Researchers from the Chinese Academy of Sciences and affiliated organizations discovered a new ubiquitin-specific protease 7 (USP7) inhibitor, YCH-2823, being developed as a potential anticancer agent.
Researchers from Haisco Pharmaceutical Group Co. Ltd. presented the discovery and preclinical characterization of a brain-penetrating BRAF paradox breaker, HSK-42360, being developed for the treatment of BRAF-driven cancers. HSK-42360 proved to be a potent BRAF V600E inhibitor (IC50=5 nM) with selectivity over wild-type BRAF.
Werner syndrome helicase (WRN), which plays important roles in DNA repair and maintenance of genome integrity, has been recently identified as therapeutic target for microsatellite instability (MSI)-H tumors, which have deficiencies in DNA damage repair.
Researchers from Dong-A Socio Holdings Co. Ltd. presented a first-in-class Src homology 2 domain-containing phosphatase 1 (SHP1) allosteric inhibitor, SB-8091, being developed as an anticancer agent.
In tumors with amino acid deprivation, eIF-2α kinase GCN2 is activated and triggers a signaling response to promote cell survival and proliferation. This is important in high metabolically active hematological cancers, such as acute myeloid leukemia (AML).
AR-V7 is the most clinically relevant androgen receptor (AR) splice variant associated with endocrine resistance and poor prognosis in patients with prostate cancer.
Using its artificial intelligence/machine learning platform, Aurigen, Auron Therapeutics Inc. has identified histone acetyltransferase KAT2A/B as a driver of tumor cell plasticity and designed new small-molecule degraders of KAT2A/B.
Despite GTPase KRAS being the most common mutated oncogene in human cancers, there is still an unmet medical need for treating KRAS G12C-mutated cancers.
Zinc transporter ZIP6, also known as LIV-1, is a transmembrane protein that is an interesting target for antibody-drug conjugate (ADC) therapy because of its higher expression in tumors and almost no expression in normal tissues.
Multiple myeloma (MM) stands as the second most common hematologic malignancy. Proteasome inhibitors are effective in MM, but many patients develop resistance, which is thought to be caused by mutations in the PSMB5 gene.
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