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CXCR4 heteromers

Conventional approach of blocking CXCR4 pathway based on existing hypothesis

Existing hypothesis: CXCR4 exists as monomers/homomers with identical signals

Real-world evidence of intracellular signaling enhancement by CXCR4 heteromers

CXCR4 heteromers

When both agonists(CXCL12 and Agonist X) were incubated, intracellular signal was substantially enhanced compared to either agonist alone. (Fig.1)

CXCR4 heteromers

No enhanced intracellular signal was detected when both agonists(CXCL12 and Agonist X) were incubated to the cell lines expressing either CXCR4 or GPCRx alone. (Fig.2, 3)

CXCR4 heteromers

No enhanced intracellular signal was detected when both agonists(CXCL12 and Agonist X) were incubated to the cell lines expressing either CXCR4 or GPCRx alone. (Fig.2, 3)

Novel hypothesis of CXCR4 heteromers and their intracellular signaling enhancement

CXCR4 heteromers

CXCR4 forms heteromers with certain GPCRs resulting in distinct, often enhanced signals

Real- world evidence of intracellular signaling inhibition by CXCR4 / GPCRx inhibitors

CXCR4 heteromers

In the absence of antagonist, both agonists(CXCL12 and Agonist X) induced an enhanced intracellular signal compared to when each agonist was treated alone. (Fig. 1)

CXCR4 heteromers

The enhanced intracellular signal was inhibited differently depending on the types and combinations of compounds that were treated. (Fig.2, 3, 4)

Existing CXCR4 antagonist did not show complete inhibition when CXCR4 heteromers were present. (Fig.2)

CXCR4 heteromers

The enhanced intracellular signal was inhibited differently depending on the types and combinations of compounds that were treated. (Fig.2, 3, 4)

CXCR4 heteromers

The enhanced intracellular signal was inhibited differently depending on the types and combinations of compounds that were treated. (Fig.2, 3, 4)

Specific combinations of antagonists completely suppressed the enhanced signals. (Fig.4)

Innovative approach of blocking CXCR4 pathway based on novel hypothesis

CXCR4 heteromers
CXCR4 heteromers

Treatment of CXCR4 inhibitors alone results in limited clinical efficacy.

CXCR4 heteromers
CXCR4 heteromers

Appropriate combination of inhibitors are needed for effective blockade of CXCR4 pathway.

CXCR4 heteromers