Researchers from the Beijing Institute of Radiation Medicine have presented the discovery of novel toll-like receptor (TLR)2/1 agonists as potential candidates for the treatment of lung cancer.
Researchers from State University of New Jersey (Rutgers) and Oklahoma State University have published preclinical data for a novel a SARS-CoV-2 papain-like protease (PLpro) inhibitor being developed as an antiviral candidate for the treatment of COVID-19.
Researchers from Shenyang Pharmaceutical University and affiliated organizations have reported the identification of a selective cyclin-dependent kinase 9 (CDK9) inhibitor, CLZX-205, being developed for the treatment of colorectal cancer.
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.
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