Portfolio
Previously highlighted programmes
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Metabolic diseases / cardiovascular | Lead optimization | Selective agonists for EPAC1
Scientists from the Yarwood Lab and the European Screening Centre have jointly published on the discovery of a new class of EPAC activators. The study, which describes the identification, optimisation and characterisation of a new chemical class of selective agonists for EPAC1, is the result of another successful collaboration within the framework of the European Lead Factory (ELF).
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Oncology | Lead optimization | KLK6 reduction
Scientists from the German Cancer Research Center (DKFZ) have successfully discovered potent and selective inhibitors of enzymes associated with the development of some cancers and neurodegenerative diseases. Published in ChemMedChem, the findings mark a significant step in the development of potential new cancer treatments.
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CNS & Neurology | On the way to clinical candidate selection | KEAP1 inhibitors to combat neurodegenerative diseases
Keapstone Therapeutics is preparing to make the next steps in clinical candidate selection and first-in-human studies. This investment brings the total seed investment to € 2,4 million. Last year Parkinson’s UK together with Sheffield University launched the virtual biotech Keapstone Therapeutics to further develop compounds that boost the internal cellular defence mechanisms against oxidative stress to combat neurodegenerative diseases.
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Metabolic diseases | Preclinical development | New target for metabolic diseases
Servier, an independent international pharmaceutical company, and Scandicure, a Swedish spin-out of the University of Gothenburg, today announced the establishment of an agreement to exploit Scandicure’s innovation in the field of metabolic disease. Scandicure, in collaboration with the IMI-funded European Lead Factory, has developed inhibitors of a novel biological target for non-alcoholic steatohepatitis (NASH), type-2 diabetes and potentially other metabolic diseases.
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Oncology | On the way to clinical candidate selection | Selective inhibitors of ACSS2
Metabomed, an Israeli biotech company that has been successful in progressing results through the European Lead Factory (ELF), has discovered a series of potent and selective inhibitors of ACSS2 (the AcetylCoA Short chain Synthase 2 enzyme) for the treatment of cancers dependent on acetate metabolism. Metabomed’s recent successes have led to the company securing a further $12.5 million in funding. These funds will go towards moving the clinical candidate for its ACSS2 programme towards IND approval.
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CNS & Neurology | Lead optimization | CNS-active NAPE-PLD inhibitor
In his screening proposal to ELF, Professor van der Stelt suggested to search for new inhibitors of NAPE-PLD, the protein responsible for the production of anandamide in the brain. The ELF partners carried out High-Throughput Screening (HTS) on the JECL and performed deselection assays ending up with five high-quality hits with four different chemotypes. Further optimisation of the hits by the Leiden chemists and their collaborators led to the discovery and characterisation of LEI-401 as the first CNS-active NAPE-PLD inhibitor. The findings presented by the team may open up new avenues for the treatment of anxiety disorders like post-traumatic stress.
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Antimicrobial resistance| Lead to candidate | Novel antibiotics
The University of Oxford takes the next step in targeting antimicrobial resistance, with help of the results and hit compounds delivered by the European Lead Factory. The Oxford team, led by Professor Chris Schofield, has got the opportunity to collaborate with the European Gram-Negative Antibacterial Engine (ENABLE) project to further progress this programme towards clinical development.
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Neglected tropical diseases | Lead optimization | New chemotherapeutic options for Leishmaniasis
Leishmania parasites cause leishmaniasis, a neglected tropical disease found in parts of tropics, subtropics and Southern Europe. The infection is transmitted through the bite of infected phlebotomine sand flies. Among the several forms of leishmaniasis, visceral leishmaniasis is the most severe form of the disease, which is fatal when left untreated. At the moment, there is no approved human vaccine and disease control relies mostly on chemotherapy, which is frequently linked to safety issues, drug resistance, among other issues, hindering disease eradication in endemic areas. Coming up with new chemotherapeutic options is, therefore, of utmost importance.
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Neglected tropical diseases |Lead optimization | Selective inhibitors over human PDEs
With help of the European Lead Factory, the Phosphodiesterase Inhibitors for Neglected Parasitic Diseases (PDE4NPD) project takes the next step towards developing novel drugs against kinetoplastid parasites such as Trypanosoma brucei, the causative parasite of African sleeping sickness, and Trypanosoma cruzi, causing Chagas disease.
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Oncology | Discontinued | IDO1 inhibitors
The Netherlands Translational Research Center (NTRC) has identified IDO1 inhibitors with best-in-class properties. They have been developed from a series of inhibitor compounds first identified by screening the JECL of the European Lead Factory against IOD1 and TDO, important targets in cancer immunotherapy. IDO1 and TDO are two structurally unrelated proteins that both catalyse the degradation of the amino acid tryptophan and regulate the T cell response. Thus, inhibition of IDO1 or TDO restore the body’s immune response against cancer cells. IDO1 and TDO inhibitors may also increase the efficacy of immunotherapy with immune checkpoint inhibitors.
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Oncology | Discontinued | Kinase inhibitor for Acute Myeloid Leukemia
Complementing the current anti-leukaemia arsenal with an inhibitor of this protein would have an impact in terms of survival, but also specifically in relapse prevention by suppressing leukemic residual disease. This target is a kinase with a pivotal role in the cytoskeleton dynamics. The cytoskeleton is involved in the cell division and proliferation of cancer. Screening this target against the compounds in the Joint European Compound Library during the Qualified Hit List (QHL) phase lead to finding chemical matter that was clearly different from what they had found before.