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Applications of the revolving motor
Published in Peixuan Guo, Zhengyi Zhao, Biomotors: Linear, Rotation, and Revolution Motion Mechanisms, 2017
The method described here has general applications in other biological systems. In fact, the first drug approved to treat multidrug-resistant tuberculosis, bedaquiline (Lakshmanan and Xavier, 2013), acts on ATP synthase which is a multisubunit biomotor (Figure 10.2c) (Watanabe et al., 2014; Yasuda et al., 1998; Kinosita et al., 1998; Stock et al., 1999; Boyer, 1999; Adachi et al., 2000; Hara et al., 2000; Masaike et al., 2000; Wada et al., 2000; Okazaki and Hummer, 2013; Ito et al., 2013; Arai et al., 2014). Although this drug's inventors were not aware of the concept of targeting multisubunit complexes, the success of this drug supports the notion of using the multisubunit complex as a potent drug target. Cancer or bacterial mutant multisubunit ATPase can also be used as targets. Drug developers can simply check the published literature and find the multisubunit machine as a drug target. For cancer treatment, the key is to find multisubunit machines with mutations (Pi et al., 2016).
Carbon nanomaterials: a new way against tuberculosis
Published in Expert Review of Medical Devices, 2019
Flavio De Maio, Valentina Palmieri, Marco De Spirito, Giovanni Delogu, Massimiliano Papi
Interestingly, RR-TB and MDR-TB treatments require regimens with a duration of 18–20 months with injectable agents, such as kanamycin and capreomycin, which are not recommended. Indeed, recent evidences indicate improve effectiveness of oral regimens against MDR-TB, based on the use of three drugs: fluoroquinolones (levofloxacin or moxifloxacin), bedaquiline and linezolid. Conversely, a shorter MDR-TB regimen foresees 9–12 months treatment with a daily injection for at least 4 months. Further anti-TB regimens are based on at least four agents in the first 6 months and three thereafter, but the duration of the therapy should be adjusted to patient response [10,25].
Syntheses and structural characterization of metal complexes of 4-(naphthalen-1-yl)-1-(quinolin-2-yl)methylene)thiosemicarbazide: their in-vitro screening studies for antitubercular activity
Published in Journal of Coordination Chemistry, 2022
Pooja Lokesh Hegde, Krishna Naik, Satish S. Bhat, Sabiha A. Shaikh, Ray J. Butcher, Naveen S., N. K. Lokanath, Vidyanand K. Revankar
Recently, molecules containing a quinoline core are attracting interest in the field of TB due to the clinical use of some quinoline derivatives like ciprofloxacin, mefloquine, bedaquiline (also called TMC-207) as anti-TB drugs (Figure 1) [19,20]. Bedaquiline has entered phase-III clinical trials and was found effective against the highly resistant form of tuberculosis strain [21]. A mechanistic study of bedaquiline revealed that it inhibits the proton pump of M. tuberculosis ATP synthase [22]. Quinolines and their derivatives also have other pharmaceutical applications as anticancer [23], antimalarial [24], antimicrobial [25], and anti-inflammatory [26] agents.