This site uses cookies to improve your experience. To help us insure we adhere to various privacy regulations, please select your country/region of residence. If you do not select a country, we will assume you are from the United States. Select your Cookie Settings or view our Privacy Policy and Terms of Use.
Cookie Settings
Cookies and similar technologies are used on this website for proper function of the website, for tracking performance analytics and for marketing purposes. We and some of our third-party providers may use cookie data for various purposes. Please review the cookie settings below and choose your preference.
Used for the proper function of the website
Used for monitoring website traffic and interactions
Cookie Settings
Cookies and similar technologies are used on this website for proper function of the website, for tracking performance analytics and for marketing purposes. We and some of our third-party providers may use cookie data for various purposes. Please review the cookie settings below and choose your preference.
Strictly Necessary: Used for the proper function of the website
Performance/Analytics: Used for monitoring website traffic and interactions
In Wednesday’s Flash Talk webinar , we covered recent highlights in targetedproteindegradation, 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.
In one approach, they mark targetedproteins with “destroy me” tags that work with smallmolecules 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.
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 smallmolecules. How does TPD work?
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 (..)
3c06622 Targetedproteindegradation relies on smallmolecules that induce new protein–protein interactions between targets and the cellular proteindegradation machinery. Most of these smallmolecules feature specific ligands for ubiquitin ligases.
Options for cell-based proteindegrader assays Interest is growing in the use of targeted-proteindegradation to induce the breakdown of disease-causing proteins after treatment with smallmoleculedrugs.
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.
This laid the groundwork for my career in drug discovery using novel modalities like smallmolecule inhibitors, antibodies, RNA interference (RNAi) and, currently, smallmoleculeproteindegraders – which are opportunities to change how we think about medicines.
Promising future Molecular glues offer exciting opportunities for targetedproteindegradation and new ways to reach some of the estimated 85% of undruggable targets in the proteome. Conventional drug development has often focused on finding smallmolecules that fit the active site of a protein.
Program focused on identifying smallmolecules 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 drugtarget universe.
a leading biotechnology company developing smallmolecule therapeutics based on its proprietary uSMITE platform of targetedproteindegradation 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.
.
Monte Rosa Therapeutics has raised $96m in Series B financing to support further develop of its pipeline of small-moleculeproteindegraders.
Source link.
Sygnature Discovery identifies potent SHP2 degrader compounds using its proprietary targetedproteindegrader platform, CHARMED, in collaboration with Japanese specialty chemical company, UBE Corporation.
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.
We organize all of the trending information in your field so you don't have to. Join 15,000+ users and stay up to date on the latest articles your peers are reading.
You know about us, now we want to get to know you!
Let's personalize your content
Let's get even more personalized
We recognize your account from another site in our network, please click 'Send Email' below to continue with verifying your account and setting a password.
Let's personalize your content