In recognition of and to commemorate Prof. Ōmura’s Nobel Prize in Physiology or Medicine in 2015, the Editorial Board of The Journal of Antibiotics has changed the name and the design of the JA Medal to the JA Ōmura Award. The first JA Ōmura Award for an article will be given for the outstanding paper entitled “Application of bacterial cytological profiling to crude natural product extracts reveals the antibacterial arsenal of Bacillus subtilis” by Kit Pogliano and colleagues at University of California San Diego [1]. In this article, the authors report the general usefulness of bacterial cytological profiling (BCP) for not only understanding the mechanism of action (MOA) but also identification of bioactive substances in crude extracts, which allowed for the identification of two distinct antibacterial activities from the culture broth of Bacillus subtilis, translation inhibition and membrane permeabilization.

As a result of the extensive use of antibiotics in the clinic, pathogenic bacteria have evolved resistance to nearly all classes of antibiotics, which poses serious threats to human health. It is therefore clearly important to identify antibacterial molecules with unique MOA. However, elucidation of MOA at the molecular level is one of the most challenging tasks in drug discovery, which generally requires multiple assays and substantial amounts of time. The winners’ group previously developed BCP, a rapid and powerful approach for identifying the cellular pathway affected by antibacterial molecules [2]. The cytological profiles of bacterial cells treated with each antibacterial drug, which are created by staining cells with multiple fluorescent dyes, successfully distinguished between inhibitors that affect different cellular pathways as well as different targets within the same pathway. In the award-winning paper, this technology was applied to identify multiple biological activities in crude natural product extracts, providing a new platform for screening for unique biological activity and guiding natural product extract fractionation. Furthermore, the authors offered an in situ version of BCP that works with strains grown on a solid medium plate. BCP is an exciting new technology for antibiotic research, and its application to the discovery of minor components possessing alternative MOAs in crude extracts, which are overlooked by traditional screening methods, is of high importance.

The 2017 winner of the JA Ōmura Award for reviews goes to a seminal and comprehensive overview on glycopeptide antibiotics, entitled “Glycopeptide antibiotics: Back to the future” authored by Matthew A. Cooper and coworkers at the University of Queensland [3]. A family of antibiotics with glycosylated tricyclic or tetracyclic heptapeptide cores are collectively called glycopeptide antibiotics (GPAs). Vancomycin, a founding member of GPAs, has been used as a ‘drug of last resort’ in the fight against many infections by Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA). Vancomycin was discovered in the 1950s by Eli Lilly & Co and continues the integral role in frontline therapy it has had for over half a century, even today. To overcome the drawbacks associated with vancomycin including the emergence of resistance, several new GPAs including semisynthetic ones have been developed. This review article comprehensively covers this evergreen topic and is considered one of the masterpiece reviews on GPAs, in addition to the article awarded the JA Medal last year on GPA biosynthesis [4].

The review begins with a history of vancomycin from discovery to its approval as a ‘certifiable antibiotic’ by the United States Food and Drug Administration (FDA) in 1958. Surprisingly, its chemical structure was not fully elucidated until 1982 and confirmed by X-ray crystallography in 1996. There are clinical limitations of vancomycin including its relatively poor pharmacokinetic properties and side effects. However, a dramatic rise in drug resistance to β-lactams due to the constant and extensive use of β-lactam antibiotics has made vancomycin re-emerge as a key weapon in the fight against β-lactam-resistant bacteria. Meanwhile, MRSA strains with reduced vancomycin susceptibility such as heterogeneous vancomycin intermediate (hVISA), vancomycin intermediate (VISA), and vancomycin resistant (VRSA) that acquired the enterococcal vanA operon gene were found in clinical practice, an issue that threatens its continued effectiveness. In this review article, the authors report the current state of development of the second generation of GPAs with improved pharmacokinetic and safety profiles. Teicoplanin is another naturally occurring GPA which is better tolerated than vancomycin, and applicable to outpatient therapy. Furthermore, semisynthetic lipoglycopeptide derivatives with improved properties such as telavancin, dalbavancin, and oritavancin have been developed and recently approved by the FDA. This review provides profound insights into further development of more effective GPAs against drug-resistant pathogens, and as such, it is a worthy recipient of the 2017 JA Ōmura Award.