Novel PDE6δ inhibitors for the treatment of K-Ras mutant pancreatic cancer


Medicine

Ref.-No.: 0803-5326-IKF

Pancreatic cancer continues to pose significant challenges in the field of oncology, with dismal survival rates and limited treatment options. Patients diagnosed with this aggressive malignancy often face an uphill battle, with a five-year relative survival rate of just 11%.

Ras proteins are well-known as pivotal regulators of cell growth, proliferation, and differentiation, with their dysfunction implicated in various cancers (Brunsveld et al., 2006; Gelb et al., 2006). Among the Ras isoforms, K-Ras is the most commonly mutated, occurring in over 90% of pancreatic cancers (Cox et al., 2014) and representing an ideal target for the treatment of this type of cancer.

However, despite substantial research efforts, finding clinically useful drugs to target oncogenic Ras proteins has remained elusive, and treatment options for patients with pancreatic cancer remain limited.

Technology

Researchers at the Max Planck Institute for Molecular Physiology have developed a novel class of inhibitors targeting PDE6δ, an enzyme critical for maintaining the dynamic distribution of K-Ras within cells.

These inhibitors are characterized by a benzene disulfonamide structure, which enables them to achieve powerful inhibition of the binding between PDE6δ and Ras. They present high affinity for PDE6δ, with a KD in the low nanomolar range.

Furthermore, in vitro experiments have provided compelling evidence of their efficacy, as these inhibitors significantly reduced proliferation of several pancreatic cancer cell lines.

Patent Information

International Patent Application No. PCT/EP2018/050699, filed on July 19, 2018.

Opportunity

We are open to research partnerships and license agreements to accelerate the integration of our PDE6δ inhibitors into the clinical practice.

PDF Download

Contact

Senior Patent- & License Manager

Dr. Ingrid Kapser-Fischer

Nutritionist, M.Sc.

Phone: +49 89 / 29 09 19-19
Email:
kapser-fischer@max-planck-innovation.de

Go back