Molecular glue degraders

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Design principles for cyclin K molecular glue degraders

Molecular glue degraders are an effective therapeutic modality, but their design principles are not well understood. Recently, several unexpectedly diverse compounds were reported to deplete cyclin K by linking CDK12-cyclin K to the DDB1-CUL4-RBX1 E3 ligase. To investigate how chemically dissimilar ...

ORGANISM(S): Hordeum vulgare (Barley)

2023-10-20 | PXD041836 | Pride

Discovery of molecular glue degraders via isogenic morphological profiling

Molecular glue degraders (MGDs) are small molecules that degrade proteins-of-interest via the ubiquitin-proteasome system. Historically, MGDs were discovered serendipitously. Current approaches for MGD discovery include cell-viability based drug screens or data mining of public transcriptomics and d...

ORGANISM(S): Homo sapiens (Human)

2023-11-20 | PXD045892 | Pride

Neo-substrate Cereblon Targeted protein degradation Molecular glue degrader E3 ubiquitin ligase

Design principles for cyclin K molecular glue degraders.

Not available

S-EPMC10746543 | biostudies-literature

Novel molecular glue degraders against broad range of myeloma and lymphoma cancer cell lines

Targeted protein degradation of neosubstrates plays a crucial role in treating hematological cancers with IMiDs therapy. However, the inevitable drug resistance and hematological toxicities remain persistent challenges, limiting their clinical efficacy. Herein, we present the discovery of a lead deg...

ORGANISM(S): Homo Sapiens

2024-06-22 | PXD053334 |

Rational Chemical Design of Molecular Glue Degraders.

Not available

S-EPMC10214506 | biostudies-literature

Rational and scalable strategies to identify small “molecular glue” degraders

PRJNA596945 | ENA

Rational Design of CDK12/13 and BRD4 Molecular Glue Degraders.

Not available

S-EPMC12831537 | biostudies-literature

Development of Potent and Selective CK1α Molecular Glue Degraders.

Not available