Article
Ischemic heart disease-associated ∆M1-Q91 PDE5A2 mutant shows reduced efficacy for cGMP, but not sildenafil, binding-induced conformational change.
FEBS letters - 1 Apr 2026
Ahmed Wesam S, Fatima Asma, Geethakumari Anupriya M, Biswas Kabir H
Abstract excerpt
Phosphodiesterase 5 (PDE5) regulates several physiological processes, including cardiovascular function. A familial PDE5A variant resulting in an N-terminal truncation (∆M1-Q91) in PDE5A2 has been linked to premature ischemic heart disease, but its functional impact is unclear. Using computational analysis and BRET-based biosensors, we show that ∆M1-Q91 deletion alters structural dynamics and reduces the efficacy...
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