Target intelligence / Profile preview

Pleckstrin homology domain-containing family O member 2 (PLEKHO2)

Target
PLEKHO2
Molecular classification
Pleckstrin homology (PH) domain-containing protein, Adapter protein, Other (not currently classified as receptor, ion channel, enzyme, transporter, transcription factor, or histone modifier)
01

Overview

Pleckstrin homology domain-containing family O member 2 (PLEKHO2) encodes an adapter protein containing a pleckstrin homology domain, which is predicted to participate in signal transduction, cell migration, and regulation of apoptotic processes. Dysregulation of PLEKHO2, often through decreased expression or loss (e.g., via miR-106b targeting), enhances colorectal cancer cell proliferation and invasion by abnormally activating MAPK signaling. PLEKHO2 is also mapped to the innate immune system and appears as a fusion partner in certain oncogenic gene fusions, suggesting wider roles in tumorigenesis. While it is studied as a mediator and possible therapeutic target, no direct drugs or inhibitors have been developed to date.

Other names
PP9099PP1628PLEKHQ1PH domain-containing family O member 2PH domain-containing family Q member 1PH domain-containing proteinpleckstrin homology domain-containing family Q member 1
02

Mechanism of action

Drugs and microRNAs (e.g., miR-106b) regulate PLEKHO2 via gene expression modulation, thereby affecting downstream cellular signaling (MAPK pathway) and cellular phenotypes like migration and proliferation

03

Biological functions

Signal transduction (modulates MAPK signaling pathways)Regulation of cell migration, invasion, and proliferation (notably in cancer cells)Apoptosis (predicted involvement in macrophage apoptotic processes)Immune response (associated with innate immune system pathways)
04

Disease associations

Cancer (especially colorectal cancer, implicated in cell migration and invasion via the MAPK axis)Liver sarcoma (association reported)Other (roles not well-established but possibly associated with additional cancers due to gene fusions)
05

Safety considerations

There are no direct safety or toxicity concerns associated with therapeutic targeting of PLEKHO2 in humans reported in public literature. The principal challenge is lack of direct pharmacological agents; concerns would relate to interfering with key cell signaling pathways involved in immunity and cancer progression
06

Interacting drugs

There are no widely established drugs that directly target PLEKHO2. Its modulation has been observed following drug or gene perturbation studies, but specific drug interactions are not documented in available datasets.
07

Biomarkers

Low or altered PLEKHO2 expression may serve as a biomarker in colorectal cancer, as its loss is linked to increased invasiveness and proliferationModulation by miR-106b and competing endogenous RNAs (ceRNAs) has biomarker relevance for tumor progression or response to targeted therapies

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