Drug Hunter

JUNE 29, 2023

In Wednesday’s Flash Talk webinar , we covered recent highlights in targeted protein degradation, with lots of great questions from the audience. KT-333 and KT-003) AR degraders and ER degraders from Arvinas (bavdegalutamide/ARV-110, ARV-766, and ARV-471) MDM2 degraders from Kymera (e.g.

Targeted Protein Degradation 221

Targeted Protein Degradation Small Molecule Drugs 221

Broad Institute

MARCH 14, 2024

In one approach, they mark targeted proteins with “destroy me” tags that work with small molecules known as molecular glues to prompt the cell’s own protein-clearing machinery to gobble up the proteins. Liu is also a Howard Hughes Medical Institute investigator and a professor at Harvard University.

Targeted Protein Degradation 141

Targeted Protein Degradation Small Molecule Medical Schools Science 141

Drug Target Review

JULY 6, 2023

TPD is a rapidly evolving therapeutic modality to degrade a disease-causing proteins, thereby eliminating their function specifically. 1 TPD is expected to challenge undruggable proteins, which are highly difficult to target by conventional small molecules. How does TPD work?

Targeted Protein Degradation 98

Targeted Protein Degradation Small Molecule Clinical Trials Science 98

Practical Cheminformatics

JANUARY 16, 2024

Property Prediction Machine Learning Methods for Small Data Challenges in Molecular Science [link] Practical guidelines for the use of gradient boosting for molecular property prediction [link] Application of message passing neural networks for molecular property prediction [link] Molecular Similarity Molecular Similarity: Theory, Applications, and (..)

Targeted Protein Degradation 140

Targeted Protein Degradation Small Molecule Computational Chemistry Bioinformatics 140

Covalent Modifiers

OCTOBER 3, 2023

3c06622 Targeted protein degradation relies on small molecules that induce new protein–protein interactions between targets and the cellular protein degradation machinery. Most of these small molecules feature specific ligands for ubiquitin ligases.

Targeted Protein Degradation 72

Targeted Protein Degradation Small Molecule Drugs 72

BMG Labtech

MAY 22, 2024

Options for cell-based protein degrader assays Interest is growing in the use of targeted-protein degradation to induce the breakdown of disease-causing proteins after treatment with small molecule drugs.

Targeted Protein Degradation 52

Targeted Protein Degradation Small Molecule Treatment Disease 52

Drug Target Review

OCTOBER 4, 2023

Antibody-drug conjugates (ADCs) have been a groundbreaking approach to cancer treatment with their ability to deliver cytotoxic drugs directly to diseased cells while sparing healthy tissues. 1 However, efforts proved less effective than the original drugs, owing mostly to insufficient toxicity against cancer cells.

Small Molecule 126

Small Molecule Drugs Immune Response Targeted Protein Degradation 126