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Oxford Drug Design in Chemistry World

8 March 2018

Oxford Drug Design has contributed to an article entitled "Countdown to the last antibiotic" in the March edition of Chemistry World. The article, written by science writer and lecturer Clare Sansom, focuses on where the next generation of antibiotics might come from and describes many of the barriers faced by those working in the field. The major role of small biotech companies, following the withdrawal of many big pharma companies from antibiotics R&D, is a feature of the article, illustrated by the innovative work at Oxford Drug Design to identify new classes of antibiotics with novel mechanisms of action.

N-Leucinyl Benzenesulfonamides as LeuRS Inhibitors

18 January 2018

ODD scientists and collaborators have published a research paper describing the discovery of a new class of aminoacyl-tRNA synthetase inhibitors, N-Leucinyl benzenesulfonamides. The binding of inhibitors to the enzyme was measured by using isothermal titration calorimetry. This provided information on enthalpy and entropy contributions to binding, which, together with docking studies, were used for structure–activity relationship analysis. Enzymatic assays revealed that N-leucinyl benzenesulfonamides display remarkable selectivity for E. coli leucyl-tRNA synthetase compared to S. aureus and human orthologues. The simplest analogue of the series, N-leucinyl benzenesulfonamide, showed the highest affinity against E. coli leucyl-tRNA synthetase and also exhibited antibacterial activity against Gram-negative pathogens, which renders it as a promising template for antibacterial drug discovery.
Read the full article published in ACS Medicinal Chemistry Letters

Oxford Drug Design attends Medicines Discovery Catapult’s Antimicrobial Resistance Workshop

16 January 2018

Dr. Michael Charlton presented a review of literature analyses of the physical properties of antibacterial compounds. This included an emphasis on our own work, extending past studies to include a much greater number of antibacterial compounds, which shows that the properties of antibacterials are not significantly different from non-antibacterial compounds. Michael touched on how we are extending the work with machine learning studies combined with our in-house ElectroShape compound descriptors.
The workshop was attended by about 75 delegates from across industry and academia and consisted of lectures, panel discussions and round-table discussions spread over a day-and-a-half. For more information, or a copy of Michael’s slides, please Contact Us

CARTNET Begins - Oxford Drug Design starts work on AMR training network

1 January 2018

Oxford Drug Design has started work on a new 3.4 Million Euro Horizon 2020 Marie Curie European Training Network - CARTNET, “Combating Antimicrobial Resistance Training Network”.
CARTNET brings together 13 academic and industrial research groups from 8 countries and will contribute to delivering solutions to the challenges of bacterial infectious diseases that affect both humans and animals.
Oxford Drug Design will use its state-of-the-art drug discovery tools to optimize existing inhibitors of the novel class of antibacterial targets, histidine kinases, and to aid the discovery of new ones. The ultimate aim is to develop antibacterial compounds with a good resistance profile as candidate novel antibiotics.
1. The project has received funding from the European Union’s Horizon 2020 research and innovation programme under the Marie Sklodowska-Curie grant agreement No 765147.

Oxford Drug Design present on novel LeuRS inhibitors at aaRS2017

6 November 2017

Dr. Michael Charlton and Dr. Grace Edmund recently reported our work in the design of novel compounds to target the synthetic active site of Leucyl-tRNA synthetase (LeuRS), responsible for the aminoacylation reaction. The critical role of this site presents a significant barrier to the development of viable mutations and makes it an attractive target for antibacterial drug discovery.
Our presentation showcased our low molecular weight series of inhibitors that bind strongly to LeuRS without the need for an adenosine mimic. The compounds are good inhibitors of Gram-negative enzymes and have promising antimicrobial activity.
We also presented a poster outlining our work on using the Molecular Mechanics/Generalized Born – Volume Integral (MM/GB-VI) approach to predict ligand-protein binding affinities for a set of E. coli LeuRS inhibitors. 

Oxford Drug Design win EU support for antibacterial research 

10 October 2017

The European Commission has awarded 3.4 Million Euro under the Horizon 2020 programme to a new Marie Curie European Training Network - CARTNET, “Combating Antimicrobial Resistance Training Network”, in which Oxford Drug Design is a consortium partner.
CARTNET brings together 13 academic and industrial research groups from 8 countries and will contribute to delivering solutions to the challenges of bacterial infectious diseases that affect both humans and animals.
This award is further recognition of the innovation that Oxford Drug Design is bringing to the search for new antibacterials. Oxford Drug Design will use its state-of-the-art drug discovery tools to optimizing existing inhibitors of the novel antibacterial target, histidine kinase, and the discovery of new ones. The ultimate aim is to develop antibacterial compounds with a good resistance profile as candidate novel antibiotics.
The project has received funding from the European Union’s Horizon 2020 research and innovation programme under the Marie Sklodowska-Curie grant agreement No 765147.

Prof. David Livermore joins the Oxford Drug Design Scientific Advisory Board

18 July 2017

Oxford Drug Design is pleased to announce the addition of Prof. David Livermore to our Scientific Advisory Board.
David Livermore gained his BSc in 1978 and his PhD in 1983. He worked at the London Hospital Medical College from 1980 until 1997 when he joined the Health Protection Agency (now Public Health England), becoming Director of its Antibiotic Resistance Monitoring and Reference Laboratory in 1998. In October 2011 he moved to become Professor of Medical Microbiology at the University of East Anglia but still retains sessions at Public Health England as its Lead on Antibiotic Resistance. He has broad interests on the mechanisms, evolution and dissemination of antibiotic resistance and its relationship to antibiotic usage. He is very active in the field of antibiotics and resistance and is a member of the UK Government's Antimicrobial Resistance & Healthcare Infections Advisory Committee. He publishes and speaks widely on resistance and has edited for several journals including Journal of Antimicrobial Chemotherapy, Journal of Medical Microbiology and International Journal of Antimicrobial Agents.
Outside of work he is a keen walker and, in 2016, completed a 3000-mile route that has taken him right around the perimeter of England.

James B. Kahn, M.D. FIDSA, joins the Oxford Drug Design Scientific Advisory Board

29 June 2017

Oxford Drug Design is pleased to announce the appointment of James B. Kahn, M.D. FIDSA, to the company’s Scientific Advisory Board.
Dr. Kahn has deep and extensive knowledge of antibacterial drug development. He is Board-certified in both I.M. and I.D. After 18 years in the solo private practice of I.D. Medicine, James was recruited by Johnson & Johnson's Ortho-McNeil Pharmaceutical to be the first Director of their new I.D. Franchise. In addition to running numerous clinical trials for the antimicrobial FLOXIN, he also took over the clinical development of LEVAQUIN and was responsible for the sNDAs that led to 8 new FDA-approved indications. He proposed and then developed the higher-dose, shorter-course approach to accelerate pathogen eradication and reduce anti-bacterial exposure.
James is the founder and principal of JBK Strategic Consultations, LLC, a small firm providing Infectious Disease expertise to the Pharmaceutical, Venture Capital, and Medico-legal communities. He attends numerous national and international I.D. meetings and maintains close personal and professional contacts with many US and global opinion leaders.

InhibOx relauches as Oxford Drug Design

10 May 2017

InhibOx has relaunched as Oxford Drug Design to reflect its transition to a biotechnology company focused on internal drug discovery. Our lead antibacterial programme has identified compounds with the potential to be developed into therapies for Gram-negative bacterial infections, including against strains resistant to multiple current antibacterial drug classes. In the European Union alone, drug-resistant bacteria are estimated to cause 25,000 deaths and cost more than $1.5 billion every year in healthcare expenses and productivity losses. Compound design is supported by a proprietary technology platform in cheminformatics, 3D molecular similarity and computer-aided drug design that has been built up over 10 years of research and development.
The potential of our programme has been validated by the award of a prestigious Innovate UK Biomedical Catalyst grant to accelerate programme progression.

Oxford Drug Design secures $1.9m financing

1 April 2017

Oxford Drug Design has raised nearly $2m (£1.5m) of private investment to enable it to progress a novel antibacterial programme and continue to build its proprietary platform.
The funding, which will also help finance the company’s commercial and research and development (R&D) activities, was supported by both existing shareholders including IP Group plc as well as new investors including Busolantix Investment SA, O2h Ventures and a number of Business Angels. 
Oxford Drug Design will continue to build and utilise its proprietary technology platform in cheminformatics, 3D molecular similarity and computer-aided drug design, in parallel with progressing the antibacterial programme.

Oxford Drug Design starts work on $1.1m project to fight drug-resistant bacteria

1 March 2017

Oxford Drug Design (formerly InhibOx) has started work on a $1.1m (£900k) grant funded project to develop novel antibiotics. The project started four years ago as part of an EU-funded collaboration into multi-drug resistance. Capitalising on drug design, chemical synthesis and biology skills across the consortium, they have discovered new molecules with activity against a range of Gram-negative bacteria. The new money comes from Innovate UK, the UK's innovation agency, as part of the biomedical catalyst fund and will be used to design dual target inhibitors of aminoacyl tRNA synthetases for the treatment of multi-drug-resistant infections.
The compounds discovered so far inhibit a member of the tRNA synthetase family which plays a key role in protein biosynthesis. They have activity against a range of Gram-negative bacteria but need to be improved in terms of the level of activity and stability. This class of bacteria (which includes species such as E. coli and Klebsiella) has an extra layer to their cell wall. This provides them with an additional barrier to drug penetration, making them much harder to treat. By targeting more than one tRNA synthetase improvements should be seen in terms of both activity and decreased levels of bacterial resistance.
The next steps are to optimize the molecules to enhance their activity and stability and to monitor the emergence of resistance. The design work will be carried by over the next two years with the aim of developing a candidate ready for clinical testing.