Checkpoint kinase 1 (CHK1) is involved in cell cycle arrest by activation of DNA damage response pathways. The aim of researchers from Shanghai Fosun Pharmaceutical (Group) Co. Ltd. was to develop a potent oral CHK1 inhibitor, XS-02, for the treatment of solid tumors.
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.
Chronic inflammatory and neuropathic pain are among the most common chronic conditions, but their treatment options present significant limitations both in efficacy and safety. Researchers from Purdue University presented data on their work aimed to develop adenyl cyclase type 1 (AC1, ADCY1) inhibitors as a new treatment for chronic pain.
Researchers from University of Belgrade, St. Jude Children’s Research Hospital and affiliated organizations have provided details on the discovery of novel orally bioavailable BET inhibitors as potential anticancer drug candidates.
Deregulation of enzymes that control lipid turnover such as adipose triglyceride lipase (ATGL) is an essential contributor to nonalcoholic fatty liver disease. Recent studies suggest that a fraction of the cytosolic pool of ATGL is proteasomal degraded by E3 ligase constitutive photomorphogenesis protein 1 (COP1).
To date, only one drug has been approved for the treatment of itch (persistent pruritus) and it only targets a small portion of the patient population. Researchers from Mallinckrodt plc have unveiled gastrin-releasing peptide receptor (GRPR) as an itch-specific receptor for nonhistaminergic itch.
Researchers from the University of Arizona presented the discovery of first-in-class dual-specificity tyrosine phosphorylation-regulated kinase 1A/B (DYRK1A/B) proteolysis targeting chimeras (PROTACs) as potential Alzheimer’s disease (AD) therapeutic candidates.
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