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Cambridge MedChem Consulting

Open Source Drug Discovery

Open Source Antibiotics

I just thought I'd share this email

Dear Friend of Open Source Antibiotics (OSA),

It's been a busy few months in OSA. Recent activity is being captured in weekly public Zoom meetings (every Friday at 2pm London at https://ucl.zoom.us/j/92800004715), and you can see the details in the recordings of those meetings (like this one) and the associated "Github Issues" (like this one).

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But as part of those discussions we were wondering about the best way to update everyone quickly. While OSA uses Twitter, there is no good substitute for a short email. So this is the first, short OSA news email. Three points:

  1. We have guessed you're interested in receiving occasional emails about OSA. If you're not, just email us back to say you'd like to opt out. Nobody likes spam.
  2. Please forward this to anyone you think might be interested in antibiotics or drug discovery or open science. As an open project, everything is in the public domain, and everyone is welcome.
  3. To keep things short, each news email has a limit of three items. If you're interested in learning more, then each project has a wiki (current project status, like this) and the Issue Tracker (current To Do list and discussion, like this).
So - drumroll - here is the first quick update, focussing on OSA Series 2 (an update on Series 1, the mur ligases, will come soon).
  1. We have confirmed the activity vs MRSA of the diarylimidazoles (exemplar compound OSA821 shown below), originally discovered and explored by Alvaro Lorente and Bill Zuercher at UNC Chapel Hill. A new potency screen is being performed this week at UCL by Paul Stapleton, and includes about 30 compounds that have been donated to the project via Ben Perry (DNDi). This time our potency assay will include a parallel screen of select compounds vs VRE, to see if there is activity vs other high priority Gram +ves.

OSA821

  1. A key aim of the project is to solve the rapid clearance of the known actives. New data from Sue Charman's lab gave clues as to which compounds to investigate next, and we are finalising negotiations for some pro bono work from a UK company towards identification of possible metabolites.
  2. The mechanism of action of these compounds is unknown, but Lee Graves's lab at UNC are in the middle of some MIBs experiments that we hope will reveal, by the end of October, some key new insights into how the compounds work.
Best wishes, Mat and all the OSA Series 2 contributors

OSA logo_low

You can read more about the Open Source Antibiotics on GitHub https://github.com/opensourceantibiotics.

There are currently two projects MurLigase and DiarylImidazoles, everything is in the open and anyone can contribute.

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Why not swing by and have a browse.