Periodic Reporting for period 1 - SUMOblock (Blocking SUMO conjugation as drug discovery strategy.)
Reporting period: 2015-06-01 to 2016-11-30
According to an increasing world population and population age, the cancer incidence is predicted to increase worldwide. The discovery and development of new therapeutic agents for cancer is essential for continued progress against the disease. In this process, the identification of novel targets is a valuable strategy for developing novel drugs with better pharmacological properties to fight the high complexity of cancer.
In eukaryotes, SUMO (Small Ubiquitin Modifier) conjugation to proteins is an essential process that regulates many aspects of cell biology. Defects in SUMO conjugation have been associated to cancer, neurodegenerative diseases and others, raising a great interest in discovering drugs targeting SUMO conjugation. Recent studies have shown that Myc-overexpressing cancers are strongly dependent on an active SUMO conjugation machinery, which has become a non-oncogene addiction target of special relevance since the oncogenic Myc is non-druggable.
In the context of this project, we have developed an innovative assay that has allowed us to identify new chemical identities that display SUMO conjugation inhibition capacity. We have also identified acute myeloid leukemia as an unmet medical need that will benefit of the development of SUMO inhibitors as anti-cancer agent. The standard treatment paradigm for AML has changed little in more than 40 years, continuing to rely on conventional cytotoxic agents, which are not tolerated by older AML patients. In addition, no effective treatment is available for patients with relapsed AML.
We have identified a novel product that belongs to a novel family of SUMO conjugation inhibitors aiming to provide an effective treatment, not currently available, for older AML patients or those with relapsed AML.
For the next steps, in order to optimize the hits identified into lead compounds, we have established an initial network of complementary expertise, including structural biologists, researcher experts in SUMO and AML, and oncologists from the Josep Carreras leukemia research institute. We have identified the creation of a spin-off company as the vehicle for taking the identified hits to the preclinical phase in the drug discovery pipeline, and provide SUMO conjugation inhibitors as an effective treatment, not currently available, for older AML patients or those with relapsed AML.
In eukaryotes, SUMO (Small Ubiquitin Modifier) conjugation to proteins is an essential process that regulates many aspects of cell biology. Defects in SUMO conjugation have been associated to cancer, neurodegenerative diseases and others, raising a great interest in discovering drugs targeting SUMO conjugation. Recent studies have shown that Myc-overexpressing cancers are strongly dependent on an active SUMO conjugation machinery, which has become a non-oncogene addiction target of special relevance since the oncogenic Myc is non-druggable.
In the context of this project, we have developed an innovative assay that has allowed us to identify new chemical identities that display SUMO conjugation inhibition capacity. We have also identified acute myeloid leukemia as an unmet medical need that will benefit of the development of SUMO inhibitors as anti-cancer agent. The standard treatment paradigm for AML has changed little in more than 40 years, continuing to rely on conventional cytotoxic agents, which are not tolerated by older AML patients. In addition, no effective treatment is available for patients with relapsed AML.
We have identified a novel product that belongs to a novel family of SUMO conjugation inhibitors aiming to provide an effective treatment, not currently available, for older AML patients or those with relapsed AML.
For the next steps, in order to optimize the hits identified into lead compounds, we have established an initial network of complementary expertise, including structural biologists, researcher experts in SUMO and AML, and oncologists from the Josep Carreras leukemia research institute. We have identified the creation of a spin-off company as the vehicle for taking the identified hits to the preclinical phase in the drug discovery pipeline, and provide SUMO conjugation inhibitors as an effective treatment, not currently available, for older AML patients or those with relapsed AML.