A platform for the rapid synthesis of molecular glues (Rapid-Glue) under miniaturized conditions for direct biological screening

J Li, C Li, Z Zhang, Z Zhang, Z Wu, J Liao… - European Journal of …, 2023 - Elsevier
molecular glue libraries is not an easy task and requires extensive resources. We
previously developed platforms for rapid synthesis … of rapid synthesis of molecular glues (Rapid-Glue) …

[HTML][HTML] Diverse synthesis of C2-linked functionalized molecules via molecular glue strategy with acetylene

B Yang, S Lu, Y Wang, S Zhu - Nature Communications, 2022 - nature.com
… In this work, we developed a photoredox-catalyzed synthetic protocol for diverse C2-linked
molecules via a molecular glue strategy that employed gaseous acetylene under mild …

Identification and optimization of molecular glue compounds that inhibit a noncovalent E2 enzyme–ubiquitin complex

D St-Cyr, DF Ceccarelli, S Orlicky, AM van der Sloot… - Science …, 2021 - science.org
… These drawbacks raised the question of whether we could discover an alternate inhibitor
scaffold with greater potential for optimization through a de novo screen for molecular glues

Discovery of fully synthetic FKBP12-mTOR molecular glues

RCE Deutscher, C Meyners, ML Repity, WO Sugiarto… - 2024 - chemrxiv.org
… the first fully synthetic FKBP12-mTOR molecular glues, which … Our results show that molecular
glues targeting flat surfaces … FKBP12 as a versatile presenter protein for molecular glues. …

Molecular glue discovery: current and future approaches

JA Dewey, C Delalande, SA Azizi, V Lu… - Journal of medicinal …, 2023 - ACS Publications
molecular glues to devise a classification system based on their mechanism of action. We find
that clinically approved molecular glues … the optimal molecular glue discovery method for a …

PROTACs, molecular glues and bifunctionals from bench to bedside: Unlocking the clinical potential of catalytic drugs

M Maneiro, E De Vita, D Conole, CS Kounde… - Progress in medicinal …, 2021 - Elsevier
… allow for the transfer of the first ubiquitin molecule from the E2 enzyme to an accessible lysine
residue on the POI. This is followed by rapid transfer of additional ubiquitin units leading to …

[HTML][HTML] Design principles for cyclin K molecular glue degraders

Z Kozicka, DJ Suchyta, V Focht, G Kempf… - Nature chemical …, 2024 - nature.com
… , we also show that these glues do not require pronounced … a conceptual framework for
rational molecular glue design. … efficient molecular glues, and that hydrophilicity of the gluing

Molecular glue degraders: exciting opportunities for novel drug discovery

T Lemaitre, M Cornu, F Schwalen, M Since… - Expert Opinion on …, 2024 - Taylor & Francis
… cellular homeostasis and the balance between protein synthesis and protein degradation.
The concept of protein degradation is concerned with molecular glues, which form part of the …

Discovery of molecular glue degraders via isogenic morphological profiling

A Ng, F Offensperger, JA Cisneros… - ACS Chemical …, 2023 - ACS Publications
… Using this protocol, we were able to rapidly synthesize a library of 132 compounds in 384-well
plates that could be used directly in biological assays. To inform and benchmark the use …

Serendipitous discovery of Class I HDAC inhibitors from rational design of molecular glue degraders targeting HDAC

D Chen, S Lin, Z Zeng, J An, W Yan, Z Gu… - European Journal of …, 2024 - Elsevier
… On the other hand, the emerging strategy of molecular glue degraders offers a unique …
In this study, we synthesized a series of candidate compounds based on the molecule glue, …