jobRxiv · @jobRxiv
959 followers · 3152 posts · Server mas.to
jobRxiv · @jobRxiv
949 followers · 3002 posts · Server mas.to
Clemens Schulte · @SchulteClemens
32 followers · 19 posts · Server mstdn.science

Out now in CDD: our work in collab with uni-wuerzburg.de/rvz/forschung spearheaded by Thamara Nishida Xavier da Silva about in vitro, in silico and biophysical characterization of FSP1 inhibition

nature.com/articles/s41419-023

MST and "iFSP1-Tracer" made it possible to quantify binding affinities of the highly hydrophobic inhibitor. The piperazine exit vector (A) could be a starting point for of FSP1. Huge thx and congrats to everyone involved!

#Ferroptosis #CellDeath #targetedproteindegradation

Last updated 2 years 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 3 years ago

CRAIG M CREWS · @crews
946 followers · 1224 posts · Server mstdn.science

nature.com/articles/s41589-022
Nice addition to the literature but I wouldn't describe it as "a new strategy of targeted protein degradation through direct substrate recruitment to the 26S proteasome" since Janse and Church first described this approach in 2004. pubmed.ncbi.nlm.nih.gov/150394

#targetedproteindegradation #PROTACs

Last updated 3 years ago

jobRxiv · @jobRxiv
688 followers · 438 posts · Server mas.to
Guillaume Laconde · @Laconde
85 followers · 25 posts · Server mstdn.science

Solid-Phase Synthesis of Cereblon-Recruiting Selective Histone Deacetylase 6 Degraders (HDAC6 PROTACs) with Antileukemic Activity. Very nice PROTAC SPPS synthesis pubs.acs.org/doi/10.1021/acs.j

#targetedproteindegradation

Last updated 3 years ago

Guillaume Laconde · @Laconde
85 followers · 24 posts · Server mstdn.science

A Comprehensive Overview of Small-Molecule Androgen Receptor Degraders: Recent Progress and Future Perspectives pubs.acs.org/doi/10.1021/acs.j

#targetedproteindegradation

Last updated 3 years ago

Guillaume Laconde · @Laconde
83 followers · 22 posts · Server mstdn.science

Bridged Proteolysis Targeting Chimera (PROTAC) Enables Degradation of Undruggable Targets pubs.acs.org/doi/10.1021/jacs.

#targetedproteindegradation

Last updated 3 years ago

Katherine Reiter · @kreiter
86 followers · 4 posts · Server mstdn.science
Guillaume Laconde · @Laconde
80 followers · 19 posts · Server mstdn.science

After some year now it's time to tweet about my former work. Today we publish a patent with a nice PROTAC approach on PXR nuclear receptor. This receptor, well knew, have not a real antagonist. So, we were decided to make a PROTAC for this target. From in-house agonist, we make a PROTAC. Tricky challenge. And after many synthesis efforts, some PROTAC have showed interesting PXR degradation. And some in-vivo results validate this approach. bit.ly/3GH6aku

#targetedproteindegradation

Last updated 3 years ago

Guillaume Laconde · @Laconde
78 followers · 18 posts · Server mstdn.science

DeepPROTACs is a deep learning-based targeted degradation predictor for PROTACs nature.com/articles/s41467-022

#targetedproteindegradation

Last updated 3 years ago

CRAIG M CREWS · @crews
430 followers · 163 posts · Server mstdn.science

It's really nice to be recognized again this year as a highly cited researcher. I thank the community for this honor.

clarivate.com/highly-cited-res

#targetedproteindegradation #TPD #ChemicalBiology

Last updated 3 years ago

Geordi Frere · @geordifrere
0 followers · 1 posts · Server mstdn.science

Hi Mastodon, I'm Geordi! I'm a /#chembio PhD student in Scott Prosser and Patrick Gunning's labs at the University of Toronto Mississauga! Lately, I've taken an interest in and I wrote a chapter on molecular glue degraders in MCB: Biomolecular Interactions! (1/2)
sciencedirect.com/science/arti

#medchem #targetedproteindegradation

Last updated 3 years ago

Guillaume Laconde · @Laconde
40 followers · 16 posts · Server mstdn.science
Guillaume Laconde · @Laconde
37 followers · 15 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 3 years ago

Guillaume Laconde · @Laconde
35 followers · 13 posts · Server mstdn.science

Old target New PROTAC 😉from
@KymeraTx CDK2 PROTAC bit.ly/3hEWJYl

#targetedproteindegradation

Last updated 3 years ago

CRAIG M CREWS · @crews
350 followers · 142 posts · Server mstdn.science
Jeffrey Dubins · @jsdubins
26 followers · 18 posts · Server mstdn.science

Hi Mastodon world. I am a recently retired Molecular biologist/in vitro pharmacologist. I spent the last 4 years researching mRNA therapeutics and vaccines at Translate Bio, now a Sanofi company. I have also done some research. I am here to keep involved with some of the ongoing research as I am not ready to completely walk away from science. I look forward to reading about all the advances everyone will make!

#targetedproteindegradation

Last updated 3 years ago