| Summary: | 碩士 === 國立中央大學 === 化學研究所 === 98 === Nanoparticles bearing surface-conjugated specific inhibitors are increasingly
being utilized for a number of bio-applications including identification, separation
and enhancement of desired proteins. These attractive bio-applications involve
specific adsorption and recognition; however, these are the major hindrances for
nanobiotechnology. To solve this question, we have investigated the effect of
nanoparticle surface displaying high affinity molecules, such as sialyltransferase
inhibitors.
Maintaining a reasonable affinity toward desired protein is generally a
prerequisite for proper design of nanoparticle-conjugated specific inhibitors. We
prepared sialyltransferase inhibitors, lithocholic acid derivatives with L-Asp or
NBD-L-Asp moiety, which have IC50 values at micromolar ranges. Next, magnetic
nanoparticle (iron oxide)-conjugated lithocholic acid derivatives, compounds
15~16, were synthesized via click chemistry.
Herein, we demonstrated that compounds 15~16 have the ability to identify, separate and enhance binding to the target alpha-2,3(N)-sialyltransferase, a glycol- and membrane-bound protein. The protein band (38 kDa) on SDS-PAGE derived from rat was confirmed by LC MS-MS analysis and proteomics searching. Extending these studies to crude cell lysate in vitro experiment, we found several interesting proteins including talin. Further investigation of talin toward metastasis in cancer is in progress.
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