L-Ala-BPA is a boron delivery agent. L-Ala-BPA is transported into tumor cells via PEPT1/2 and LAT-1 (SLC7A5) pathways and is rapidly cleaved systemically by endogenous proteases including FAP to yield L-BPA. L-Ala-BPA shows antitumor activity and can be used for the research of Boron Neutron Capture Therapy (BNCT) [1].
In Vivo, L-Ala-BPA (200 mg/kg; i.v.; single bolus dose; 90 minutes prior to neutron irradiation) plus 12-minute neutron irradiation produces complete, durable tumor control in syngeneic CT26 colon carcinoma-bearing BALB/c mice[1].
In Vitro, L-Ala-BPA (2 h) mediates dose-dependent boron uptake in AsPC-1 cells via the PEPT1/2 transport pathway[1]. L-Ala-BPA (2 h) mediates dose-dependent boron uptake in FaDu cells via the LAT-1 transport pathway[1].
References:
[1]. Samkeliso Dlamini, et al. Highly Soluble Prodrug 4-1-Boronophenylalanine (L-BPA) Containing Dipeptide Exhibits Notable Tumor Suppression whi Vaccine Effect And Abscopal Tumor Suppression Post Neutron Irradiation Treatment. April 202686(7_Supplement):4641-4641.
In Vivo, L-Ala-BPA (200 mg/kg; i.v.; single bolus dose; 90 minutes prior to neutron irradiation) plus 12-minute neutron irradiation produces complete, durable tumor control in syngeneic CT26 colon carcinoma-bearing BALB/c mice[1].
In Vitro, L-Ala-BPA (2 h) mediates dose-dependent boron uptake in AsPC-1 cells via the PEPT1/2 transport pathway[1]. L-Ala-BPA (2 h) mediates dose-dependent boron uptake in FaDu cells via the LAT-1 transport pathway[1].
References:
[1]. Samkeliso Dlamini, et al. Highly Soluble Prodrug 4-1-Boronophenylalanine (L-BPA) Containing Dipeptide Exhibits Notable Tumor Suppression whi Vaccine Effect And Abscopal Tumor Suppression Post Neutron Irradiation Treatment. April 202686(7_Supplement):4641-4641.