| Info. | Vol.3 - No.3 (2009.09.20) |
|---|---|
| Title | Protein Chip-based Dipeptidyl Peptidase IV Assay System |
| Authors | Eung-Yoon Kim2,3 & In-Cheol Kang1,2,3 |
| Institutions | 1Department of Biological Science, Hoseo University 2BioChip Research Center, Hoseo University 3Innopharmascreen Inc., Asan 336-795, Korea Correspondence and requests for materials should be addressed to I.C. Kang (ickang@hoseo.edu) |
| Abstract | Dipeptidyl peptidase IV (DPP-IV) is known to be a serine amino-peptidase that cleaves N-terminal X-Ala or X-Pro from target polypeptides. The enzyme plays a pivotal role in fatal diseases such as diabetes mellitus, obesity, tumor growths, and HIV infection. Inhibition of DPP-IV is currently being explored as a novel therapy for type II diabetes. Thus, we have developed a protein chip-based DPP-IV assay system for the screening of enzyme inhibitors. A biotin-labeled Gly-Pro sequence as a substrate was designed for immobilization on a ProteoChipTM. DPP-IV was incubated with the substrate-immobilized ProteoChip. Also, Cy5-labeled streptavidin was applied to the chip, and the fluorescence intensities on the spots were detected using a laser scanner. DPP-IV activity on the chip was determined using data obtained from the fluorescence intensities. Galvus (vildagliptin) and virtually screened leads were tested using the DPP-IV assay chip for identification as novel diabetes inhibitors. |
| Keyword | DPP-IV, ProteoChipTM, Protease assay, Diabetes inhibitor, Galvus |
| PDF File |
|
