Ever since the Epidermal Growth Factor Receptor (EGFR, HER1) was found to overexpress in human tumours back in 1984, Human Epidermal Growth factor Receptors have proven to form a hub of the utmost importance in oncogenesis and the progression regulation of many a kind of cancer as well as the apparition of resistance against treatment, and therefore this family can be considered a group of putative therapeutic targets.

HER dimerization leads to allosteric activation of their kinase domain and subsequent signaling. Alone amongst HERs, HER3 has very little kinase activity due to its impaired kinase dominion, but nonetheless this kinase dominion activates upon dimerisation and its signaling is very powerful. HER3 is thus a central piece of this system, dimerising with HER2, a therapeutic target of breast cancer to which resistance to treatments commonly arises. The complexity of the HER3-HER2 axis, in which many mechanisms of regulation intervene, makes it quite robust.

SunRock Biopharma S.L.

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