Thienopyrimidinone derivatives that inhibit bacterial tRNA (guanine37-N1)-methyltransferase (TrmD) by restructuring the active site with a tyrosine-flipping mechanism

• المؤلفون الرئيسيون: Zhong, Wenhe, Pasunooti, Kalyan Kumar, Balamkundu, Seetharamsing, Wong, Yee Hwa, Nah, Qianhui, Gadi, Vinod, Gnanakalai, Shanmugavel, Chionh, Yok Hian, McBee, Megan E., Gopal, Pooja, Lim, Siau Hoi, Olivier, Nelson, Buurman, Ed T., Dick, Thomas, Liu, Chuan Fa, Lescar, Julien, Dedon, Peter C.
• مؤلفون آخرون: School of Biological Sciences
• التنسيق: مقال
• اللغة: English
• منشور في: 2021
• الموضوعات: Science::Biological sciences; Inhibitors; Peptides and Proteins
• الوصول للمادة أونلاين: https://hdl.handle.net/10356/148942
• المؤسسة: Nanyang Technological University

Among the >120 modified ribonucleosides in the prokaryotic epitranscriptome, many tRNA modifications are critical to bacterial survival, which makes their synthetic enzymes ideal targets for antibiotic development. Here we performed a structure-based design of inhibitors of tRNA-(N1G37) methyltra...