PDE5A dimer binds PDE5A inhibitors

Stable Identifier
Reaction [binding]
Homo sapiens
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The cGMP-specific phosphodiesterase PDE5A is highly expressed in vascular and bronchial smooth muscle, in renal tubules and in platelets. It is prominent in the retina and the corpus cavernosa, the pair of erectile tissues in the penis. It catalyses the degradation of cGMP in these tissues, facilitating muscle contraction. Clinically used PDE5A inhibitors target PDE5A in vascular muscle to treat erectile dysfunction (Ventimiglia et al. 2016, Gong et al. 2017) and bronchial smooth muscle to treat pulmonary arterial hypertension (Palacios et al. 2020).

Erectile dysfunction drugs such as Viagra (sildenafil), Cialis (tadalafil) and Levitra (vardenafil) inhibit PDE5A (Boolell et al. 1996, Ballard et al. 1998, Moreland et al. 1998), increasing cGMP levels and thereby allowing smooth muscle relaxation and vasodilation. This allows blood flow into the corpus cavernosa leading to erection (Raheem & Kell 2009).

Literature References
PubMed ID Title Journal Year
9598563 Effects of sildenafil on the relaxation of human corpus cavernosum tissue in vitro and on the activities of cyclic nucleotide phosphodiesterase isozymes

Tang, K, Naylor, AM, Turner, LA, Ballard, SA, Gingell, CJ, Price, ME

J Urol 1998
9600334 Sildenafil, a novel inhibitor of phosphodiesterase type 5 in human corpus cavernosum smooth muscle cells

Goldstein, I, Traish, A, Moreland, RB

Life Sci 1998
8858389 Sildenafil: an orally active type 5 cyclic GMP-specific phosphodiesterase inhibitor for the treatment of penile erectile dysfunction

Boolell, M, Naylor, AM, Muirhead, GJ, Gingell, C, Gepi-Attee, S, Ballard, SA, Osterloh, IH, Allen, MJ

Int J Impot Res 1996
28741090 Direct comparison of tadalafil with sildenafil for the treatment of erectile dysfunction: a systematic review and meta-analysis

Gong, B, Huang, Y, Yang, X, Huang, J, Xie, W, Sun, T, Luo, Y, Ma, M

Int Urol Nephrol 2017
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