Target intelligence / Profile preview

Phosphodiesterase 11A1 (PDE11A1)

Target
PDE11A1
Molecular classification
Enzyme, Phosphodiesterase, 3',5'-cyclic nucleotide phosphodiesterase
01

Overview

Phosphodiesterase 11A1 (PDE11A1) is a splice variant of the PDE11A enzyme, a member of the phosphodiesterase family that hydrolyzes the secondary messengers cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) [1, 4]. As a dual-specificity enzyme, PDE11A1 regulates the intracellular levels of both cyclic nucleotides, thereby modulating signaling pathways critical for cellular homeostasis and endocrine regulation [1, 7]. This specific isoform is primarily expressed in the prostate, testis, and skeletal muscle, distinguishing it from other variants like PDE11A4 which is found in the brain [4, 5]. Mutations in the PDE11A gene are clinically significant as they are linked to the development of adrenocortical tumors and Cushing syndrome, where impaired PDE activity results in elevated cAMP levels [4, 8]. Furthermore, PDE11A1 is involved in physiological processes such as spermatogenesis and has been studied as a potential biomarker in various cancers [4, 7]. From a pharmacological perspective, PDE11A is a known off-target of the drug tadalafil, which may lead to side effects like myalgia due to its expression in skeletal muscle [10]. Research continues to explore the potential of targeting PDE11A for treating endocrine disorders and certain types of cancer [1, 10].

Other names
PDE11APhosphodiesterase 11AcAMP and cGMP-dependent phosphodiesterase 11A
02

Mechanism of action

Inhibition of the catalytic activity of the enzyme, preventing the hydrolysis of cyclic nucleotides (cAMP and cGMP), thereby increasing their intracellular concentrations and downstream signaling.

03

Biological functions

Signal transductioncAMP hydrolysiscGMP hydrolysisRegulation of intracellular signalingSpermatogenesis
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Disease associations

Cushing syndromeAdrenocortical tumorProstate cancerTesticular cancerGlioblastoma
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Safety considerations

MyalgiaBack painPotential endocrine disruption
06

Interacting drugs

Tadalafil
07

Biomarkers

PDE11A mutationPDE11A expression level

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