CNS-related signaling proteins and receptors

CNS-related signaling proteins and receptors represent a broad and heterogeneous superfamily of molecular entities essential for the physiological functioning of the brain and spinal cord (Purves et al., 2018). This category encompasses various protein classes, including G protein-coupled receptors (GPCRs) such as dopamine and serotonin receptors, ionotropic receptors like GABA and NMDA receptors, and transporters such as the serotonin transporter (SERT) (Alexander et al., 2023; Rang et al., 2019). These molecules are fundamental to signal transduction, mediating the effects of neurotransmitters and neuromodulators that govern behavior, cognition, and homeostasis (Purves et al., 2018). In pathological states, these signaling pathways are often disrupted, contributing to the etiology of neurodegenerative diseases, mood disorders, and epilepsy (Rang et al., 2019). As such, they are among the most heavily researched therapeutic targets in the pharmaceutical industry. However, drug development for these targets is uniquely challenging due to the necessity of blood-brain barrier permeability and the high risk of complex neurological side effects (Pardridge, 2005; Abbott et al., 2010).

Other names

Central nervous system signaling moleculesNeurotransmitter receptors and transportersCNS drug targetsNeurosignaling proteins

The mechanisms of action for drugs targeting these proteins are diverse and depend on the specific molecule involved; they include orthosteric and allosteric agonism or antagonism of receptors to modulate signal transduction, inhibition of enzymes responsible for neurotransmitter synthesis or degradation, and blockade of transporters to alter synaptic neurotransmitter concentrations (Alexander et al., 2023; Rang et al., 2019).