G-protein coupled receptors (GPCRs) are membrane proteins that make cells respond to chemical signals like hormones.
Tuning GPCR activities up or down can use our body's cellular activities to treat diseases. That's why 30% of all approved drugs target GPCRs.
75% of the 400 GPCRs remain undrugged. Many control important disease-treating biological programs.
Off-target toxicity
Small molecules often have off-target activity for structurally similar GPCRs, leading to side effects.
Metabolic toxicity
Small molecules can also be processed by the body to yield toxic metabolites.
Lack of efficacy
Small molecules often cannot be found to affect the activity of a GPCR of interest, such as targets that normally respond to large protein-based signals.
Naturally strong binders that inactivate
Nature evolved antibodies as our body's own drugs to selectively and potently inactivate pathogens.
Proven drugs, but rare for GPCRs
7 of the top 10-selling drugs are engineered antibodies.
However, out of 100 antibody drugs, only 2 target GPCRs.
Antibody GPCRs drugs limited to blockers until now
It's hard enough finding a GPCR blocker. It's hard to bind a GPCR in just the right way to activate it.
There is not a single antibody GPCR activator drug approved or in clinical trials.
Abalone Bio's Functional Antibody Selection Technology platform (FAST) combines engineered living cells and data-driven computation to identify antibodies that functionally affect the GPCR target- including activators.