Speaking before the 5th International Conference on Relaxin and Related Peptides in Maui, Hawaii, Dr. Ronen Shemesh of Compugen Ltd. has presented experimental results for three Compugen discovered Relaxin related molecules that could have therapeutic activity in various clinical indications, including labor complications, infertility, inflammation, congestive heart failure and fibrotic diseases.
The three novel peptides, CGEN-25009, 25010 and 25011, were predicted in silico through the use of Compugen’s GPCR Peptide Discovery Platform and were then shown to activate the GPCRs LGR7 (RXFP1) and LGR8 (RXFP2). These receptors are known to be activated by Relaxin and Insulin-like 3 (INSL3), respectively.
CGEN-25009, 25010 and 25011 are short and linear peptides derived through the use of the GPCR platform novel cleavage sites predictor from a precursor protein for which there was no known function.
In his presentation, Dr. Shemesh, project manager for the GPCR platform, summarized recently obtained results from a series of further experiments with the three peptides – such as cAMP measurements and downstream changes measured by cell impedance.
In these experiments, the activation of the GPCRs LGR7 and LGR8 was further confirmed and additional information obtained regarding the activity of these novel molecules. By activation of these receptors, these peptides could potentially have a therapeutic effect in a large number of key pathophysiological conditions. A provisional patent application covering the peptides has been filed by Compugen.
“Our GPCR Peptide Discovery Platform relies on a series of sequential computational biology predictive models and machine learning capabilities,” stated Dr. Shemesh.
“Therefore – and particularly in view of both the critical role of GPCR receptors in the pharmaceutical world and the difficulty in finding novel ligands through traditional experimental methods -- it is extremely rewarding for the project team to see the continuing validation of the platform’s exceptional efficiency and accuracy,” Dr. Shemesh concluded.