The calcineurin inhibitor tacrolimus is an immunosuppressive drug frequently used to prevent transplant rejection in solid organ transplant patients. Tacrolimus acts by suppressing T-cell activity within and around the transplanted organ. However, this drug also inhibits T-cell function in the skin, contributing to a high incidence of skin cancer among transplant recipients.
Flare Therapeutics Inc. has patented peroxisome proliferator-activated receptor γ (PPARγ, PPARG) inverse agonists reported to be useful for the treatment of bladder cancer.
Researchers at Firefly Bio Inc. have prepared antibody-drug conjugates (ADCs) comprising monoclonal antibodies targeting HER2 covalently linked to stimulator of interferon genes protein (STING; TMEM173) agonists through a linker. They are reported to be useful for the treatment of cancer, autoimmune disease, inflammation and infections.
Researchers from Jiangsu Chia Tai Fenghai Pharmaceutical Co. Ltd. and affiliated organizations have published preclinical data for the novel rearranged during transfection (RET) kinase inhibitor, FHND-5071.
Reninomas are rare renin-secreting kidney tumors, resulting from a neoplastic expansion of juxtaglomerular cells of the kidney, which are cells that regulate blood pressure via the secretion of renin. Based on previous research that has proposed a central role for NOTCH1 signaling in the regulation of renin secretion by juxtaglomerular cells, researchers from Wellcome Sanger Institute, University of Cambridge, and affiliated organizations aimed to investigate the role of NOTCH1 in reninoma.
Several Insilico Medicine Inc. patents describe diacylglycerol kinase α (DGK-α, DGKA) inhibitors reported to be useful for the treatment of cancer and viral infection.
Sichuan Huiyu Pharmaceuticals Co. Ltd. and Sichuan Huiyu Seacross Pharma Technology Ltd. have jointly described new phosphatidylinositol 3-kinase (PI3K) and/or GTPase KRAS (G12C mutant) inhibitors reported to be useful for the treatment of cancer and autoimmune diseases.
Researchers from the University of Minnesota and collaborators have synthesized and evaluated a novel series of antiproliferative benzofuran derivatives that led to the identification of [I] as the most potent candidate.
Pathios Therapeutics Ltd. has been awarded a £567,000 (~US$727,000) grant from the U.K. Government’s innovation agency, Innovate UK, that will enable the company to expand its development of novel small-molecule GPR65 inhibitors into the area of malignant brain tumors.
Researchers from Birla Institute of Technology & Science, Pilani and Jadavpur University have reported novel HDAC3 inhibitors as potential candidates for the treatment of breast cancer. Synthesis and optimization of a series of pyrazino-hydrazide-based HDAC3 inhibitors led to the characterization of compound [I] as the lead candidate with potent HDAC3 inhibitory activity (IC50=14 nM) and at least 121-fold selectivity.
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