The intracellular MAPkinase/ERK pathway is a ubiquitous signaling cascade that activates hundreds of molecules. They fulfill a plethora of functions such as cell adhesion, cell cycle progression, cell survival, differentiation, metabolism, proliferation.
Overview in oncology: Aberrant activation of the ERK signaling cascade is associated with genetic mutations in about one-third of all human cancers. Inhibition of components of this cascade by targeted inhibition represents an important anti-tumor strategy with enormous perspectives.
Overview in CNS: Within the Central Nervous System (CNS), ERK activation is associated with synaptic plasticity, learning and memory processes. Dysregulations of ERK activity and ERK-dependent molecular events meet up with a vast array of cognitive and psychiatric impairments.
Inhibitors of ERK cascade components (RAS, Raf, MEK, ERK inhibitors…) have been developed and identified as promising therapeutics. However, so far, these inhibitors induce a too large-scale inhibition of the pathway, leading to numerous undesired side effects.
MELKIN Pharma develops innovative solutions to target specific components of the MAPkinase/ERK pathway. These drugs are small peptides displaying major properties:
To enter into the cell
To selectively block downstream components of the MAPK/ERK pathway without interfering with its global activity.
To be devoid of side effects.