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Bacterial peptide deformylase inhibitor PMT analogs inhibit cancer cell growth by interacting with human peptide deformylase |
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| Authors: | Won-Je Kim Woo Sung Son Kyoung-Seok Ryu Seung-Kyu Lee Kwang-Hyun Choi Jong-Sun Lee Bong-Jin Lee |
| Institution: | 1. College of Pharmacy, Seoul National University, Seoul, 151-742, Korea 2. College of Pharmacy, CHA University, Seongnam, Gyeonggi-do, 487-010, Korea 3. Division of Magnetic Resonance, Korea Basic Science Institute, Ochang Campus, Seoul, Chungcheongbuk-Do, 363-883, Korea 4. Promeditech Ltd, Seoul National University, Seoul, 151-742, Korea |
| Abstract: | Potent inhibitors of human peptide deformylase(HsPDF)were screened using known PMT analog inhibitors of bacterial peptide deformylase.Forty-three species of PMT analogs that are non-peptidyl bacterial PDF inhibitors like actinonin were selected using virtual screening GOLD.Ten species out of 43 that could bind to HsPDF were selected and their antitumor activities were tested.Among them,four species(PMT-172,PMT-173,PMT-199,and PMT-201)showed excellent growth inhibition of cancer cell in the MTT assay.HsPDF-PMT binding was confirmed through a1H-CPMG-T2filter NMR experiment leading to a significant change in peak intensity for PMT-172 and PMT-199.These results suggest that PMT analogs could possibly interact with HsPDF and be a novel anticancer drug candidate. |
| Keywords: | Bacterial peptide deformylase inhibitor Homo sapience peptide deformylase PMT analogs Anticancer effect CPMG T filter Docking simulation |
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