Universitą degli studi di Pavia
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Armijos Rivera's curriculum
Curriculum
Publications
Research project
Molecular anticancer therapy targeting cellular protein kinases
Protein kinases are master regulators of the different metabolic pathways in human cells. The human kinome comprises more than 500 protein kinases, belonging to different families. Based on their substrate specificity, they can be divided into two main groups: tyrosine kinases and serene/threonine kinases. They can exist in soluble forms as well as components of membrane receptors. Deregulation of the expression and/or activity of several protein kinases is now recognised as a major oncogenic driver. A prototypic example is the aberrant form of the kinase Abl (BCR-Abl), which is the oncogene whose activity is recognised as the major transforming determinant in chronic myeloid leukaemia. Due to their roles in timor transformation, protein kinases are considered promising targets for the molecular targeted anticancer chemotherapy. The aim of this project will be to identify small molecules active against the oncogenic forms of different cellular kinases, as well as their mutant drug resistant variants selected in patients after chemotherapy with approved agents. Screening assays, coupled to mechanism of action kinetic studies, will allow to select hit compounds which, after optimisation, will generate lead drug candidates. Dr. Rivera will perform the enzymatic screening and kinetic mechanism of action studies on a panel of human kinases, starting from libraries of compounds sent by different medicinal chemistry collaborating groups.
Publications
Research project
Molecular anticancer therapy targeting cellular protein kinases
Protein kinases are master regulators of the different metabolic pathways in human cells. The human kinome comprises more than 500 protein kinases, belonging to different families. Based on their substrate specificity, they can be divided into two main groups: tyrosine kinases and serene/threonine kinases. They can exist in soluble forms as well as components of membrane receptors. Deregulation of the expression and/or activity of several protein kinases is now recognised as a major oncogenic driver. A prototypic example is the aberrant form of the kinase Abl (BCR-Abl), which is the oncogene whose activity is recognised as the major transforming determinant in chronic myeloid leukaemia. Due to their roles in timor transformation, protein kinases are considered promising targets for the molecular targeted anticancer chemotherapy. The aim of this project will be to identify small molecules active against the oncogenic forms of different cellular kinases, as well as their mutant drug resistant variants selected in patients after chemotherapy with approved agents. Screening assays, coupled to mechanism of action kinetic studies, will allow to select hit compounds which, after optimisation, will generate lead drug candidates. Dr. Rivera will perform the enzymatic screening and kinetic mechanism of action studies on a panel of human kinases, starting from libraries of compounds sent by different medicinal chemistry collaborating groups.
