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Cambridge MedChem Consulting

Covalent Modification

I've written a page in the Drug Discovery Resources on covalent inhibitors.

This publication suggests this area is going to become more important "An activity-guided map of electrophile-cysteine interactions in primary human immune cells" https://www.biorxiv.org/content/10.1101/808113v1.

Here, we present a global map of cysteines in primary human T cells that are susceptible to covalent modification by electrophilic small molecules. More than 3000 covalently liganded cysteines were found on functionally and structurally diverse proteins, including many that play fundamental roles in immunology.

Covalent Inhibtors page updated

I've updated the covalent inhibitors page to include details of two covalent fragment libraries that have been used in fragment screening.

NUD7hits

Updated Drug Discovery Resources

I've done some updates to the Drug Discovery Resources.

The Following Pages have been Updated

Macrocycles
Predicting Metabolism
Covalent Inhibitors

PROteolysis TArgeting Chimeras (PROTACs), Lysosome Targeting Chimeras (LYTACs), and ENDosome TArgeting Chimeras (ENDTACs)

Drug Discovery Resources Updated

I've made a few additions and updated to the Drug Discovery Resources pages. In particular I've updated the covalent inhibitors page and added additional examples to the molecular interactions page. I've also started updating the ADME section and added a page on half-life and how it might be modulated.

repeated

Covalent Inhibitors

I've just added a page on irreversible covalent inhibitors, this is just the first iteration I plan to add more when I have some spare time.

hcv