Data on the poly(ADP-ribose) glycohydrolase (PARG) inhibitor SYX-3759, being investigated for the treatment of homologous recombination deficient (HRD) malignancies, were recently discussed by researchers from Hangzhou Synrx Therapeutics Technology Co. Ltd.
Researchers from Hangzhou Polymed Biopharmaceuticals Inc. have reported the discovery and preclinical evaluation of HPB-092, an FMS-like tyrosine kinase 3 (FLT3) and interleukin-1 receptor-associated kinase 4 (IRAK-4) dual inhibitor, being developed for the treatment of acute myeloid leukemia (AML).
Researchers from Dong Wha Pharmaceutical Co. Ltd. presented preclinical evaluation of a newly discovered histone-lysine N-methyltransferase EZH1/2 dual inhibitor, DW-91170, being developed for the treatment of lymphoma.
The Janus kinase/signal transducer and activator of transcription (JAK-STAT) pathway comprises four JAK kinases and seven STAT transcription factors. Among the latter, STAT3 is the best-known oncogene and its essential role in normal tissue makes its complete blockage useless for treatment due to severe side effects.
Macrophages are specialized immune cells that can either stimulate or inhibit inflammation. Studies in mice suggest that phosphoinositide 3-kinase γ (PI3Kγ), a key mediator in macrophage signaling pathways predominantly expressed in myeloid cells, may promote immune suppression both in inflammation and in the tumor microenvironment.
Prostaglandin E2 (PGE2) regulates inflammation and the tumor microenvironment, thought to happen through engagement with the E-type prostanoid EP2 and EP4 receptors, exerting immunosuppression in the tumor microenvironment. The simultaneous blockade of EP2 and EP4 – not blocking either alone – is needed to overcome this immunosuppressor effect.
Cyclin-dependent kinase 8 (CDK8) is implicated in both transcription and cellular response to environmental stress signals. Due to its association with the complex that sustains cell proliferation and viability, and its role in cancer cell stress response to radiotherapy and chemotherapy, CDK8 is considered a target to watch in cancer therapy.
Cyclin-dependent kinase 4 and 6 (CDK4 and CDK6) are validated targets for the treatment of ER+/HER2- breast cancer, but resistance to therapy is still a problem in these patients, with >20% of them developing intrinsic resistance and up to 70% developing acquired resistance within 3 years.
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