New epigenetic agents: therapeutic approach in cancer. Lead optimization stage.

  • Epigenetic modifications are a major driver of biological complexity and can have a role in the development of a variety of disease treatments.

  • Epigenetics is an emerging area covering a broad range of mode of actions. However, only four drugs are currently approved and eleven agents are in early-stage trials.

  • Novel proprietary compounds binding two epigenetic targets have been developed:

    • more effective than reference epigenetic compounds vs different cancer cell lines.

    • first-in-class dual reversible inhibitors of DNMT and HMT.

  • Indication: cancer.

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Novel therapeutic strategy in B-cell malignancies: targeting a key microenvironmental ion carrier machinery

  • Despite recent outstanding advances in chemo-immunotherapy having shifted certain B-cell tumor subtypes from uniformly lethal to curable, most mature B-cell malignancies still remain incurable.

  • The use of therapies combining direct B-cell targeting and immunotherapy implementing T-cell anti-tumor responses by repression of Tregs may improve cure rates of B-cell malignancies.

  • A ion carrier numbered as 17 (IC17) has been found as a new target for tumor immunotherapy. Blocking IC17 function exerts a dual anti-tumor effect on a large number of B-cell malignancies by: 

    • direct targeting of tumor B cells that are forced to undergo apoptosis.

    • triggering of T-cell anti-tumor responses through decreasing Treg numbers and potentiating effector T cells. 

  • Indication: B-cell malignancies (B-cell lymphoma, leukemia and multiple myeloma).

Inhibitors of FOXP3 Transcription Factor for cancer therapy. Assay validation stage.

  • Immunoregulatory function of T regulatory cells (Treg) may hinder the induction of immune responses against cancer and infectious agents.

  • FOXP3 transcription factor is essential for the specification and maintenance of Treg cells and it is considered its "master regulator".

  • Inhibition of FOXP3-NFAT interaction might lead to the impairment of specific functions of FOXP3 and Treg activity and thus, be beneficial in the development of vaccines and tumor therapies.

  • F39, a peptide able to disrupt Foxp3/NFAT interaction has been found:

    • F39 interferes with the ability of FOXP3 to repress expression of IL2 and Treg immunosuppressive activity in vitro and in vivo.

    • F39 is able to improve T cell proliferation and cytokine production by effector T cells after TCR stimulation. 

  • A virtual screening is being conducted to select small molecules that may fit the Foxp3-NFAT hot spot and identify new pharmacological compounds. Experimental assay is currently on-going.

  • Indication: Chronic viral infections (HBV), Cancer (prostate, colorectal, breast…).

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Contact us:

Contact:
Center for Applied Medical Research (CIMA)
Avenida Pío XII, 55
31008 Pamplona
Spain

+34 948 194700
cima@unav.es