We have designed bifunctional compounds capable of damaging HIV-1 Env irreversibly and permanently. Each compound is composed of two independent and covalently linked units. The first component is the recognition motif  , which is a protein, griffithsin, that binds non-covalently to the target molecule, HIV-1 Env; whereas the second unit, the ATCUN, corresponds to the effector motif  , which damages the target permanently. Such �metallo-griffithsin� is designed to be specifically target Env and introduce irreversible damage. The ATCUN is a short peptide, with sequence aa1-aa2-His, coordinating a Cu(II) or a Ni(II) atom that can be activated in the presence of oxidizing agents. Since the recognition and the effector motifs are covalently linked, the target protein is in the vicinity of these highly reactive species, and should selectively suffer irreversible damage. Our work represents an important step toward the development of new drugs for targeting HIV.

Metallomicrobicides: A smarter way to target HIV

243rd National Meeting (2012)

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