Tiumbio Co Ltd. has described bromodomain-containing protein 4 (BD2 domain) (BRD4 BD2) inhibitors reported to be useful for the treatment of cancer, fibrosis, diabetes, metabolic syndrome, and renal and inflammatory disorders.
Jiangsu Hansoh Pharmaceutical Group Co. Ltd. and Shanghai Hansoh Biomedical Co. Ltd. have divulged proprotein convertase subtilisin/kexin-type 9 (PCSK9) inhibitors acting as LDL-lowering agents reported to be useful for the treatment of stroke, hepatic steatosis, dyslipidemia, coronary artery disease, metabolic syndrome and atherosclerosis.
Nutshell Biotech (Shanghai) Co. Ltd. has identified eukaryotic translation initiation factor 4E (eiF4E) inhibitors reported to be useful for the treatment of cancer.
Beijing Primegene Therapeutics Co. Ltd. has synthesized Mas-related G-protein coupled receptor member X2 (MRGPRX2) antagonists reported to be useful for the treatment of urticaria and asthma.
Pretzel Therapeutics Inc. has disclosed DNA polymerase subunit γ-1 (POLG) modulators reported to be useful for the treatment of neurodegeneration and mitochondrial diseases.
Forkhead box protein L2 (FOXL2) is a protein involved in ovary development and maintenance, among other functions. Mutations in its gene are involved in ovarian failure and granulosa cell tumors, being the latter a rare cancer type caused in most cases by the C134W mutation (c.402C>G) in the FOXL2 gene. By using CRISPR/Cas9 technology, researchers from Spain have aimed to remove this mutation in the FOLX2 gene from granulosa tumor cells.
Researchers from Universidade Estadual da Paraíba, Universidade Federal da Paraiba and affiliated organizations presented the design, synthesis and bio-evaluation of new small-molecule candidates for the treatment of leishmaniasis, a neglected tropical disease that affects approximately 12 million people in four continents.
Venetoclax, a selective Bcl-2 inhibitor, has proven effective in chronic lymphocytic leukemia (CLL), but genetic mutations or adaptive changes over time can result in resistance to treatment and disease relapse. Researchers from Newave Pharmaceutical Inc. and collaborators described the preclinical efficacy of LP-118, a Bcl-2 inhibitor, in venetoclax-resistant models of CLL.
Researchers from Ocean University of China and Qingdao Marine Science and Technology Center published data from a preclinical study that investigated the impact of the quinazolinone derivative MR-2938 on gut microbiota during colitis. A dextran sodium sulfate (DSS)-induced colitis mouse model was constructed, and the animals were treated with MR-2938 (50 or 100 mg/kg).
The absent, small or homeotic-like 1 (ASH1L) protein regulates the expression of HOXA genes, which are critical for the development of MLL1 translocations frequently found in leukemia patients. Knockdown of ASH1L leads to growth arrest and apoptosis of leukemia cells, thereby inhibiting leukemia progression suggesting that ASH1L can be considered as a therapeutic target in this setting.
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