Journal of Proteomics & Bioinformatics
Open Access
ISSN: 0974-276X
+44 1223 790975
ISSN: 0974-276X
+44 1223 790975
Ho Jeong Kwon
Scientific Tracks Abstracts: J Proteomics Bioinform
Unbiased phenotypic based screening of small molecules has provided a number of unique small molecules with unknown target proteins and modes of action in biological context. Chemical proteomics is a new integrated research engine that bridges over a hurdle to identify target proteins of biologically active small molecules for functional studies of proteome and drug discovery. Accordingly, our effort has focused on the identification of target proteins that play a critical role in angiogenesis using new angiogenesis inhibitors. In particular, we have established phage display biopanning which is an affinity-based target protein selection method from human cDNA libraries expressed on the surface of bacteriophages using immobilized small molecules as ligands. With application of this method, we recently identified Ca2+/calmodulin (Ca2+/CaM) as a cellular target of a new curcumin analog, HBC (4-{3,5-bis-[2-(4-hydroxy-3-methoxyphenyl)ethyl]-4,5-dihydropyrazol-1 -yl}benzoic acid). HBC potently inhibited angiogenesis and suppressed the expression of HIF-1α, a key regulator of angiogenesis, at the translational level via antagonizing of Ca2+/CaM function. In addition, HBC enhanced the anti-angiogenic activity of known HIF-1 inhibitors, suggesting that Ca2+/CaM is an emerging target for cancer chemotherapy. Taken together, these results demonstrate that chemical proteomics is a powerful means for identification of target protein of bioactive small molecules and discovery of new cancer biomarker.
Ho Jeong KWON has completed his Ph.D from University of Tokyo and postdoctoral studies from Harvard University. He is professor, Dept. of Biotechnology, Yonsei University, Korea and director of chemical genomics national research laboratory. He served as a council member of HUPO (05-08), the president of KHUPO (10-11) and has been serving a council member of AOHUPO (10-present). He has published more than 126 papers in reputed journals and serving as editorial board member of repute journals; J. Proteomics, Int. J. Proteomics, J. of Proteomics & Bioinformatics, J. Antibiotics, Oncology Research, J. Microbiology & Biotechnology and BMB reports.