- Drugs that stimulate the β2-adrenergic receptors (β2AR) can facilitate the relaxation of lung airway muscles and alleviate airway constriction observed in asthma and other lung conditions.
- Prolonged use of these drugs is associated with a decline in their therapeutic efficacy and the potential worsening of asthma symptoms.
- Using a combination of computational simulations and laboratory experiments, a recent study identified new molecules that selectively enhance the therapeutic effects of drugs that stimulate the β2-adrenergic receptors without affecting other pathways.
Until recently, most efforts to develop drugs have focused on molecules that bind to a receptor to activate or inhibit intracellular signaling pathways inside the cells.
However, these molecules that bind to the primary site on the target receptor can lead to significant adverse effects upon binding to other receptors that share a similar structure.
A novel approach involves the use of
Such allosteric modulators do not directly impact signaling pathways on their own but only enhance or inhibit the effects of the agonist binding at the primary site of the receptors. Thus, allosteric modulators are less likely to produce side effects.
The overuse of drugs that activate β2AR for the treatment of asthma and other obstructive lung conditions is associated with a decline in therapeutic efficacy.
A recent study published in the journal PNAS identified allosteric modulators that selectively enhanced signaling pathways in airway muscle cells involved in mediating the therapeutic effects of β2-adrenergic drugs.
Consistently, these allosteric modulators also amplified the ability of β2-adrenergic drugs to induce the relaxation of airway muscles.
Researchers say the use of these…
Read the full article here