Thetis Pharmaceuticals LLC and Harvard Medical School have presented data on the stable salt chelate of Resolvin E1, TP-317, for the potential treatment of immune checkpoint inhibitor (ICI)-resistant and sensitive tumors. TP-315 is an activator of ChemR23, a receptor expressed on immune cells in the tumor microenvironment. In vivo murine models of lung, melanoma (B16F10) and pancreatic (Panc2-H7) tumors were used to investigate TP-317 monotherapy and in combination with ICI.
The inhibition of an enzyme associated with neurodegeneration processes reduced the toxic effect of tau, one of the proteins that damage neurons in Alzheimer’s disease (AD). A group of scientists from the University of Helsinki have shown in vitro and in animal models of AD how inhibition of the prolyl endopeptidase (PREP) enzyme reduced tau protein aggregations.
The Chinese National Institute of Pharmaceutical R&D Co. Ltd. has described sulfonamide compounds acting as tyrosine-protein phosphatase non-receptor type 11 (PTPN11; PTP-2C; SHP-2) inhibitors reported to be useful for the treatment of diabetes, obesity, cancer, Noonan and LEOPARD syndromes.
Research at Enveric Biosciences Canada Inc. has led to the development of aminated psilocybin derivatives acting as 5-HT1A or 5-HT2A receptor modulators and reported to be useful for the treatment of psychiatric disorders.
Vifor Pharma Ltd. has identified solute carrier family 40 member 1 (SLC40A1; ferroportin) inhibitors reported to be useful for the treatment of iron metabolism disorders, among others.
Shionogi & Co. Ltd. has synthesized spiroheterocycle derivatives acting as 5-HT2A and 5-HT2C receptor antagonists and/or inverse agonists reported to be useful for the treatment of neurodegeneration.
Among over 100 members of the PTP family, protein-tyrosine phosphatase 1B (PTP-1B) and T-cell protein-tyrosine phosphatase (PTPN2, TCPTP) have the most closely related homology (72%), sharing identical catalytic subunits. Significantly, together they serve nonredundant functions suppressing CD8+ T-cell activation and negatively impacting on tumor cells antigen presentation. Agents that can simultaneously target both PTP-1B and TCPTP have the potential to provide therapeutic benefits in the context of cancer and/or diabetes by increasing T-cell activation and reversing suppression of tumor cell MHC1 expression.
Expression of the tyrosine-protein phosphatase non-receptor type 22 (PTPN22) is restricted to hematopoietic cells where it serves critical functions in regulating T-cell signaling that have made PTPN22 the focus of potential future cancer immunotherapy.
Researchers from Astrazeneca plc described the development and preclinical evaluation of AZD-5335, a novel antibody-drug conjugate (ADC) consisting of folate receptor α (FR-α)-targeting antibody conjugated to a proprietary topoisomerase 1 inhibitor (TOP1i), being developed as a potential new therapeutic against ovarian cancer.
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