Target intelligence / Profile preview

Poly(ADP-ribose) Polymerase 5a (TNKS1)

Target
TNKS1
Molecular classification
Enzyme, Poly(ADP-ribose) polymerase (PARP), ARTD superfamily, Diphtheria toxin-like ADP-ribosyltransferases (ARTDs)
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Overview

Poly(ADP-ribose) polymerase 5a, also known as Tankyrase 1 (TNKS1), is an enzyme that catalyzes the transfer of ADP-ribose units to target proteins, regulating their function and stability. It plays critical roles in telomere maintenance, Wnt signaling activation, cell cycle progression, and DNA damage response. As a regulator of pathways central to cancer biology, particularly Wnt signaling, TNKS1 is an attractive target for anticancer drug development.

Other names
Tankyrase 1PARP5aARTD5TNKS
02

Mechanism of action

Inhibition of PARsylation activity, stabilization of negative regulators of Wnt signaling and telomere maintenance proteins

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Biological functions

Telomere maintenanceWnt signaling activationCell cycle regulationDNA damage responseGlucose metabolismMyogenesis
04

Disease associations

CancerCancer progression/metastasis
05

Safety considerations

Potential for bone loss due to role in bone homeostasisPotential for off-target effects due to redundancy with TNKS2

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