Ziemowit_Pokladek

Targeted protein #degradation: from mechanisms to #clinic. New molecular mechanisms can rapidly be translated - we can learn so much from nature. Great to be able to share this piece with @jonathanMtsai Ben Ebert and Eric Fischer @fischerlab1. #TPD nature.com/articles/s4158…

📚💡Linker-free PROTACs efficiently induce the degradation of oncoproteins nature.com/articles/s4146… #TPD #Targeted_Protein_Degradation #PROTAC

❗ 📚💡A comprehensive mechanistic investigation of factors affecting intestinal absorption and bioavailability of two PROTACs in rats sciencedirect.com/science/articl… #TPD #Targeted_Protein_Degradation #CRBN

📚💡Proteome-Wide Discovery of Degradable Proteins Using Bifunctional Molecules from AbbVie biorxiv.org/content/10.110… #TPD #Targeted_Protein_Degradation

📚Equilibrium Drives Cyclosporine Membrane Permeability: The Goldilocks Energy Barriers pubs.acs.org/doi/10.1021/ac… #permeability

❗📚💡Discovery of Daraxonrasib (RMC-6236), a Potent and Orally Bioavailable RAS(ON) Multi-selective, Noncovalent Tri-complex Inhibitor for the Treatment of Patients with Multiple RAS-Addicted Cancers from Revolution Medicines pubs.acs.org/doi/10.1021/ac…

❗ 📚💡 PK/PD modeling of targeted protein degraders: Charting new waters and navigating the shallows sciencedirect.com/science/articl… #TPD #Targeted_Protein_Degradation

📚Leveraging Structural and Computational Biology for Molecular Glue Discovery lnkd.in/d-4wKV7p #TPD #Targeted_Protein_Degradation

📚 Structures of the 26S proteasome in complex with the Hsp70 cochaperone Bag1 reveal a novel mechanism of ubiquitin-independent proteasomal degradation biorxiv.org/content/10.110… #TPD #Targeted_Protein_Degradation

📚 Design and Discovery of Preclinical Candidate LYG-409 as a Highly Potent and Selective GSPT1 Molecular Glue Degraders pubs.acs.org/doi/10.1021/ac… #TPD #Targeted_Protein_Degradation #CRBN #GSPT1

📚💡 Replacing a Cereblon Ligand by a DDB1 and CUL4 Associated Factor 11 (DCAF11) Recruiter Converts a Selective Histone Deacetylase 6 PROTAC into a pan-degrader chemrxiv.org/engage/chemrxi… #TPD #Targeted_Protein_Degradation

📚💡 E2–Ub-R74G strategy reveals E2-specific ubiquitin conjugation profiles in live cells nature.com/articles/s4158… #TPD #Targeted_Protein_Degradation #E2

❗📚💡 The efflux pump ABCC1/MRP1 constitutively restricts PROTAC sensitivity in cancer cells from CeMM and Centre for Targeted Protein Degradation cell.com/cell-chemical-… #TPD #Targeted_Protein_Degradation

📚 Temporal and Spatial Characterization of CUL3KLHL20-driven Targeted Degradation of BET family, BRD Proteins by the Macrocycle-based Degrader BTR2004 biorxiv.org/content/10.110… #TPD #Targeted_Protein_Degradation

📚💡Frustration in the Protein-Protein interface Plays a Central Role in the Cooperativity of PROTAC Ternary Complexes biorxiv.org/content/10.110… #TPD #Targeted_Protein_Degradation

❗ 📚💡A Kinetic Scout Approach Accelerates Targeted Protein Degrader Development #TPD #Targeted_Protein_Degradation

📚💡 Degrading the key component of the inflammasome: Development of an NLRP3 PROTAC chemrxiv.org/engage/chemrxi… #TPD #Targeted_Protein_Degradation #Protac

Crystal structures of DCAF1-PROTAC-WDR5 ternary complexes provide insight into DCAF1 substrate specificity nature.com/articles/s4146… #TPD #Targeted_Protein_Degradation #PROTAC #TCF

📚💡 Covalent Targeting of Histidine Residues with Aryl Fluorosulfates: Application to Mcl-1 BH3 Mimetics pubs.acs.org/doi/10.1021/ac… #Covalent

❗❗ 📚💡 Structural basis for C-degron selectivity across KLHDCX family E3 ubiquitin ligases nature.com/articles/s4146… #TPD #Targeted_Protein_Degradation