Nano-Combinatorial Chemistry Approach for Nanomedicine Research
Bing Yan
St. Jude Children’s Research Hospital, Memphis, TN, U.S.A.
E-mail address: [email protected]
Nanomaterials are being investigated for their applications in medicine in addition to their wide
potential use in industry and our daily life. However, the binding affinity to specific target and the
ADMET properties of nanoparticles in vivo are largely unknown and cannot be controlled.
Furthermore, due to their small size and large surface areas, nanoparticles bind biomolecules may
enter cells, and induce toxicity in cells and in animals.
Due to the large surface areas on nanoparticles, chemistry modification of their surface may
have a major impact on their bioactivity. To test this hypothesis, we designed and synthesized carbon
nanotube and gold nanoparticle combinatorial libraries and studied the possible enhancement of
target binding of a ligand through multi-valency effect and the modified biological activities. The
actual synthesis posed challenges on reaction monitoring and product characterization on
nanoparticle’s surface. We developed a series of analytical techniques and methods to assist the
synthesis of nanoparticle libraries. Biological screening results showed that the selected second
ligand can enhance the target binding of the primary ligand. Surface chemistry diversity can also
modulate nanoparticle’s interactions with proteins, and control their cellular activities. Biocompatible
or enzyme-specific nanoparticles can be selected and surface structure-activity relationship can be
elucidated using this approach.
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