#PROTAC 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.
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! #TargetedProteinDegradation #TPD #PROTAC
https://www.nature.com/articles/s41571-023-00736-3
#targetedproteindegradation #TPD #PROTAC
Happy #Heterobifunctional Holidays from the Crewslab! #PROTAC #chemicalbiology #Yale
#heterobifunctional #PROTAC #ChemicalBiology #yale
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
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 #PROTAC project to be successful, may need my leg.
Nice #minireview on the post-#PROTAC #heterobifunctional #TPD world in #naturebiotechnology
https://www.nature.com/articles/s41587-022-01594-7
#minireview #PROTAC #heterobifunctional #TPD #naturebiotechnology
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. #TPD #TargetedProteinDegradation #PROTAC
https://www.wiley.com/en-gb/Inducing+Targeted+Protein+Degradation%3A+From+Chemical+Biology+to+Drug+Discovery+and+Clinical+Applications-p-9783527350179
#TPD #targetedproteindegradation #PROTAC
Nice paper from the Schapira lab identifying potential #ligand binding pockets for future #PROTAC development.
https://www.sciencedirect.com/science/article/pii/S2001037022005049#b0040
I'd like to join in on some conversations so here are some #hashtags #TPD #targetedproteindegradation #PROTAC #PROTACs #degraders #chemicalbiology #biochem #cellbiology #biotech #biopharma #ligase #ubiquitin #proteasome #ligand #labhumor #chemistry #biology #proteome #proteins #drug #pharma #startup
#hashtags #TPD #targetedproteindegradation #PROTAC #PROTACs #degraders #ChemicalBiology #biochem #cellbiology #biotech #biopharma #ligase #Ubiquitin #proteasome #ligand #labhumor #chemistry #biology #proteome #proteins #drug #pharma #startup