Practical Fragments

This blog is meant to allow Fragment-based Drug Design Practitioners to get together and discuss NON-CONFIDENTIAL issues regarding fragments.

Showing posts with label fragment-growing. Show all posts
Showing posts with label fragment-growing. Show all posts
03 May 2021

Fragments in the clinic: AG-270

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A promising oncology approach is to target “synthetic lethal” proteins that are required for cancer cells but not for ordinary cells. Methio...
10 September 2018

Fragment flipping during optimization

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Last month we highlighted a study that asked how often the binding mode of a fragment changed during optimization. A new paper in J. Med....
03 September 2018

From generic fragment to selective BET-family BD2 inhibitor

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Fragments have been a rich source of leads against bromodomain-containing proteins, epigenetic readers that recognize acetylated lysine re...
13 August 2018

Fragment growing and merging: an inverse agonist of RORγt2

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The nuclear receptor transcription factor RORγt2 is involved in the differentiation of Th17 cells, and is thus a target for inflammatory di...
23 July 2018

Fragments score a win against WDR5-WIN

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Protein-protein interactions (PPIs) can be difficult targets for multiple reasons. First, the contacts often cover large, flattish areas wi...
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