June 2020 PMID 34094158

Macrocycle synthesis strategy based on step-wise "adding and reacting" three components enables screening of large combinatorial libraries.

Ganesh K Mothukuri, Sangram S Kale, Carl L Stenbratt, Alessandro Zorzi, Jonathan Vesin, Julien Bortoli Chapalay, Kaycie Deyle, Gerardo Turcatti, Laura Cendron, Alessandro Angelini, Christian Heinis

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Mentions

Peak: 10 in Jul 2020

across 2 sources since Jun 2020

Extended reach

133,927

potential audience

Total likes

Video views

1,425

Mentions per month

Jun 2020 – Feb 2023

Where it's discussed

X / Twitter15 posts
YouTube2 videos

AI synopsis

What people are saying

The discussions reflect enthusiasm for the new synthesis strategy, exemplified by posts praising the paper and collaborators, such as 'Recent exciting paper' and congratulatory remarks. The use of words like 'diverse', 'high-throughput', and 'congratulation' underscores both technical interest and recognition of the research's potential influence.

AgreementModerate agreement

Most discussions appreciate the significance of the new macrocycle synthesis strategy, with some explicitly congratulating the authors and recognizing its potential.

InterestHigh interest

The discussions show high interest, with many posts highlighting technical aspects like combinatorial strategies and high-throughput methods.

EngagementModerate engagement

Posts demonstrate moderate engagement through mentions of collaborations, methods, and enthusiastic remarks about the research's excitement.

ImpactModerate impact

The overall tone suggests that the community recognizes this research's potential impact on drug discovery and materials science, though it's mostly preliminary excitement.

Abstract in brief

The study presents a new stepwise macrocycle synthesis method that combines three building blocks through efficient reactions, avoiding purification steps, to create large compound libraries for drug discovery.
Using this approach, researchers generated a library of 3,780 macrocycles by reacting different amino acids, amines, and cyclization linkers, which was then screened against thrombin, resulting in a potent and selective inhibitor.
Structural analysis showed that two of the three building blocks worked together to enhance activity, highlighting the importance of combinatorial screening, and the method's versatility suggests it can be applied to develop ligands for other biological targets.]

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All mentions

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Diamond MX Beamlines

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New Paper from I03 https://t.co/I3Y3qCUN9m (https://t.co/qJMqkbmR7m)

Oct 3, 2020 · 1,424 followers View post →