Publications by authors named "E Fernandez-Salas"

Article Synopsis
  • * CD39 breaks down eATP, which helps provoke immune responses against tumors, into adenosine, which has an opposite effect. By blocking CD39, AB598 preserves eATP levels, encouraging a proinflammatory environment that boosts immune cell activity.
  • * Preclinical studies show that AB598 not only inhibits CD39 effectively but also enhances tumor control and immune activation, suggesting it could significantly improve standard cancer treatments.
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Lysine specific demethylase 1 (LSD1) acts as an epigenetic eraser by specifically demethylating mono- and histone 3 lysine 4 (H3K4) and H3 lysine 9 (H3K9) residues. LSD1 has been pursued as a promising therapeutic target for the treatment of human cancer, and a number of LSD1 inhibitors have been advanced into clinical development. In the present study, we describe our discovery of pyrrolo[2,3-]pyridines as a new class of highly potent and reversible LSD1 inhibitors, designed on the basis of a previously reported LSD1 inhibitor GSK-354.

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Multi-tyrosine kinase inhibitors (MTKIs) have thus far had limited success in the treatment of castration-resistant prostate cancer (CRPC). Here, we report a phase I-cleared orally bioavailable MTKI, ESK981, with a novel autophagy inhibitory property that decreased tumor growth in diverse preclinical models of CRPC. The anti-tumor activity of ESK981 was maximized in immunocompetent tumor environments where it upregulated expression through the interferon gamma pathway and promoted functional T cell infiltration, which resulted in enhanced therapeutic response to immune checkpoint blockade.

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