PKMYT1 is a promising target for #cancer #drug developmenent. While some inhibitors such as RP-6036 are available for some time, researchers from InSilico #Medicine have now introduced a novel #PROTAC degrader based on their computational design of a novel inhibitor. This study was now published in #Nature Communications (2025):
https://www.nature.com/articles/s41467-025-65796-8
#drugdesign #chemistry #MedicinalChemistry #research #science
C=CC(O)=C9C)=C8C#N)N7)C=N6)CC5)C4)CC3)C(F)=C2)CCC1=O
Yazhou Wang et al. Nature Communication 16, 10759 (2025)
10.1038/s41467-025-65796-8](https://files.mastodon.social/cache/media_attachments/files/115/704/561/145/954/113/original/595df0fd29334962.png)
🤖 Can AI help us predict and prevent off-target effects in PROTAC drug design?
🔗 Predicting PROTAC off-target effects via warhead involvement levels in drug–target interactions using graph attention neural networks. Computational and Structural Biotechnology Journal, DOI: https://doi.org/10.1016/j.csbj.2025.10.028
📚 CSBJ: https://www.csbj.org/
#DrugDevelopment #StructuralBiology #ChemicalBiology #PROTAC #DrugDiscovery #Cheminformatics #Bioinformatics #PrecisionMedicine #TargetedProteinDegradation
🧩 The future of drug discovery may depend on how well we understand PROTAC-driven protein partnerships.
🔗 Mapping the energy landscape of PROTAC-mediated protein-protein interactions. Computational and Structural Biotechnology Journal, DOI: https://doi.org/10.1016/j.csbj.2023.02.049
📚 CSBJ: https://www.csbj.org/
#StructuralBiology #PROTAC #DrugDiscovery #ComputationalBiology #ProteinEngineering #ProteinDegradation #Biopharma #MedicinalChemistry #TargetedTherapies #AIinBiotech #MolecularModeling
AI Breakthrough By UW Scientists Targets ‘Undruggable’ Proteins, Paving Path to Novel Therapies.
#UndruggableNoMore, #AIDrugDiscovery, #PROTAC, #TargetedProteinDegradation, #UWMedicine, #CancerTherapy, #AlzheimersResearch, #MedicalBreakthrough,
Postdoctoral Fellow
Ruijin Hospital
The new Frontiers in Therapeutics Research Laboratory is an exciting opportunity to launch your career in translational research.
See the full job description on jobRxiv: https://jobrxiv.org/job/ruijin-hospital-27778-postdoctoral-fellow/?feed_id=97619
#Cancer_Pharmacology #cell_biology #lnp_mrna #protac #ScienceJobs #hiring #research
https://jobrxiv.org/job/ruijin-hospital-27778-postdoctoral-fellow/?feed_id=97619
Postdoctoral Fellow
Ruijin Hospital
The new Frontiers in Therapeutics Research Laboratory is an exciting opportunity to launch your career in translational research.
See the full job description on jobRxiv: https://jobrxiv.org/job/ruijin-hospital-27778-postdoctoral-fellow/?feed_id=97290
#Cancer_Pharmacology #cell_biology #lnp_mrna #protac #ScienceJobs #hiring #research
https://jobrxiv.org/job/ruijin-hospital-27778-postdoctoral-fellow/?feed_id=97290
Postdoctoral Fellow
Ruijin Hospital
The new Frontiers in Therapeutics Research Laboratory is an exciting opportunity to launch your career in translational research.
See the full job description on jobRxiv: https://jobrxiv.org/job/ruijin-hospital-27778-postdoctoral-fellow/?feed_id=97031
#Cancer_Pharmacology #cell_biology #lnp_mrna #protac #ScienceJobs #hiring #research
https://jobrxiv.org/job/ruijin-hospital-27778-postdoctoral-fellow/?feed_id=97031
Postdoctoral Fellow
Ruijin Hospital
The new Frontiers in Therapeutics Research Laboratory is an exciting opportunity to launch your career in translational research.
See the full job description on jobRxiv: https://jobrxiv.org/job/ruijin-hospital-27778-postdoctoral-fellow/?feed_id=96653
#Cancer_Pharmacology #cell_biology #lnp_mrna #protac #ScienceJobs #hiring #research
https://jobrxiv.org/job/ruijin-hospital-27778-postdoctoral-fellow/?feed_id=96653
Postdoctoral Fellow
Ruijin Hospital
The new Frontiers in Therapeutics Research Laboratory is an exciting opportunity to launch your career in translational research.
See the full job description on jobRxiv: https://jobrxiv.org/job/ruijin-hospital-27778-postdoctoral-fellow/?feed_id=96527
#Cancer_Pharmacology #cell_biology #lnp_mrna #protac #ScienceJobs #hiring #research
https://jobrxiv.org/job/ruijin-hospital-27778-postdoctoral-fellow/?feed_id=96527
Postdoctoral Fellow
Ruijin Hospital
The new Frontiers in Therapeutics Research Laboratory is an exciting opportunity to launch your career in translational research.
See the full job description on jobRxiv: https://jobrxiv.org/job/ruijin-hospital-27778-postdoctoral-fellow/?feed_id=96324
#Cancer_Pharmacology #cell_biology #lnp_mrna #protac #ScienceJobs #hiring #research
https://jobrxiv.org/job/ruijin-hospital-27778-postdoctoral-fellow/?feed_id=96324
Postdoctoral Fellow
Ruijin Hospital
The new Frontiers in Therapeutics Research Laboratory is an exciting opportunity to launch your career in translational research.
See the full job description on jobRxiv: https://jobrxiv.org/job/ruijin-hospital-27778-postdoctoral-fellow/?feed_id=95939
#Cancer_Pharmacology #cell_biology #lnp_mrna #protac #ScienceJobs #hiring #research
https://jobrxiv.org/job/ruijin-hospital-27778-postdoctoral-fellow/?feed_id=95939
Postdoctoral Fellow
Ruijin Hospital
The new Frontiers in Therapeutics Research Laboratory is an exciting opportunity to launch your career in translational research.
See the full job description on jobRxiv: https://jobrxiv.org/job/ruijin-hospital-27778-postdoctoral-fellow/?feed_id=95680
#Cancer_Pharmacology #cell_biology #lnp_mrna #protac #ScienceJobs #hiring #research
https://jobrxiv.org/job/ruijin-hospital-27778-postdoctoral-fellow/?feed_id=95680
Postdoctoral Fellow
Ruijin Hospital
The new Frontiers in Therapeutics Research Laboratory is an exciting opportunity to launch your career in translational research.
See the full job description on jobRxiv: https://jobrxiv.org/job/ruijin-hospital-27778-postdoctoral-fellow/?feed_id=95470
#Cancer_Pharmacology #cell_biology #lnp_mrna #protac #ScienceJobs #hiring #research
https://jobrxiv.org/job/ruijin-hospital-27778-postdoctoral-fellow/?feed_id=95470
The July Issue of @CellChemBiol is live! Read it here: https://www.cell.com/cell-chemical-biology/current?utm_source=dlvr.it&utm_medium=mastodon #smoothened #hedgehog #optogenetics #NaVs #Rho-GTPase #YAP1 #MesenchymalStemCells #K2Pchannels #PROTAC #deubiquitylase #chromatin #PARPinhibitors
Targeted protein degradation #PROTAC is a promising avenue for drug development. This study shows that alkenyl oxindole compounds act as novel #E3ligase ligands & recruit the CRL4-DCAF11 E3 #ubiquitin ligase complex for substrate degradation #PLOSBiology https://plos.io/3WV1U9q
#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. https://www.biorxiv.org/content/10.1101/2023.04.09.536153v1
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
… need to wrangle molecule geometries, etc, to achieve productive ubiquitination by unnatural ligase for TPD therapeutics. And thus less chemistry = quicker development. Great example of ever expanding induced proximity modalities. #TPD #proximity #PROTAC #ubiquitin /end
The lysosomal degraders
#PROTAC +derivatives
An update on Research & Commercialization of #MolecularGlue for targeted protein degradation
"LYTACs, ATACs, AbTACs, KineTACs, PROTABs, AUTACs, ATTECs and AUTOTACs"
Ken Garber Nature Biotech 2022
https://www.nature.com/articles/s41587-022-01594-7
Happy #Heterobifunctional Holidays from the Crewslab! #PROTAC #chemicalbiology #Yale
