A method for parallel sequencing of single-cell extrachromosomal circular DNA (ecDNA) and full-length mRNA transcriptomes has enabled new insights into the roles of ecDNA in cancer progression, researchers from Charité hospital and the Max Delbrück Center for Molecular Medicine reported in Nature Genetics on May 8, 2023. Circular DNAs are present in at least a third of cancer cells, and their presence correlates with poor prognosis in many cases. They can carry driver genes that have separated themselves from their chromosome of origin, and some research suggests that they serve as “reserve copies” of driver genes. Boundless Bio Inc. is in phase I trials targeting ecDNAs.
Biosplice Therapeutics Inc. has described 1H-pyrrolo[2,3-b]pyridines acting as dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1A (DYRK1A) inhibitors reported to be useful for the treatment of cancer, diabetes and neurological disorders.
Gossamer Bio Inc. has divulged trisubstituted pyridines acting as non-receptor tyrosine-protein kinase TYK2 inhibitors reported to be useful for the treatment of asthma, atopic dermatitis, contact dermatitis, inflammatory bowel disease, multiple sclerosis, psoriasis, rheumatoid arthritis and allergic rhinitis, among others.
Stemline Therapeutics Inc. has identified proto-oncogene tyrosine-protein kinase receptor Ret (RET; CDHF12; PTC) (mutant) inhibitors reported to be useful for the treatment of cancer.
F. Hoffmann-La Roche Ltd. and Hoffmann-La Roche Inc. have synthesized GABA-A receptor γ1 subunit positive allosteric modulators (PAMs) reported to be useful for the treatment of cognitive and neurological disorders.
Philochem AG has disclosed conjugates comprising fibroblast activation protein α (FAP) ligands covalently linked to radiolabeled payloads through a linker. They are reported to be useful for the diagnosis of atherosclerosis, cancer, fibrosis, inflammation and keloids.
The B-raf kinase (BRAF oncogene) controls cell proliferation and survival through the mitogen-activated protein kinase (MAPK) pathway. By contrast, constitutively activated mutated BRAF causes uncontrolled tumorigenesis while small-molecule inhibition arrests growth to cause tumor regression.
T-cell exhaustion is a differentiation state of T cells associated with tumor progression in the context of cancer. One of the co-stimulatory molecules in the tumor microenvironment, 4-1BB, triggers a signaling cascade resulting in cytokine secretion and upregulation of antiapoptotic molecules.
Although FMS-like tyrosine kinase 3 (FLT3) inhibitors have shown success treating FLT3-mutated acute myeloid leukemia (AML), around 30% to 50% of patients show primary resistance to both type I and type II inhibitors. Therefore, identifying therapeutic strategies to overcome this resistance and enhance the efficacy of FLT3 inhibitors remains an urgent need.
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.webp?height=488&t=1670008838&width=650 "Acute myeloid leukemia")