Matthieu Schapira · @mattschap
81 followers · 37 posts · Server fediscience.org

from @Novartis team recruiting DCAF1, an E3 ligase essential in cancer, rescues BTK degradation in a cell line that acquired resistance to a CRBN-recruiting PROTAC. Great mechanistic PoC, even though overall effect on cell viability is not as pronounced.

#PROTAC

Last updated 1 year ago

Keith Hornberger · @KRHornberger
195 followers · 141 posts · Server mstdn.science

Now online at @Nature Reviews Clinical Oncology from my Arvinas colleague Debbie Chirnomas, myself, and Craig @crews: Protein degraders enter the clinic -- a new approach to cancer therapy. Check it out!
nature.com/articles/s41571-023

#targetedproteindegradation #TPD #PROTAC

Last updated 2 years ago

CRAIG M CREWS · @crews
946 followers · 1224 posts · Server mstdn.science
Guillaume Laconde · @Laconde
84 followers · 23 posts · Server mstdn.science

New patent from
@C4Therapeutics
EGFR DEGRADERS TO TREAT CANCER METASTASIS TO THE BRAIN OR CNS. A lot of CRBN E3 ligand was used in this approach !!! very nice work and impressive results.

#PROTAC #egfr #osimertinib

Last updated 2 years ago

Corey_Hopkins · @Hopkins_Lab
20 followers · 2 posts · Server mstdn.science

First post an a short intro. I’m a medicinal chemist/drug discoverer in academia. My group works on a variety of areas: cancer and neuroscience mainly. For (permanent) fun, when my students discover an in vivo probe, it gets tattooed on me. Can’t wait for our project to be successful, may need my leg.

#PROTAC

Last updated 2 years ago

CRAIG M CREWS · @crews
350 followers · 142 posts · Server mstdn.science
Keith Hornberger · @KRHornberger
66 followers · 21 posts · Server mstdn.science

The eBook of Inducing Targeted Protein Degradation (Ed. Philipp Cromm, published by Wiley-VCH) is now available! Get yours today. Featuring a chapter by me and Erika Araujo. Print edition coming in December.
wiley.com/en-gb/Inducing+Targe

#TPD #targetedproteindegradation #PROTAC

Last updated 2 years ago

CRAIG M CREWS · @crews
350 followers · 142 posts · Server mstdn.science

Nice paper from the Schapira lab identifying potential binding pockets for future development.

sciencedirect.com/science/arti

#ligand #PROTAC

Last updated 2 years ago

CRAIG M CREWS · @crews
350 followers · 142 posts · Server mstdn.science