MUDASSAR SALEEMThe proteins that haunted scientists for 50+ years, transcription factors, scaffolding proteins, βundruggableβ targets, are now vulnerable.
We're not improving old drugs. We're creating an entirely new class of medicine.
Welcome to the protein degradation revolution. π§¬π
What disease area needs this tech most? π #PROTACs #DrugDiscovery #Biotech #Innovation
John Vaccaro (johniac)
Cell Chemical BiologyInduced proximity in biology and therapeutics: Read the editorial to learn more about Induced Proximity and the articles you will find in the Special Issue. #PROTACs #RNATACs #Therapeutics #Velcrins #Wnt #KEAP1 #MolecularGlues #Bifunctional #PPI #Epigenetics #glycoRNA #photocatalytic #TPD #LyTACs https://www.cell.com/cell-chemical-biology/fulltext/S2451-9456(24)00218-6?rss=yes&utm_source=dlvr.it&utm_medium=mastodon
CellBioNewsReview: #PROTACs targeting #epigenetic #proteins
https://phys.org/news/2023-12-protacs-epigenetic-proteins.html
Review: PROTACs targeting epigenetic proteins
The field of epigenetics focuses on alterations in gene function that are inherited without changes in the DNA sequence, including histone modifications, post-translational modifications of amino acids, and covalent modifications of DNA bases. These alteration pathways modulate the transformation of genotypes into specific phenotypes.
Girinath PillaiJust learned about #PROTACs, a promising new class of drugs that target #protein degradation! Exciting times in the world of drug discovery. π§ͺπ
Did you know that #PROTACs work by recruiting an E3 ubiquitin ligase to a target protein, tagging it for degradation by the proteasome? #sciencefacts π€π¬
I'm fascinated by the potential of #PROTACs to target disease-causing proteins that are traditionally considered "undruggable." Can't wait to see what the future holds. #drugdiscovery π
jobRxivThe Ferguson lab is recruiting for multiple postdoc positions in San Diego! @FleurMFerguson
Chemical Biology / Neurodegeneration
Med Chemistry, Chemical Biology
Cancer Chemical Biology, Pharmacology
CRAIG M CREWShttps://www.nature.com/articles/s41589-022-01218-w
Nice addition to the #targetedproteindegradation 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. https://pubmed.ncbi.nlm.nih.gov/15039430/ #PROTACs
Nice addition to the #targetedproteindegradation 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. https://pubmed.ncbi.nlm.nih.gov/15039430/ #PROTACs
Targeted degradation via direct 26S proteasome recruitment - Nature Chemical Biology
Discovery of macrocyclic ligands to the 19S regulatory particle protein PSMD2 enables the synthesis of heterobifunctional molecules that demonstrate proof-of-concept, targeted degradation of BRD4 through direct engagement of the 26S proteasome.
@angadmehta Itβs was good to visit again and thank you for the honor of inviting me to give this yearβs Rinehart Lecture. #chemicalbiology #Protacs #naturalproducts
Ingo HartungQuality criteria for traditional chemical #probes (reversible inhibitors of protein function or protein-protein interactions) have been broadly embraced by cell biology & target validation labs. Covalent protein modulators & small molecular protein degraders are now becoming very popular and will likely soon be used for target validation studies. This calls for a discussion about quality criteria for such probes as well. Here is a first proposal for such criteria for degrader probes. Comments are welcome. #TPD #PROTACs #OpenScience #SGC
Ni-catalyzed photoredox couplings in an oscillatory flow reactor (to allow for handling of slurries) for accessing versatile CRBN-engaging building blocks for #PROTACs. From our collaboration with the Kappe group at University Graz: now published in ChemCatChem https://chemistry-europe.onlinelibrary.wiley.com/doi/10.1002/cctc.202201184
