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 182

Targeted Protein Degradation Small Molecule Drugs 182

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 135

Targeted Protein Degradation Small Molecule Computational Chemistry Bioinformatics 135

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

Sygnature Discovery

SEPTEMBER 25, 2023

Sygnature Discovery identifies potent SHP2 degrader compounds using its proprietary targeted protein degrader platform, CHARMED, in collaboration with Japanese specialty chemical company, UBE Corporation.

Targeted Protein Degradation 52

Targeted Protein Degradation Small Molecule Science Disease 52

Drug Target Review

JULY 23, 2024

This laid the groundwork for my career in drug discovery using novel modalities like small molecule inhibitors, antibodies, RNA interference (RNAi) and, currently, small molecule protein degraders – which are opportunities to change how we think about medicines.

Small Molecule 116

Small Molecule Targeted Protein Degradation Science Disease 116

BMG Labtech

APRIL 16, 2024

Promising future Molecular glues offer exciting opportunities for targeted protein degradation and new ways to reach some of the estimated 85% of undruggable targets in the proteome. Conventional drug development has often focused on finding small molecules that fit the active site of a protein.

Targeted Protein Degradation 40

Targeted Protein Degradation Small Molecule Drug Development Disease 40

The Pharma Data

DECEMBER 21, 2020

Program focused on identifying small molecules that target a GPCR for degradation as potential therapeutic agents for gastrointestinal disorders. Unique combination of novel technologies to enhance GPCR drug discovery and expand capabilities into wider drug target universe.

Targeted Protein Degradation 40

Targeted Protein Degradation Small Molecule Structure Based Drug Design (SBDD) Drugs 40

The Pharma Data

OCTOBER 15, 2020

a leading biotechnology company developing small molecule therapeutics based on its proprietary uSMITE platform of targeted protein degradation technology, today announced that the company’s internal program to develop selective degraders that target key proteins within the TRK family has been published by the Journal of Medicinal Chemistry.

Targeted Protein Degradation 40

Targeted Protein Degradation Small Molecule Science Disease 40

The Pharma Data

SEPTEMBER 25, 2020

. Monte Rosa Therapeutics has raised $96m in Series B financing to support further develop of its pipeline of small-molecule protein degraders. Source link.

Targeted Protein Degradation 40

Targeted Protein Degradation Small Molecule Clinical Development Disease 40

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 127

Small Molecule Drugs Immune Response Targeted Protein Degradation 127

LifeSciVC

FEBRUARY 5, 2025

Given this ever-increasing body of evidence, why is it that for so long, they have not been the focus of drug discovery? Lacking active sites entirely, transcription factors are instead largely regulated by post-translational modification, which in turn impacts changes in conformation, behavior, and interaction with other proteins.

Small Molecule 67

Small Molecule Targeted Protein Degradation Regulations Disease 67