Cycloicaritin (CICT) is a bioactive natural flavonoid extracted from Epimedium species with anti-inflammatory, antimicrobial or antiproliferative effects but with low bioavailability.
Enliven Therapeutics Inc. has divulged Raf kinase inhibitors reported to be useful for the treatment of cancer. An exemplified compound (Ex 5 [isomer B] pg 130) inhibited ERK phosphorylation in human melanoma A-375 cells (IC50=12.4 nM) in ELISA assays.
Resistance to radiotherapy is a crucial factor in the outcome of colorectal cancer (CRC). The Janus kinase/signal transducer and activator of transcription (JAK/STAT) signaling pathway plays a key role in cell growth, differentiation, proliferation and immune function.
In a presentation at the American Chemical Society meeting, Halda Therapeutics Inc. described its androgen receptor (AR)-targeting RIPTAC (regulated induced proximity targeting chimera) therapeutics as a new class of heterofunctional small molecules designed to selectively kill cancer cells that express tumor-specific targeting protein (TIP) into a stable intracellular ternary complex with a protein essential for cell survival for the treatment of prostate cancer.
Colorectal cancer (CRC) is rated as the second most deadly cancer after lung cancer. Identifying new mechanisms responsible for CRC pathogenesis is crucial for the development of new therapies.
Both casein kinase 1α (CK1α) and zinc finger protein Helios (IKZF2) are among the targets most recently evaluated for the treatment of acute myeloid leukemia (AML). A growing number of molecules against these targets acting as degraders or inhibitors are actively being investigated.
Chengdu Duote Antibody Pharmaceutical Co. Ltd. has described antibody-drug conjugates comprising antibody or antigen-binding fragments covalently linked to eribulin derivatives through a linker reported to be useful for the treatment of cancer.
Nanjing Mingde New Drug Research Co. Ltd. has divulged proteolysis targeting chimeras (PROTACs) comprising an E3 ubiquitin ligase-binding agent coupled to an estrogen receptor α (ER-α; ESR1)-targeting moiety via linker. They are reported to be useful for the treatment of breast cancer.
Beijing Zheyuan Technology Co. Ltd. has synthesized serine/threonine-protein kinase PLK1 (STPK13) inhibitors reported to be useful for the treatment of cancer and sepsis.
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