Receptor tyrosine kinase-like orphan receptor 1 (ROR1), a receptor tyrosine kinase activated by Wnt5, is mainly expressed during fetal development and plays a crucial role in processes such as neurodevelopment and angiogenesis. ROR1 is nearly absent in most adult and pediatric tissues but is overexpressed in various malignancies, including leukemia and lung and breast cancers. Its expression has been correlated with poor clinical outcomes, and therefore, it is considered a promising cancer therapeutic target.
Multiple myeloma (MM) is a complex and heterogeneous blood cancer, and current risk assessment tools like the Revised International Staging System (R-ISS) have limitations in accurately predicting prognosis, especially for the intermediate-risk R-ISS II group.
Being able to detect and monitor the aggregation of α-synuclein in situ could lead to more objective, earlier diagnosis of Parkinson’s disease as well as allow real-time monitoring of whether patients are responding to treatment.
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.
