On April 20th, 2021, Gain Therapeutics announced a multi-target drug discovery and development deal with Zentalis Pharmaceuticals to identify and address novel oncology targets.
Gain will be using its proprietary Site-Directed Enzyme Enhancement Therapy (SEE-Tx™) computational platform technology to identify new and previously difficult-to-drug oncology targets. Gain CEO Eric Richman said “Our proprietary algorithm, based on a patented method to analyze molecular dynamics and powered by supercomputers, is designed to enable discovery of novel targets in various therapeutic areas. Zentalis’ team brings extensive industry experience and a proven track record in the discovery and clinical development of innovative cancer therapies, which will be beneficial as we work to further validate SEE-Tx for use in combating cancers and other devastating diseases. Together, we are looking forward to changing the way the industry thinks about drug discovery in oncology.”
This partnership aims to identify newly-discovered targets or target protein interactions that can then be drugged for therapeutic benefit to intervene on protein misfolding. This small molecule approach is unique in the industry, as most current cancer therapies and therapies being developed are immunotherapies–a class of therapy that utilizes the body’s own immune system. These immunotherapies can cost hundreds of thousands of dollars and can be incredibly invasive. The potential for a small molecule, oral drug for the treatment of cancer is groundbreaking in that it would allow patients easy and affordable access to care. Additionally, the discovery of novel targets will further progress our knowledge of cancers and the importance of misfolded proteins in disease.
What is SEE-Tx?
SEE-Tx is the first proprietary technology platform exclusively designed to use the 3D structure of proteins to systematically identify allosteric binding sites never described previously and predict their druggability. Powered by supercomputers, its novel algorithm orchestrates molecular modeling at a speed and efficiency that has the potential to redefine drug discovery.
What is the role of protein misfolding in cancer?
Chaperones that mediate protein folding have been identified as critical modulators of proper cellular functions. Most proteins have a half-life of one to two hours, many oncogenes have half-lives of just a few minutes, meaning that they are continually being synthesized, folded and degraded, offering significant opportunities for misfolding. Due to the highly transitional nature of the misfolded state, a misfolded protein can trigger malignant transformation through a variety of unique mechanisms.
How can Gain use allostery to address cancers?
Gain typically utilizes allostery to restore misfolded proteins to the correct conformation thereby restoring function. In the case of cancers, allostery can be utilized to turn off the function of proteins contributing to cancers.