Provided herein are methods for inhibiting contraction and/or promoting relaxation of airway smooth muscle cells (e.g., human airway smooth muscle cells), comprising contacting the cells with a Gα12 or RhoA inhibitor. Also provided herein are methods for inhibiting and/or treating bronchoconstriction or promoting bronchodilation in a subject, for example, a subject with airway hyperresponsiveness and/or a disease associated with bronchoconstriction, such as asthma, chronic obstructive pulmonary disease, chronic bronchitis, bronchiectasis or cystic fibrosis, using a Gα12 or RhoA inhibitor, as well as pharmaceutical compositions comprising a Gα12 or RhoA inhibitor.
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