonists reported to be useful for the treatment of nonalcoholic fatty liver disease, obesity, liver fibrosis, type 2 diabetes and hypercholesterolemia.
Janssen Pharmaceutica NV has described 4-amino-6-oxo-pyridazine derivatives acting as NLRP3 inflammasome inhibitors reported to be useful for the treatment of cancer, asthma and metabolic, autoimmune, liver, renal, cardiovascular and inflammatory disorders, among other disorders.
Mindset Pharma Inc. has patented indole derivatives acting as 5-HT2A receptor agonists reported to be useful for the treatment of neurological disorders and psychosis, among other disorders.
Guangzhou Henovcom Bioscience Co. Ltd. has identified new imidazole TGF-β receptor type-1 (TGFBR1; ALK5; SKR4; TβR-I) inhibitors reported to be useful for the treatment of cancer, hepatic fibrosis, inflammation, osteoporosis, Alzheimer's disease, idiopathic pulmonary fibrosis, diabetic nephropathy and renal disorders, among other disorders.
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