Target intelligence / Profile preview

Cyclin-dependent kinase 16 (CDK16)

Target
CDK16
Molecular classification
Enzyme, Serine/threonine-protein kinase, Cyclin-dependent kinase family (PCTAIRE subfamily)
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Overview

Cyclin-dependent kinase 16 (CDK16), also called PCTAIRE1 or PCTK1, is an atypical member of the cyclin-dependent kinase family that functions as a serine/threonine-protein kinase. It is activated via interaction with cyclin Y and 14-3-3 proteins in a phosphorylation-dependent manner. CDK16 is highly expressed in the testis and brain, where it regulates key processes such as spermatogenesis and neurite outgrowth; it also influences vesicle trafficking, exocytosis, muscle differentiation, and glucose homeostasis. Genetic knockout studies demonstrate its essential role in male fertility: CDK16 deficiency leads to impaired sperm motility and morphology. CDK16 is implicated in cancer cell proliferation and migration, and targeting its ATP-binding site with kinase inhibitors such as dabrafenib, rebastinib, and indirubin E804 offers pharmacological intervention potential. Its structural and mechanistic properties distinguish it from classical CDKs, notably its unique PCTAIRE cyclin-binding motif and requirement for cyclin partners for full activity. In clinical and laboratory settings, CDK16 is under exploration as both a therapeutic target in cancer and a biomarker in reproductive health.

Other names
PCTAIRE1PCTK1PCTAIREPCTGAIREFLJ16665Cell division protein kinase 16PCTAIRE-motif protein kinase 1Serine/threonine-protein kinase PCTAIRE-1testis secretory sperm-binding protein Li 224n
02

Mechanism of action

Kinase inhibition (by drugs targeting the ATP-binding pocket, e.g. both type I and II kinase inhibitors; dabrafenib and rebastinib specifically stabilize inactive conformations of CDK16)

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Biological functions

Cell cycle regulationSpermatogenesisNeurite outgrowthVesicle traffickingExocytosis and vesicle transportGlucose homeostasisMuscle differentiation
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Disease associations

Cancer (proliferation, migration, drug resistance)Infertility (male, due to impaired spermatogenesis)
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Safety considerations

Potential impact on fertility (e.g., risk of male infertility due to role in spermatogenesis)Off-target effects due to structural similarity with other CDKsLack of fully selective inhibitors may affect other kinases leading to unwanted toxicity
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Interacting drugs

Dabrafenib

2 more in the full profile.

07

Biomarkers

Expression levels of CDK16 (potential cancer and male infertility biomarker)Altered phosphorylation states (potential for monitoring activation)

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