Target intelligence / Profile preview

Phosphoinositide-dependent protein kinase 1 (PDK1)

Target
PDK1
Molecular classification
Enzyme, Kinase, AGC kinase
01

Overview

Phosphoinositide-dependent protein kinase 1 (PDK1), also known as PDPK1, is a serine/threonine kinase that plays a central role in cell signaling, growth, and survival. It acts as a "master" upstream kinase that phosphorylates and activates several members of the AGC family of protein kinases, including Akt/PKB, S6 Kinase(s), and RSK. PDK1 functions downstream of PI3-Kinase signaling and its activity is crucial for regulating cell size and development. Small-molecule inhibitors have been developed targeting either the ATP-binding pocket or allosteric sites.

Other names
PDPK1
02

Mechanism of action

Competitive inhibition at ATP-site or allosteric modulation

03

Biological functions

Cell signalingCell growth regulationCell survivalmTOR pathway activationAuxin transport regulation
04

Disease associations

Cancer
05

Interacting drugs

Small-molecule inhibitors (ATP-binding pocket)

1 more in the full profile.

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