Oxford University Innovations Ltd. has synthesized hypoxia-activated proteolysis targeting chimeras (hypoxia-activated PROTACs; HAP-TAC) comprising a hypoxia-activated moiety modified E3 ubiquitin ligase-binding moiety coupled to a protein targeting moiety through a linker reported to be useful for the treatment of cancer.
Researchers from Lund University and collaborators have investigated the potential of selectively targeting TUBG1 as a therapeutic strategy in cancer treatment.
Mutations in the oncogene KRAS are widespread in several human cancers, including pancreatic ductal adenocarcinomas (92%), colorectal carcinomas (49%) and lung adenocarcinomas (35%). These mutations hyperactivate various downstream signaling pathways, including the MAPK and PI3K/ AKT pathways. In KRAS-mutant tumors, both primary and acquired resistances are common.
Briacell Therapeutics Corp.’s subsidiary, Briapro Therapeutics Corp., is developing novel, high affinity antibodies to B7-H3 using molecular modeling techniques. As both an immune checkpoint molecule that regulates T-cell activity and a cell surface molecule expressed on many types of cancer cells, B7-H3 is a promising drug target.
Although CD19-directed CAR T cells can initially induce remission in 70-90% of patients with relapsed/refractory B-cell acute lymphoblastic leukemia (B-ALL), post-CAR relapses are frequent. These relapses are driven by insufficient persistence of CAR T cells, allowing for antigen-positive B-ALL re-emergence and loss of the targeted epitope either in isolation or as part of lineage-switching.
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.
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.
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.
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