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Biology subjects

Hsu, L.-Y.

Publications and source records attributed to Hsu, L.-Y..

3 recordsLinked to original sources

Soquelitinb, A selective inhibitor of interleukin-2-inducible kinase (ITK), is active in several murine models of T cell-mediated inflammatory disease

Interleukin-2-inducible T cell kinase (or ITK) is a tyrosine kinase predominantly expressed by T lymphocytes. It plays a major role in T cell activation, differentiation, and receptor signaling. Studies in mouse models have established that the absence or inhibition of ITK reduces the secretion of Th2 and Th17 cytokines, while favoring the production of Th1 cytokines and the differentiation of T cells to regulatory T cells (T regs). We recently characterized the activity of soquelitinib (SQL), a selective, covalent inhibitor of ITK in vitro using mouse or human T cells and in vivo in murine models of cancer. We hypothesized that selective pharmacologic blockade of ITK could attenuate a variety of T cell-mediated inflammatory diseases including murine models that resemble asthma, pulmonary fibrosis, systemic sclerosis, psoriasis, and acute graft versus host disease. In each model, SQL demonstrated substantial ability to ameliorate the disease process along with effects on cytokines and/or T cell subsets consistent with the reported function of ITK. Our studies demonstrate that selective inhibition of ITK by SQL is potentially a novel therapeutic approach for several forms of T cell-mediated, inflammatory diseases.

immunology↗

Selective inhibition of interleukin-2 inducible T cell kinase (ITK) enhances anti-tumor immunity in association with Th1-skewing, cytotoxic T cell activation, and reduced T cell exhaustion

ITK is a tyrosine kinase expressed predominantly by T lymphocytes. In mice, selective knock-out of the ITK gene produces Th1 skewing of T helper cell differentiation. We synthesized a covalent ITK inhibitor, soquelitinib, that binds ITK with greater than 100-fold selectivity compared to binding to resting lymphocyte kinase (RLK). In vitro studies with normal or malignant T cells demonstrated that soquelitinib suppresses Th2 cytokine production preferentially with relative sparing of Th1 cytokines. Soquelitinib inhibits the in vivo growth of several syngeneic murine tumors including those that do not express ITK. Treatment with soquelitinib leads to increased tumor infiltration of normal CD8+ cells that possess enhanced T effector function. Soquelitinib inhibited expression of T cell exhaustion markers and was able to restore T effector function to exhausted cells. Pharmacologic selective ITK inhibition may represent a novel approach to cancer immunotherapy.

cancer biology↗

Reporters of TCR signaling identify arthritogenic T cells in murine and human autoimmune arthritis

How pathogenic CD4 T cells in Rheumatoid Arthritis (RA) develop remains poorly understood. We used Nur77--a marker of T cell antigen receptor (TCR) signaling--to identify antigen-activated CD4 T cells in the SKG mouse model of autoimmune arthritis and in patients with RA. Using a fluorescent reporter of Nur77 expression in SKG mice, we found that higher levels of Nur77-eGFP in SKG CD4 T cells marked their autoreactivity, arthritogenic potential, and ability to more readily differentiate into IL-17 producing cells. Moreover, the enhanced autoreactivity was associated with upregulation of IL-6 cytokine signaling machinery. As a result, the more autoreactive GFPhi CD4 T cells from SKGNur mice were hyper-responsive to IL-6. This suggests that, despite impaired TCR signaling, autoreactive T cells exposed to chronic antigen stimulation exhibit heightened sensitivity to IL-6 which contributes to the arthritogenicity in SKG mice, and perhaps in patients with RA. Additionally, endogenous Nur77 protein expression was enriched in a subset of synovial CD4 T cells from arthritic joints in SKG mice, consistent with antigen-activated T cells. This was was extended to patients with seropositive RA, suggesting that pathogenic CD4 T cells are enriched in RA joints and are likely recognizing an intra-articular auto-antigen(s).

immunology↗