On November 4, 2020 Shuttle Pharmaceuticals, Inc (Shuttle Pharma) a clinical stage, Maryland-based, biopharmaceutical company developing new drugs for cancer treatment in combination with radiation therapy, reported that it was awarded patent number 10,745,352 by the U.S. Patent and Trademark Office (Press release, Shuttle Pharmaceuticals, NOV 4, 2020, View Source [SID1234569904]). These novel compounds enable cancer treatment by the combination of an inhibitory epigenetic mechanism and a stimulatory DNA repair activation process using a single molecule. The patent is the first issued based on Shuttle Pharma’s platform technology linking an ATM activating domain to an HDAC inhibitory domain for cancer treatment and protection of normal tissue. Shuttle Pharma holds the exclusive rights for development of this drug platform.
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Lead inventor Scott Grindrod, PhD describes histone deacetylase (HDAC) inhibitors as a novel class of drugs targeting enzymes involved in regulation of gene expression. HDACs regulate gene expression by changing the conformation of chromatin in cells into a tightly coiled and transcriptionally inactive form. However, acetylated chromatin is more open and supports transcription. Inhibitors of HDAC enzymes can inhibit cell growth, regulate tubulin stability, turn on transcription of tumor suppressor genes, and activate cellular immunity. These are key target functions for cancer treatment.
Ataxia-telangiectasia is a human genetic disease characterized by extreme radiation sensitivity, neurological immune impairment, and premature aging. The mutated gene product (ATM) regulates the responses of cells to DNA damaging agents. In normal cells, ATM protein activation enables efficient repair of radiation damage to protect the genome and promote cell survival.
There are 12 HDAC enzymes with important functions for maintaining health. Clinical applications of pan-HDAC inhibitors have been limited by off target toxicities. Shuttle Pharma has focused its discovery platform technology on HDAC enzyme selectivity. According to Dr. Anatoly Dritschilo, Shuttle Pharma’s CEO, the interest in immunotherapy to treat cancers in combination with other modalities has focused particular attention on HDAC6 selective inhibitors.