Practical Fragments

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

30 December 2021

Review of 2021 reviews

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As the year winds down SARS-CoV-2 continues its relentless drive through Greek letters and the planet. But there is hope: vaccines seem to b...
2 comments:
22 December 2021

Pacifichem 2021

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Pacifichem , the last significant conference of 2021, has just ended. Traditionally held every five years, these meetings usually bring thou...
13 December 2021

Fragments vs AXL, with help from an ELF

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The receptor tyrosine kinase AXL has been implicated in multiple cancers, and more recently as a possible target for COVID-19. The protein h...
06 December 2021

Merging fat fragments for fat mass obesity-associated protein

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Despite its name, fat mass obesity-associated protein (FTO) is implicated not just in obesity but also cancer and neurological disorders. Th...
29 November 2021

DeepFrag: fragment optimization by machine learning

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Machine learning is becoming increasingly common in drug discovery. Just a few months ago we highlighted its use to design a library of pri...
22 November 2021

Selective fragments vs GPCRs, guided by modeling

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Earlier this year we highlighted a fragment optimization success story against a G protein-coupled receptor (GPCR) which made no use of str...
15 November 2021

Fragments vs SETD2: a chemical probe

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Among the various epigenetic “writers,” only one is capable of trimethylating lysine 36 of histone H3. SET domain-containing protein 2 (SETD...
08 November 2021

Fragments in the clinic: 2021 edition

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Since our last clinical update in 2020 two new fragment-derived drugs, asciminib and sotorasib, have been approved, bringing the total to s...
2 comments:
30 October 2021

Asciminib: the sixth fragment-derived drug approved

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Yesterday, on October 29, the US FDA approved asciminib (ABL001, from Novartis) for two subsets of patients with chronic myeloid leukemia ...
1 comment:
25 October 2021

Fragments vs TIM-3

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In order to thrive, cancer cells need to evade the immune system. Preventing them from doing so is the goal of cancer immunotherapy . Althou...
18 October 2021

Fragments vs the SARS-CoV-2 main protease – this time by NMR

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Last week we highlighted NMR screens against RNA from SARS-CoV-2. As we noted then, much of the drug discovery action has focused on the vi...
11 October 2021

Fragments vs SARS-CoV-2 RNA

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The first mention of SARS-CoV-2 on Practical Fragments in early March of last year highlighted a crystallographic fragment screen against ...
04 October 2021

Nineteenth Annual Discovery on Target Meeting

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Cambridge Healthtech Institute held its annual Discovery on Target meeting last week. For the first time the event was hybrid, with slightl...
26 September 2021

Success in drug discovery is not necessarily fast or inevitable

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The biotech industry rightly prizes speed: every day people die of diseases we are trying to prevent or cure. And developments can indeed ha...
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