Inhibition of HIV fusion with multivalent gold nanoparticles.
The design and synthesis of a multivalent gold nanoparticle therapeutic is presented. SDC-1721, a fragment of the potent HIV inhibitor TAK-779, was synthesized and conjugated to 2.0 nm diameter gold nanoparticles. Free SDC-1721 had no inhibitory effect on HIV infection; however, the (SDC-1721)-gold nanoparticle conjugates displayed activity comparable to that of TAK-779. This result suggests that multivalent presentation of small molecules on gold nanoparticle surfaces can convert inactive drugs into potent therapeutics.
Bowman
Mary-Catherine
MC
Department of Medicine, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599-7435, USA.
Ballard
T Eric
TE
Ackerson
Christopher J
CJ
Feldheim
Daniel L
DL
Margolis
David M
DM
Melander
Christian
C
D000577:Amides / Q000737:chemistry / Q000494:pharmacology*; D006046:Gold / Q000737:chemistry* / Q000494:pharmacology*; D023581:HIV Fusion Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D015658:HIV Infections / Q000188:drug therapy; D015497:HIV-1 / Q000502:physiology; D053768:Metal Nanoparticles / Q000737:chemistry* / Q000627:therapeutic use; D000644:Quaternary Ammonium Compounds / Q000737:chemistry / Q000494:pharmacology*
D000577:Amides; D023581:HIV Fusion Inhibitors; D000644:Quaternary Ammonium Compounds; D006046:Gold; C119369:TAK 779