结核分枝杆菌的肽脱甲酰基酶抑制剂：合成、结构研究及生物学结果。
Peptide deformylase inhibitors of Mycobacterium tuberculosis: synthesis, structural investigations, and biological results.
作者信息
Pichota Arkadius, Duraiswamy Jeyaraj, Yin Zheng, Keller Thomas H, Alam Jenefer, Liung Sarah, Lee Gladys, Ding Mei, Wang Gang, Chan Wai Ling, Schreiber Mark, Ma Ida, Beer David, Ngew Xinyi, Mukherjee Kakoli, Nanjundappa Mahesh, Teo Jeanette W P, Thayalan Pamela, Yap Amelia, Dick Thomas, Meng Wuyi, Xu Mei, Koehn James, Pan Shi-Hao, Clark Kirk, Xie Xiaoling, Shoen Carolyn, Cynamon Michael
机构信息
Novartis Institute for Tropical Diseases, 10 Biopolis Road, #05-01 Chromos, Singapore 138670, Singapore.
出版信息
Bioorg Med Chem Lett. 2008 Dec 15;18(24):6568-72. doi: 10.1016/j.bmcl.2008.10.040. Epub 2008 Oct 14.
Bacterial peptide deformylase (PDF) belongs to a subfamily of metalloproteases catalyzing the removal of the N-terminal formyl group from newly synthesized proteins. We report the synthesis and biological activity of highly potent inhibitors of Mycobacterium tuberculosis (Mtb) PDF enzyme as well as the first X-ray crystal structure of Mtb PDF. Structure-activity relationship and crystallographic data clarified the structural requirements for high enzyme potency and cell based potency. Activities against single and multi-drug-resistant Mtb strains are also reported.
细菌肽脱甲酰酶（PDF）属于金属蛋白酶亚家族，催化从新合成的蛋白质中去除N端甲酰基。我们报告了结核分枝杆菌（Mtb）PDF酶高效抑制剂的合成及生物活性，以及Mtb PDF的首个X射线晶体结构。构效关系和晶体学数据阐明了高酶活性和细胞活性的结构要求。还报告了对单药耐药和多药耐药Mtb菌株的活性。
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