Imaging and inhibition of key cell cycle regulator (EBNA1/Plk1/Cyclin(s))
A specific and selective agent for both imaging and targeting of the virus-associated tumor has not been available in the literature currently. One of the direction in my group is going to design and synthesis some dual bioprobe which available for imaging and inhibition of dimerization of EBNA1 in vitro.
EBNA1-specific small molecule (JLP2) had been synthesised with strong binding and inhibition on the dimerization of EBNA1 in vitro, JLP2 may be used as a selective luminescent agent for the imaging and inhibition of EBV-latently-infected cancer cells. (Chem. Commun., 2014, 50, 6517)
Cyclin(s) and Plk1, involved in many key steps throughout mitosis, is found to be of great important in cancer treatment since its activity appears to be limited to mitosis in proliferating cells. However, the lack of selective small-molecule inhibitors of the kinase remains a major obstacle to further elucidate its precise functions. For instance, using anticancer agents that target microtubules may engender various adverse effects partially because of the diverse functions of microtubules in the cell. To date, only few small molecules can show the very specificity to Cyclin A/D or Plk1 or Plk1 for imaging and inhibition. In my group, we are going to develop a new generation of lanthanide materials to achieve the goal – imaging and anti-tumor. It is hoped that the success in research could also lead to the success in practice, thereby providing more powerful tools to get a more complete picture of the role of Cyclin A/D and Plk1.
The antenna efficiency of complexes is increased upon the binding of the Cyclin A and the long range effect was observed that the emission enhancement is affected by the bulk medium of the protein. (Dalton Trans., 2013, 42, 13495; Chem. Commun., 2011, 47, 8052)
Our newly developed water soluble, cell permeable and highly visible to NIR emissive (via near-infrared excitation) lanthanide material as a dual bioprobe for Cyclin D imaging and inhibition in vitro. (J. Mat. Chem. B, 2014, 84.)
Tailored made for Plk1 multi-tasking bio-probe (Por-P2) have been synthesized and gave the real time signaling towards Plk1 in-vitro and also shown the significance cell deaths (dark and light) with the interruption of cell mitosis after Plk1 binding in cancer cell specify. (Org. Bio. Chem., 2014, 2, 84-91)