2022
DOI: 10.26434/chemrxiv-2022-vjcpx
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Molecular glues: The adhesive connecting targeted protein degradation to the clinic

Abstract: Targeted protein degradation is a rapidly exploding drug discovery strategy which uses small molecules to recruit disease-causing proteins for rapid destruction mainly via the ubiquitin-proteasome pathway. It shows great potential for treating diseases such as cancer, infectious, inflammatory, and neurodegenerative diseases, especially for those with “undruggable” pathogenic protein targets. With the recent rise of the ‘molecular glue’ type of protein degraders, which tighten and simplify the connection of an … Show more

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Cited by 4 publications
(2 citation statements)
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“…A plethora of excellent review articles on molecular glues and the complexes they stabilize have been published in the recent years, each focusing on a slightly different aspect of the topic, with the majority of them focusing on the discovery history, mechanism of action, and design strategy [28][29][30][31][32][33][34][35][36][37] . This review seeks to compile and analyze the current, published molecular glue ternary complex structures with the aim of identifying and quantifying any structural requirements for PPIs that are induced by molecular glues, as well as surveying the best computational methods to predict potential 'gluable' interfaces.…”
Section: Introductionmentioning
confidence: 99%
“…A plethora of excellent review articles on molecular glues and the complexes they stabilize have been published in the recent years, each focusing on a slightly different aspect of the topic, with the majority of them focusing on the discovery history, mechanism of action, and design strategy [28][29][30][31][32][33][34][35][36][37] . This review seeks to compile and analyze the current, published molecular glue ternary complex structures with the aim of identifying and quantifying any structural requirements for PPIs that are induced by molecular glues, as well as surveying the best computational methods to predict potential 'gluable' interfaces.…”
Section: Introductionmentioning
confidence: 99%
“…Recently, a certain class of small molecule compounds known as molecular glues were serendipitously discovered and were successfully shown to modulate PPI interaction [3]. However, for rational in-silico molecular glue design there is still no established method(s) reported in the literature [3][4][5][6]. In this research we aim to address this gap by appealing to a combination of known and novel in-silico methods for small molecules including NCE generation, NCE optimization, molecular docking, and molecular dynamic simulations for design of molecular glues.…”
Section: Introductionmentioning
confidence: 99%