Target intelligence / Profile preview

Connector enhancer of kinase suppressor of Ras 1 (CNKSR1)

Target
CNKSR1
Molecular classification
Adapter/scaffold protein, Other (specifically a scaffold protein, not a classic enzyme, receptor, or channel)
01

Overview

Connector enhancer of kinase suppressor of Ras 1 (CNKSR1) is a scaffold/adaptor protein encoded by the *CNKSR1* gene in humans. It contains multiple protein-protein interaction domains (PDZ, PH, and SAM domains) and serves as a critical mediator in receptor tyrosine kinase signaling by facilitating the assembly and localization of various signaling proteins, especially in the RAS/RAF/MAPK pathway. CNKSR1 can act as an effector for Rho and Ras GTPase pathways, controlling cellular processes such as proliferation via positive regulation of EGFR and HER2 phosphorylation and crosstalk with downstream effectors including AKT and ERK. It is implicated as a regulator in oncogenic signaling and has associations with neurological diseases, but is not currently an established therapeutic target in the sense of frequently targeted enzymes or receptors

Other names
CNKSR1CNKCNK1connector enhancer of KSR 1hCNK1KSRCNK homolog protein 1connector enhancer of KSR-like
02

Mechanism of action

Inhibition of scaffold function and membrane localization via PH-domain inhibition (for PHT-7.3)

03

Biological functions

Signal transductionRegulation of RAF and MAPK pathwayCell proliferationProtein-protein interaction
04

Disease associations

Cancer (oncogenic signaling)Neurological disorders (autism spectrum disorder, epilepsy)
05

Safety considerations

None documented in clinical contextpotential challenges involve pathway complexity and network redundancy (general to scaffold protein targeting)
06

Interacting drugs

PHT-7.3 (experimental inhibitor)

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