Researchers from National Health Research Institutes reported the discovery and preclinical characterization of a novel long half-life Aurora A (AURKA) inhibitor being developed for the treatment of MYC-amplified solid tumors. Lead optimization of a previously reported series of small-molecule Aurora kinase inhibitors led to the discovery of AURKA kinase inhibitor 6K465, which was then developed into the acyl-based prodrug DBPR-728.
Scientists at Cerevance Inc. and Cerevance Ltd. have described potassium channel subfamily K member 13 (KCNK13; THIK-1) blockers reported to be useful for the treatment of fibrosis, depression, diabetes, gout, psoriasis, atherosclerosis, inflammatory bowel disease and traumatic brain injury.
Xuanzhu Pharma Co. Ltd. has divulged poly (ADP-ribose) polymerase 1 (PARP-1; ARTD1) inhibitors reported to be useful for the treatment of atherosclerosis, cancer, epilepsy, hyperlipidemia, ischemia, osteoarthritis, pain and Alzheimer’s disease.
Sitryx Therapeutics Ltd. has identified compounds acting as pyruvate kinase M2 (PKM2) and/or PKLR activators reported to be useful for the treatment of cancer, obesity, inflammation, diabetes and hematologic disorders.
Petra Pharma Corp. has synthesized phosphatidylinositol 3-kinase α (PI3Kα) inhibitors, particularly H1047R and/or E545K mutant allosteric inhibitors. They are described as potentially useful for the treatment of cancer, PIK3CA-related overgrowth spectrum, congenital lipomatous overgrowth, vascular malformations, epidermal naevi and skeletal abnormalities.
Researchers from Federation University Australia and affiliated organizations have reported data from a study that aimed to assess the therapeutic efficacy of the poly (ADP-ribose) polymerase (PARP) inhibitor olaparib in a large animal model of pulmonary fibrosis.
Tumor-associated macrophages (TAMs), located within the tumor microenvironment (TME), are involved in immunosuppression, metastasis, chemoresistance and angiogenesis. Reprogramming TAMs intratumorally by targeting glutamine metabolism may provide a robust antitumor effect.
Previous studies have demonstrated that CaMKKβ/AMPK signaling plays an important role in regulating mitochondrial homeostasis and that down-regulation of CaMKKβ could contribute to the pathogenesis of diabetic kidney disease (DKD).
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