Haven't got a glue: Protein surface variation for the design of molecular glue degraders.
Sign Up to like & getrecommendations! Published in 2021 at "Cell chemical biology"
DOI: 10.1016/j.chembiol.2021.04.009
Abstract: Molecular glue degraders are small, drug-like compounds that induce interactions between an E3 ubiquitin ligase and a target, which result in ubiquitination and subsequent degradation of the recruited protein. In recent years, serendipitous discoveries revealed… read more here.
Keywords: molecular glue; glue degraders; protein surface;
CRISPR Screen Reveals BRD2/4 Molecular Glue-like Degrader via Recruitment of DCAF16.
Sign Up to like & getrecommendations! Published in 2023 at "ACS chemical biology"
DOI: 10.1021/acschembio.2c00747
Abstract: Molecular glues (MGs) are monovalent small molecules that induce an interaction between proteins (native or non-native partners) by altering the protein-protein interaction (PPI) interface toward a higher-affinity state. Enhancing the PPI between a protein and… read more here.
Keywords: compound; screen; degrader; molecular glue ... See more keywords
SJPYT-195: A Designed Nuclear Receptor Degrader That Functions as a Molecular Glue Degrader of GSPT1.
Sign Up to like & getrecommendations! Published in 2022 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.2c00223
Abstract: We previously reported a specific inverse agonist (SPA70) of the nuclear receptor pregnane X receptor (PXR). However, derivatization of SPA70 yielded only agonists and neutral antagonists, suggesting that inverse agonism of PXR is difficult to… read more here.
Keywords: nuclear receptor; sjpyt 195; degrader; molecular glue ... See more keywords
Reversible Dual-Covalent Molecular Locking of the 14-3-3/ERRγ Protein–Protein Interaction as a Molecular Glue Drug Discovery Approach
Sign Up to like & getrecommendations! Published in 2023 at "Journal of the American Chemical Society"
DOI: 10.1021/jacs.2c12781
Abstract: Molecules that stabilize protein–protein interactions (PPIs) are invaluable as tool compounds for biophysics and (structural) biology, and as starting points for molecular glue drug discovery. However, identifying initial starting points for PPI stabilizing matter is… read more here.
Keywords: drug discovery; covalent; molecular glue; protein ... See more keywords
Molecular glue concept solidifies
Sign Up to like & getrecommendations! Published in 2019 at "Nature Chemical Biology"
DOI: 10.1038/s41589-019-0414-3
Abstract: Molecular-glue-mediated proximity-induced degradation now allows unprecedented therapeutic targeting of previously undruggable proteins. Structures showing how aryl-sulfonamides mediate recruitment of the splicing factor RBM39 to the E3 CRL4 DCAF15 broaden the mechanistic principles by which molecular… read more here.
Keywords: concept solidifies; molecular glue; glue concept; biology ... See more keywords
A theranostic abscisic acid-based molecular glue
Sign Up to like & getrecommendations! Published in 2023 at "Chemical Science"
DOI: 10.1039/d2sc06995d
Abstract: Molecular glues, capable of selectively controlling the interactions between specific pairs or groups of proteins and the associated downstream effects, have become a promising strategy for manipulating cellular functions and developing novel therapies for human… read more here.
Keywords: glue; theranostic molecular; abscisic acid; molecular glue ... See more keywords
Abstract 3424: Template-assisted covalent modification of DCAF16 enables BRD4 molecular glue degraders
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-3424
Abstract: Molecular glue degraders have emerged as a powerful class of small-molecule therapeutics, as demonstrated by the clinical successes of thalidomide analogs in the treatment of hematological malignancies. These small molecules act by recruiting ubiquitin ligases… read more here.
Keywords: dcaf16; glue degraders; covalent modification; molecular glue ... See more keywords
Targeted protein degradation and regulation with molecular glue: past and recent discoveries.
Sign Up to like & getrecommendations! Published in 2021 at "Current medicinal chemistry"
DOI: 10.2174/0929867328666210806113949
Abstract: The evolution in research and clinical settings of targeted therapies has been inspired by the progress of cancer chemotherapy to use small molecules and monoclonal antibodies for targeting specific disease-associated genes and proteins for noninfectious… read more here.
Keywords: molecular glue; degradation regulation; protein degradation; targeted protein ... See more keywords