Articles with "molecular glues" as a keyword



Molecular Glues: The Adhesive Connecting Targeted Protein Degradation to the Clinic

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Published in 2022 at "Biochemistry"

DOI: 10.1021/acs.biochem.2c00245

Abstract: Targeted protein degradation is a rapidly exploding drug discovery strategy that 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… read more here.

Keywords: drug discovery; targeted protein; protein degradation; molecular glues ... See more keywords

Molecular Glues: A New Approach to Modulating GPCR Signaling Bias

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Published in 2025 at "Biochemistry"

DOI: 10.1021/acs.biochem.4c00734

Abstract: G-protein-coupled receptors (GPCRs) transmit an extracellular chemical/biological signal across the cell membrane, stimulating an array of intracellular signaling cascades. Canonically, these extracellular signaling molecules bind to the endogenous ligand pocket (orthosteric pocket), which stabilizes either… read more here.

Keywords: glues new; gpcr signaling; molecular glues; signaling bias ... See more keywords

Designing Selective Drug-like Molecular Glues for the Glucocorticoid Receptor/14-3-3 Protein–Protein Interaction

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Published in 2022 at "Journal of Medicinal Chemistry"

DOI: 10.1021/acs.jmedchem.2c01635

Abstract: The ubiquitously expressed glucocorticoid receptor (GR) is a nuclear receptor that controls a broad range of biological processes and is activated by steroidal glucocorticoids such as hydrocortisone or dexamethasone. Glucocorticoids are used to treat a… read more here.

Keywords: protein protein; glucocorticoid receptor; designing selective; receptor ... See more keywords

Trends in Neosubstrate Degradation by Cereblon-Based Molecular Glues and the Development of Novel Multiparameter Optimization Scores.

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Published in 2024 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.3c01872

Abstract: Molecular glues enable the degradation of previously "undruggable" proteins via the recruitment of cereblon (CRBN) to the target. One major challenge in designing CRBN E3 ligase modulating compounds (CELMoDs) is the selectivity profile toward neosubstrates,… read more here.

Keywords: cereblon; chemistry; molecular glues; degradation ... See more keywords

Research Progress in Targeting GSPT1: Molecular Glues, Bifunctional Degraders, and Antibody-Enabled Molecular Glues for Cancer Therapy.

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Published in 2025 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.5c00783

Abstract: G1 to S phase transition 1 (GSPT1, also known as eRF3a) is a crucial translation termination factor that plays a vital role in acute myeloid leukemia (AML) and MYC-driven lung cancer. Degrading GSPT1 can induce… read more here.

Keywords: glues bifunctional; cancer; molecular glues; bifunctional degraders ... See more keywords

Application of Weighted Interaction-Fingerprints for Rationalizing Neosubstrate Potency and Selectivity of Cereblon-Based Molecular Glues.

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Published in 2025 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.5c01919

Abstract: Cullin-RING Ligase 4 Cereblon (CRL4CRBN) (CRBN) E3 ligase modulatory drugs (CELMoDsTM) make up a successful class of compounds targeting neosubstrates for proteasome-dependent degradation. Early immunomodulatory drugs (IMiDsTM) target Ikaros and Aiolos degradation. In addition, there… read more here.

Keywords: cereblon; molecular glues; degradation; selectivity ... See more keywords

Single-Molecule-Based, Label-Free Monitoring of Molecular Glue Efficacies for Promoting Protein–Protein Interactions Using YaxAB Nanopores

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Published in 2024 at "ACS Nano"

DOI: 10.1021/acsnano.4c11436

Abstract: Modulating protein–protein interactions (PPIs) is an attractive strategy in drug discovery. Molecular glues, bifunctional small-molecule drugs that promote PPIs, offer an approach to targeting traditionally undruggable targets. However, the efficient discovery of molecular glues has… read more here.

Keywords: molecule; molecular glues; protein; yaxab nanopores ... See more keywords

Modulation of Protein–Protein Interactions with Molecular Glues in a Synthetic Condensate Platform

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Published in 2025 at "Journal of the American Chemical Society"

DOI: 10.1021/jacs.4c17567

Abstract: Misregulation of protein–protein interactions (PPIs) underlies many diseases; hence, molecules that stabilize PPIs, known as molecular glues, are promising drug candidates. Identification of novel molecular glues is highly challenging among others because classical biochemical assays… read more here.

Keywords: environment; molecular glues; protein; protein protein ... See more keywords

Scaffold-hopping for molecular glues targeting the 14-3-3/ERα complex

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Published in 2025 at "Nature Communications"

DOI: 10.1038/s41467-025-61176-4

Abstract: Molecular glues, small molecules that bind cooperatively at a protein-protein interface, have emerged as powerful modalities for the modulation of protein-protein interactions (PPIs) and “undruggable” targets. The systematic identification of new chemical matter with a… read more here.

Keywords: chemistry; molecular glues; scaffold hopping; hopping molecular ... See more keywords

A theranostic abscisic acid-based molecular glue

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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

MGDB: a curated database for molecular glues.

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Published in 2025 at "Nucleic acids research"

DOI: 10.1093/nar/gkaf1131

Abstract: Abstract Molecular glues (MGs) represent a unique class of small molecules that modulate protein–protein interactions by altering target protein surface properties, enabling targeted degradation, pathway modulation, or functional control of proteins, including traditionally undruggable targets.… read more here.

Keywords: database; molecular glues; mgdb; database molecular ... See more keywords