Potent Inhibition of HIV-1 Entry with a Chemically Programmed Antibody Aided by an Efficient Organocatalytic Synthesis

An organocatalytic conspiracy: Organocatalysis and an organocatalytic antibody conspire to create a novel HIV‐1 entry inhibitor. A D‐proline catalyzed aldol reaction was used to set the key stereochemistry of CCR5 inhibitor, Aplaviroc, prior to introduction as a targeting unit for chemical programming of aldolase antibody 38C2. The resulting antibody conjugate was a potent inhibitor of HIV‐1 and SIV entry.