Oxford University Innovation Ltd. has reported radiolabeled compounds reported to be useful for the diagnosis and treatment of cancer. An unlabeled form of an exemplified compound ([68Ga]-KK02 pg 33) inhibited PARP1 activity (IC50=9.1 nM).
A Suven Life Sciences Ltd. patent has detailed new N-aryl benzamide derivatives acting as P2X purinoceptor 7 (P2RX7; P2X7) antagonists. As such, they are believed to be potentially useful for the treatment of cancer, pain, renal, neurological, endocrine and psychiatric disorders.
Work at Vir Biotechnology Inc. has led to the identification of 3C-like proteinase (3CLpro; Mpro; nsp5) (SARS-CoV-2; COVID-19 virus) inhibitors reported to be useful for the treatment of SARS-CoV-2 infections (COVID-19).
Aurigene Oncology Ltd. has patented new proteolysis targeting chimera (PROTACs) compounds comprising a protein cereblon (CRBN)-binding moiety covalently bound to a CREB-binding protein (CREBBP; CBP)-targeting moiety through a linker.
Several recent Atavistik Bio Inc. patents describe substituted aminopyridine compounds acting as RAC-α serine/threonine-protein kinase (AKT1; PKBα) inhibitors, particularly AKT1 (E17K mutant) reported to be useful for the treatment of cancer.
When an autoimmune disease disrupted the life of someone close to scientist Dario Gutierrez, an idea emerged for a new company called Merida Biosciences focused on removing misdirected antibodies and their negative effects using Fc biotherapeutics.
Neddylation is a post-translational modification that conjugates the NEDD8 protein to protein substrates, such as the cullins, which once neddylated join complex to form cullin-RING ubiquitin E3 ligases (CRLs), which in turn play a crucial role in regulating proteasomal degradation. The University of Kentucky has presented preclinical data on their neddylation inhibitor TK-59 as a cancer therapeutic.
In Parkinson’s disease (PD), damaged mitochondria build up in the dopaminergic system of the substantia nigra, partly due to impaired mitochondrial autophagy (mitophagy) and autophagosome accumulation.
Pancreatic ductal adenocarcinom a (PDAC), frequently detected at advanced stages, has a 5-year survival rate of 12%. Metastases are common, including hepatic metastasis, which is particularly lethal due to the liver’s immune-tolerant environment and rich blood supply that facilitate tumor growth.
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