SEP 16, 2015 5:00 AM PDT

Synthetic Chemists to Aid the Community for Open Antimicrobial Drug Discovery

Speaker
  • Program Coordinator: Community for Open Antimicrobial Drug Discovery, University of Queensland
    Biography
      Dr. Mark Blaskovich is Program Coordinator: Hit Validation & Chemistry for the Community for Open Antimicrobial Drug Discovery, and a Senior Research Officer at the Institute for Molecular Bioscience at The University of Queensland. He has extensive medicinal chemistry expertise and over 15 years of industrial drug development experience, most recently as Chief Operating Officer at Mimetica (Australia), where he managed the drug discovery and development program for melanocortin-5 receptor antagonists leading to a compound currently in Phase II human trials for treatment of acne. In his previous role at CEPTYR (Seattle) he led a multidisciplinary team that developed a preclinical candidate for protein tyrosine phosphatase 1B, while at Molecumetics (Seattle) he headed a $2m/yr industrial collaboration on peptidomimetic compounds targeting proteases and GPCRs. Since starting at The University of Queensland, Mark has been working on developing new antibiotics to treat drug resistant pathogens. He has published over thirty articles, is an inventor on eight patent families with over 100 granted and pending applications, and is author of 'The Handbook on Syntheses of Amino Acids'.

    Abstract
    The antibiotic pipeline is broken, with a dearth of new antibiotics, a collapse in pharmaceutical company research1, and the exhaustion of chemical diversity contained in pharma libraries. "The low hanging fruit from the antibiotic tree has probably already been picked and new sources of compounds are needed."2 We believe that there is an untapped resource contained in the laboratories of synthetic organic chemists; synthetic compounds prepared for other projects that have never been tested for their antimicrobial potential. These compounds, which are sitting at the back of benches and freezers, may have been synthesised to validate new synthetic routes, develop new methodologies, or create unusual structures. A global screening initiative will uncover this significant and rich chemical diversity held outside of corporate screening collections by providing a low-barrier access to testing. Antibacterial drugs occupy a unique property space that is vastly different to drugs developed for other therapeutic areas, suggesting that commercially available chemical compounds lack the physicochemical properties ideal for activity against bacteria and therefore, a varied source of chemical diversity needs to be investigated. We have created a Wellcome Trust-supported not-for-profit Open-Access initiative, The Community for Open Antimicrobial Drug Discovery [CO-ADD], to provide unencumbered free antimicrobial screening for any interested researcher.3 CO-ADD builds upon a suite of established in vitro and in vivo assays, medicinal chemistry and core researcher expertise and aims to unearth fresh chemical diversity for the treatment of bacterial infection.

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