Syracuse University recently presented a comprehensive preclinical program describing the rational design and optimization of peptide antagonists targeting the GDF15/GFRAL/RET receptor complex to mitigate nausea, emesis, anorexia and wasting associated with chemotherapy-induced stress signaling.
Researchers from the Government College University Faisalabad reported the discovery and preclinical characterization of IMS-48, a benzimidazole analogue designed to inhibit both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE).
Hyperuricemia is defined as elevated uric acid levels in serum, usually exceeding 6.8 mg/dL, and the primary pathological cause of gout. Chinese investigators have reported recent results on the urate transporter 1 (URAT1) inhibitor HYJ-2 for the potential treatment of hyperuricemia.
Mixed lineage kinase domain-like pseudokinase (MLKL), a key effector of necroptosis, is highly expressed in hepatocellular carcinoma (HCC), and its targeting may promote parthanatos-mediated immunogenic cell death. Researchers from the Chinese Academy of Sciences and collaborators described the discovery and preclinical characterization of C-116, a MLKL PROTAC degrader developed using AI-assisted rational drug discovery.
Cisplatin is widely used in chemotherapy regimens for many solid tumors, yet its therapeutic benefit is counterbalanced by significant toxicity and immunologically related limitations. Researchers from Jiangxi University of Chinese Medicine described the preclinical efficacy of the PD-L1-targeted cisplatin prodrug MN42-81, designed to overcome these limitations.
Signal transducer and activator of transcription 3 (STAT3) is a central mediator of cytokine and growth factor signaling and is aberrantly activated in approximately 70% of human cancers. Persistent STAT3 signaling drives tumor proliferation, survival, metastasis, angiogenesis, immune evasion and inflammation. Researchers from the University of Michigan reported the discovery and preclinical characterization of SD-965, a selective STAT3 PROTAC degrader.
Genes that are switched on or off in the human brain differ between men and women. Moreover, these differences are not uniform. They vary across cortical regions and cell types. Scientists at the National Institute of Mental Health (NIMH) and the National Institute on Aging (NIA) used single-cell sequencing and unveiled distinct gene expression patterns regulated by hormones and sex chromosomes. This detailed map of the brain’s molecular biology shows how women and men switch on and off more than 3,000 brain genes differently and expands the catalogue of X chromosome genes that escape inactivation.
Addex Pharma SA has disclosed new GABA(B) receptor positive allosteric modulators (PAMs) potentially useful for the treatment of chronic cough, urinary incontinence, neuropathic pain, postoperative pain, neurological and psychiatric disorders.
Corbus Pharmaceuticals Inc. has divulged new cannabinoid CB1 receptor antagonists or inverse agonists potentially useful for the treatment of cancer, dyslipidemia, diabetes, obesity, cardiovascular, inflammatory and liver diseases.
Cogent Biosciences Inc. has discovered new tyrosine-protein kinase JAK2 V617F (JH2 domain) inhibitors potentially useful for the treatment of cancer and myeloproliferative diseases.
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