Metabolite Tales Blog

Hypha’s “Metabolite Tales” blog articles are purely science-focussed commentary on interesting developments and papers relevant to the role of metabolism in drug discovery and development. The content is particularly relevant to those with a background in medicinal chemistry, drug metabolism and biotransformation.

We also recommend the following excellent blogs:

Drug Hunter – a trusted, independent source of curated, factual information for the drug discovery community, in particular the articles, case studies and cheat sheets!

In The Pipeline – Derek Lowe’s commentary on drug discovery and the pharma industry.

Hypha's Metabolite Tales Blog Articles

Andrew Parkinson, Consultant and former Founder and CSO/CEO at Xenotech, debates whether drugs that induce CYP1A enzymes via activation of the AhR receptor should be a cause for concern or not.

This blog highlights the prospect of exploiting orphan human CYPs for development of targeted anti-cancer agents through a prodrug strategy.

In this blog Consultant and Medicinal Chemistry expert Rob Young explores some of the potential impacts of hydroxyl groups in medicinal chemistry, contextualising opportunities alongside other fundamental structural changes and considering the physical consequences of its introduction.

Steve Djuric, Consultant and ex VP of Medicinal Chemistry at Abbvie, shares his thoughts on the challenges we face today in selecting drug candidates.

In this blog Steve delves into some of the PK demands, including permeability of PROTACs, CYP and AO metabolism, and the impact of AI.

In this blog we explore the relevance of the mainly extrahepatic epoxygenase CYP2J2. Given it’s role at the crossroads of drug metabolism and endogenous bioactive oxy-lipid synthesis, we discuss whether there is a case for greater importance to be placed on this CYP.

Cyclopropyl groups are an appealing substituent to use in drug design because they impart constraint in aliphatic systems while retaining a high fraction of sp3. Furthermore, the ring strain produces shorter, stronger, more polarised C-H bonds that impart some novel properties, not least the reduced susceptibility to oxidative metabolism by cytochrome P450 (CYP) enzymes. In this blog post we explore the metabolism of various drug structures that contain cyclopropyl groups, revealing that cyclopropyl groups can be used advantageously to diminish oxidative metabolism in some circumstances, but when coupled to amines can lead to potentially reactive intermediates.

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