Researchers from Sichuan University synthesized new pyrazole amides based on the previously described NADH-ubiquinone oxidoreductase (complex I, CI) inhibitor IACS-010759. Subsequent optimization resulted in the identification of SCAL-255 and SCAL-266 as lead candidates with potent CI inhibitory activity.
Intelligent Omics Ltd. has established a target discovery collaboration with Janssen Research & Development LLC, one of the Janssen Pharmaceutical Companies of Johnson & Johnson, to evaluate novel biological targets for the treatment of hematological cancers.
A Pelemed Co. Ltd. patent details new indirubin derivatives acting as inhibitors of FLT3 (FLK2/STK1) and/or proto-oncogene tyrosine-protein kinase receptor Ret (RET; CDHF12; PTC) and its mutants. They are reported to be useful for the treatment of acute myeloid leukemia.
Research at Pharos Ibio Co. Ltd. has led to the identification of son of sevenless homolog 1 (SOS1) inhibitors reported to be useful for the treatment of cancer.
Aurigene Oncology Ltd. has reported the discovery of proteolysis targeting chimeras (PROTACs) comprising an E3 ubiquitin ligase binding agent coupled to probable global transcription activator SNF2L2 (SMARCA2; BAF190B; SNF2-α) and/or transcription activator BRG1 (SMARCA4; BAF190A; SNF2-β) targeting moiety via linker. They act as SMARCA2 and/or SMARCA4 degradation inducers and are reported to be useful for the treatment of cancer.
Synthesis and optimization of a series of 1H-pyrazolo[4,3d]pyrimidine molecules at Bristol Myers Squibb Co. led to the identification of compound [I] as the lead Toll-like receptor 7 (TLR7) agonist, with EC50 values of 21 and 94 nM for human and mouse TLR7, respectively.
A Spanish study led by scientists from the Cajal Institute and the National Center of Oncological Research (CNIO) combined the power of artificial neural networks and biological neuronal circuits to identify abnormal brain activity produced by secondary metastases in the CNS and classify these tumors. The work, published online on Aug. 30, 2023, in Cancer Cell, showed how damage in the brain did not depend on the tumor size but on the effect it produced on neuronal circuits, interrupting cell communication.
Purdue Research Foundation has prepared and tested new peptides acting as N-terminal Xaa-Pro-Lys N-methyltransferase 1 (NTMT1) inhibitors reported to be useful for the treatment of cancer.
Research at Aurigene Oncology Ltd. has led to the identification of fused bicyclic heterocyclyl compounds acting as ubiquitin carboxyl-terminal hydrolase 1 (USP1) inhibitors and reported to be useful for the treatment of cancer.
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