Quadriga is developing QBS72S, a novel, first-in-class chemotherapeutic agent that is transported by L-type Amino Acid Transporter 1 (LAT1) across the blood brain barrier (BBB) and into rapidly growing cancer cells.
Composition
QBS72S is comprised of nitrogen mustard, a well understood DNA crosslinking moiety, covalently fused to a non-natural amino acid scaffold – resulting in the structural features of a selective LAT1 substrate.
Composition
QBS72S is comprised of, nitrogen mustard, a well understood DNA crosslinking moiety, covalently fused to a non-natural amino acid scaffold – resulting in the structural features of a selective LAT1 substrate.
Accessing the Brain
LAT1 is highly expressed at the blood-brain barrier (BBB) and on the surface of rapidly dividing cancer cells, facilitating transport of QBS72S into the brain and enabling the potential treatment of cancer.
The “Trojan Horse” Approach
Many aggressive solid tumors and hematologic malignancies overexpress the LAT1 transporter to increase nutrient intake and fuel growth; high LAT1 expression is often correlated with poor prognosis1. QBS72S acts as a ‘Trojan Horse’ by mimicking LAT1-transported aromatic amino acids, facilitating its intracellular uptake via LAT1. Once inside the cell, QBS72S can exert its desired oncolytic effect through irreversibly interacting with DNA of the rapidly dividing tumor cells.
The “Trojan Horse” Approach
Many aggressive solid tumors and hematologic malignancies overexpress LAT1 to increase nutrient intake and fuel growth. QBS72S acts as a ‘Trojan Horse’ by mimicking LAT1-transported aromatic amino acids, facilitating its intracellular uptake through the LAT1 transporter of cancer cells. Once inside the cell, QBS72S can exert its desired oncolytic effect through irreversibly interacting with DNA of the rapidly dividing tumor cells.
