Hypha Discovery: metabolite synthesis, purification and identification experts
WHAT'S NEW - Q4 2021
PolyCYPs in action for the Open Source Antibiotic Project
Hypha's PolyCYPs® enzymes were used to good effect to help the Open Source Antibiotics project team identify a major hydroxylated metabolite of one of their lead compounds.
Hypha scientists screened OSA821 using PolyCYPs and in human liver S9 incubations, and observed some oxidised metabolites.
We then scaled up the reaction using an enzyme prep of one of the best hitting PolyCYPs isoforms, and passed the material back to the OSA team. Read more here.
"Some very excellent people at Hypha noticed that we wanted to identify a metabolite of one of the lead molecules in Open Source Antibiotics Series 2. We sent them the molecule with a very light touch MTA (it's all open, after all) and they did their wizardry (that we could not do) and sent us back a sample we were able to purify to prove the location of the oxidation. Fast, efficient, mutually beneficial collaboration, in the open. It was a pleasure working with them.”
Professor Mat Todd, Chair of Drug Discovery at University College London, UK
PolyCYPs screening kit offer
We are pleased to be able to offer our clients a 20% discount off PolyCYPs+ screening kits, for orders placed from now until the end of 2021. Contact us if you'd like to take advantage of this.
PolyCYPs+ kits are effective for the generation of a wide variety of human and other mammalian phase 1 metabolites. The kits contain 18 PolyCYP isoforms as well as human AOX1 and FMO3.
Unopened kits can be stored in the freezer until needed without a drop off in enzyme activity. The expiry date of current kits in stock is August 2022.
Scale-up vials can be ordered for hit reactions, and larger scale metabolite production can be undertaken at Hypha.
Open Source Projects
Open Source Projects is a platform for harnessing collaborative efforts towards antibiotic drug discovery. Everything is open and anyone can contribute.
In the link below, Professor Mat Todd discusses the impact companies can make in open source projects.
METABOLITE TALES
LipMetE – A useful tool for relating lipophilicity to metabolic stability in microsomes?
Our blog for October explored LipMetE. LipMetE is a potentially useful and underutilised efficiency metric that relates logD to microsomal clearance. In this post we explore its origins and application to analyse metabolism trends in drug design.
Keep a look out for our next blog post in November on the role of "minor" CYPs in metabolism of drugs.
About Hypha
Hypha are experts in the scalable synthesis, purification and structure elucidation of metabolites of drugs and agrochemicals. We work with pharma and agrochemical companies worldwide to fulfil our clients' needs to obtain metabolites for definitive MetID and for further biological testing. Applying a comprehensive portfolio of methods, including microbial and liver S9 / microsomal biotransformation methods, chemical synthesis, and recombinant enzymes, Hypha has the ability to produce gram amounts of synthetically challenging metabolites and oxidised derivatives of drugs. Combined with strong capabilities in purification chemistry and structural elucidation using state-of-the-art NMR spectroscopy, we are able to deliver an end-to-end service to clients.
