Target intelligence / Profile preview

Inactive tyrosine-protein kinase 7 (PTK7)

Target
PTK7
Molecular classification
Receptor tyrosine kinase, Pseudokinase, Cell adhesion molecule, Receptor
01

Overview

Inactive tyrosine-protein kinase 7 (PTK7), also known as Colon carcinoma kinase 4 (CCK4), is a member of the receptor tyrosine kinase (RTK) family that lacks detectable catalytic activity, classifying it as a pseudokinase (UniProt P35091). Despite its lack of kinase activity, PTK7 functions as a critical scaffold and co-receptor in the non-canonical Wnt signaling pathway, where it regulates cell polarity, migration, and tissue morphogenesis during embryonic development (NCBI Gene: 5754). In adult tissues, PTK7 expression is generally low, but it is significantly upregulated in various malignancies, including lung, breast, and colorectal cancers, where it is associated with increased tumor invasiveness and poor prognosis (PMID: 33430931). This differential expression profile makes PTK7 an attractive target for therapeutic intervention, particularly for antibody-drug conjugates (ADCs). For example, cofetuzumab pelidotin (PF-06647020) is an ADC designed to bind PTK7 and deliver a potent microtubule inhibitor directly into cancer cells (PMID: 28455364). Beyond its role as a drug target, PTK7 is also being investigated as a biomarker for cancer stem cells and metastatic potential in solid tumors.

Other names
Colon carcinoma kinase 4CCK4Protein-tyrosine kinase 7CCK-4
02

Mechanism of action

Antibody-drug conjugate (ADC) targeting PTK7 to deliver cytotoxic payloads (e.g., Auristatin-0101) to tumor cells; potential modulation of non-canonical Wnt signaling pathways.

03

Biological functions

Signal transductionCell migrationCell polarityWnt signaling pathwayAngiogenesisEmbryonic developmentPlanar cell polarity
04

Disease associations

CancerColorectal cancerLung cancerBreast cancerOvarian cancerAcute myeloid leukemiaMetastasis
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Safety considerations

NeutropeniaGastrointestinal toxicityAlopeciaPotential off-target effects in normal tissues expressing PTK7 (e.g., lung, esophagus)
06

Interacting drugs

Cofetuzumab pelidotin

1 more in the full profile.

07

Biomarkers

PTK7 protein expression (IHC)PTK7 mRNA expression

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