In research conducted at West China Hospital of Sichuan University and Chengdu University of Traditional Chinese Medicine, coupling of the pan-FGFR inhibitor erdafitinib with a CRBN binder led to a new series of fibroblast growth factor receptor (FGFR) degraders, with compound [I] identified as the lead candidate.
Leukemia inhibitory factor (LIF) is an IL-6 type cytokine involved in the inflammatory response, stem cell self-renewal and tumor progression, that binds to LIFR and gp130 on the cell surface. LIF is overexpressed in several types of cancer such as pancreatic, breast or prostate cancer and thus is considered a therapeutic target for the treatment of cancer.
DeepSA, an edit-based generative framework that utilizes deep simulated annealing (SA), was used to develop novel local anesthetics with multiple activities. Researchers from Sichuan University applied DeepSA to generate over 400 analogs of the local anesthetic articaine.
Targeting human glutaminyl-peptide cyclotransferase (QPCT) has emerged as a potential strategy in Alzheimer’s disease (AD). As the main substrates of this enzyme are involved in biological processes associated with neurodegenerative diseases, Parkinson’s disease (PD) and others may be other options to explore as well.
Signal transducer and activator of transcription 3 (STAT3) plays a key role in cell proliferation observed in colorectal cancer (CRC), where up-regulation of STAT3 accelerates tumorigenesis and promotes metastasis.
Receptor-interacting protein kinase 1 (RIPK1) regulates cell cycle and counteracts necroptosis, and is hence considered a target to watch in necroptosis-related conditions such as cancer or inflammatory diseases. Researchers from Sichuan University have reported on the discovery and structural optimization of a novel series of selective RIPK1 inhibitors intended for use in the treatment of inflammatory disorders.
T-cell acute lymphoblastic leukemia (T-ALL) is an aggressive form of leukemia that accounts for around 25% of ALL cases. In recent years, novel strategies have emerged to reduce the dependence on intensive chemotherapy or hematopoietic stem cell transplantation, but there is still a need for new options with better efficacy in this setting.
Researchers from Sichuan University and Chengdu Normal University have reported the discovery of novel G9a/GLP covalent inhibitors for the treatment of triple-negative breast cancer (TNBC).
Researchers from West China Hospital of Sichuan University presented data from a study that aimed to investigate the associations between serum cystatin C (CysC) levels and the progression and survival of patients with amyotrophic lateral sclerosis (ALS).
West China Hospital of Sichuan University has disclosed piperidine derivatives acting as μ-opioid receptor agonists and sigma non-opioid intracellular receptor 1 (SIGMAR1) antagonists.
