One of my must-read papers in J. Med. Chem. @[email protected] is the annual compilation of fragment-to-lead cases. The 2021 edition comprises 28 entries, several for difficult-to-drug targets. For kinases fragments can provide an entry into structure-based design https://pubs.acs.org/doi/10.1021/acs.jmedchem.2c01827
🐦🔗: https://twitter.com/HartungIngo/status/1619997596784955392
Progress in targeted protein degradation (#TPD) is limited by a scarcity of know-how about human E3s. High quality chemical probes can help to bridge that gap as now exemplified for #GID4 by scientists @[email protected] & @[email protected] #OpenScience https://www.biorxiv.org/content/10.1101/2023.01.17.524225v1 @[email protected]
🐦🔗: https://twitter.com/HartungIngo/status/1619664917963104257
Stop by the Molecular Glue Degrader Summit today to hear Sharon Townson discuss the advanced capabilities of Monte Rosa's QuEEN platform.
🐦🔗: https://twitter.com/MonteRosaTx/status/1618224310992408579
Is it BCP? Cubane?
Oh no, it is O-[2.2.2] - ideal Ph-bioisoster!
@[email protected]: http://bit.ly/3XAJKY1
🐦🔗: https://twitter.com/MykhailiukChem/status/1618127144756088833
The phenyl ring is a basic structural element in chemistry, and we learn about it already in school. We have developed an “ideal” saturated bioisoster of the para-substituted phenyl ring, - 2 oxabicyclo[2.2.2]octane. Its incorporation into Imatinib drug led to dramatic improvement of all physicochemical properties. This study opens new horizons in science, given the commonplace of the phenyl ring everywhere.
They developed a confirmation specific antibody that probes the active state of CRL1-4 to allow workflows to characterize active ligases in various cell lines, types, and in response to environmental stimuli.
Today we expanded our commitment to An Accord for a Healthier World to now enable access to ~500 Pfizer patented and off-patent medicines and vaccines on a not-for-profit basis to 45 lower-income countries. Learn More: https://on.pfizer.com/3knurTN #WEF23 #HealthEquity
Today we pay tribute to the extraordinary life and legacy of Dr. King, and reflect on the lessons he taught us. Thanks to everyone who joined the @[email protected] to lend a hand in Chicago.
🐦🔗: https://twitter.com/BarackObama/status/1615100038409248769
IRAK4 PROTAC after @[email protected] and @[email protected] now it's @[email protected] to find other degrader for this "Hot🔥" Target. https://bit.ly/3QAUi6H
🐦🔗: https://twitter.com/Trankill34/status/1613549922871316480
This disclosure relates to compounds of Formula (A): Formula (A), or a pharmaceutically acceptable salt thereof, wherein DSM is a degradation signaling moiety that is covalently attached to the linker L, L is a linker that covalently attaches IRAK to DSM; and IRAK is an IRAK4 binding moiety represented by Formula (I) that is covalently attached to linker L; Formula (I) in which all of the variables are as defined in the application. Compounds or pharmaceutically acceptable salts thereof as described herein are capable of activating the selective ubiqitination of IRAK4 proteins via the ubiquitin-proteasome pathways (UPP) and cause degradation of IRAK4 proteins. The present disclosure also provides methods of treating disorders responsive to modulation of IRAK4 activity and/or degradation of IRAK4 with at least one compound described herein.
DEGRADERS OF WILD-TYPE AND MUTANT FORMS OF LRRK2 from @[email protected] @[email protected] #NathanaelGray again and always 😉https://bit.ly/3CIPZjR
🐦🔗: https://twitter.com/Trankill34/status/1613539470674124800
It's day 3 of #JPM2023! Today, #Arvinas Pres & CEO, @[email protected], will be presenting on Arvinas’ role in pioneering the future of #Targetedproteindegradation at 1:30 PM PT.
If you’re attending #JPM2023, we hope to see you at today’s presentation!
🐦🔗: https://twitter.com/ArvinasInc/status/1613173868507828225
