On September 25, 2017 SignalRx Pharmaceuticals Inc. reported the presentation of scientific data on the company’s in silico platform technology for the rational design of dual small-molecule PI3K/BRD4 inhibitor for immune-oncology relative to activating anti-tumor immunity (Press release, SignalRx, SEPT 25, 2017, http://www.ireachcontent.com/news-releases/signalrx-presents-in-silico-design-of-dual-pi3kbrd4-inhibitors-for-combinatorial-activation-of-anti-tumor-immunity-in-treating-cancer-647615323.html [SID1234527320]). The presentation by Dr. Donald L. Durden, MD, PhD, senior scientific advisor for SignalRx, was made at the Immunomodulatory Small Molecules section of the 15th Annual Discovery on Target meeting in Boston, MA on September 25, 2017 at 8:40 a.m.
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The presentation was entitled "A Novel Dual PI3K/BRD4 Inhibitor, SF2523 for Combinatorial Activation of Anti-Tumor Immunity in Cancer via the Orthogonal Inhibition of MYCN and MYC" and highlighted advancements in the development of single small-molecules that simultaneously inhibit both PI3 kinase (PI3K) and the new epigenetic cancer target BRD4 in vivo.
Key highlights presented are:
Dual inhibitory chemotype disclosed which blocks MYC via two orthogonal independent pathways.
Synergistic anticancer effects of dual inhibition: PI3K inhibition induces MYCN degradation and BRD4 inhibition blocks MYCN transcription.
Dual PI3K/BRD4 inhibitor SF2523 blocks MYCN transcription and induces MYCN degradation
SF2523 shown to block tumor growth, metastasis, and PI3K/BRD4 signaling in vivo.
Demonstrated that SF2523 abrogates the macrophage immunosuppressive effects on tumor immunity via the blockade of the M1- M2 transition in vivo, and activates the adaptive T cell immune response against the tumor.
Data also was also presented related to the recent discovery of SRX3207, a novel dual inhibitor which inhibits PI3K and a recently discovered new immune checkpoint kinase. This inhibitor has potent immunostimulatory properties and blocks the immunosuppressive macrophage compartment.
SignalRx, focused on developing more effective oncology drugs through molecular design imparting multiple target-selected inhibition, is also announcing that it is seeking partnerships to accelerate the development of their novel small molecules into first-in-man clinical trials. These molecules include single-targeted novel BRD4 inhibitors and CDK inhibitors with picomolar potencies.