Kinetolab

Published a study about a gluing docking method for finding small molecules that bind to both the GAP and the mutated KRAS molecules

KINETO Lab proudly announcing that research in the frame of KRAS consortium about new approach for finding small molecules that can be used to attach GAP molecules to RAS proteins mutations to cure the most hard-to-treat cancers, was published in the International Journal of Molecular Sciences.

A significant number of cancers in humans are related to changes in the genetic material, i.e. DNA mutations. More than 600 cancer-causing mutations are currently known. The most important of these are mutations of the RAS protein, which are found in 30% of all human tumors. The most difficult-to-treat human carcinomas such as adenocarcinomas of pancreas, colon and the lung, can be linked to them.

Mutations in RAS prevent the GAP protein from binding to the RAS molecule, thereby allowing unrestricted cell division, thus the disease. Therefore, specific molecules are needed to glue the RAS and GAP molecules together, and restore normal fuction of RAS.

KINETO Lab developed this strategy in the frame of KRAS consortium with partners.

The preliminary results show that the best two small “glue” molecules found based on the new method compete with the best similar molecules found so far in the world, targeting KRAS-G12D mutation.

The continuation of this work, may lead to find new drugs that are effective against the deadliest cancers and have few side effects, since the method does not interfere with the basic mechanisms of cell division, as is the case with chemotherapy interventions today, but instead restores the physiologically normal healthy state.

The publication can be accessed under the following link.