Stephan HackerOct 24, 2024
Very interesting talk by Kyle Mangano of Amgen at the Dana-Farber Targeted Protein Degradation Webinar #TPD #TPDWebinar. He talked about his work on hijacking viral E3 ligases for targeted protein degradation using the VIPER-TAC modality. https://www.biorxiv.org/content/10.1101/2024.08.13.607762v1
Stephan HackerSep 12, 2024
Interesting talk by Liron Bar-Peled at #TPDWebinar. He talked about his group's work on expanding the druggable proteome in cancers by using chemoproteomics to profile ligandable cysteines. Interesting insights into ligandability across diverse cancers. https://www.sciencedirect.com/science/article/abs/pii/S0092867424003180
Interesting results also on molecules with two cysteine-directed reactive groups that act as molecular superglues that permanently link together two proteins. https://www.biorxiv.org/content/10.1101/2024.07.16.603666v1
DrugMap: A quantitative pan-cancer analysis of cysteine ligandability

Cysteine-focused chemical proteomic platforms have accelerated the clinical development of covalent inhibitors for a wide range of targets in cancer. …

Stephan HackerSep 12, 2024
Interesting talk by Pamela Ting from Novartis at #TPDWebinar. She talked about the application of degraders in the field of Sickle cell disease. They identified a degrader for the transcription factor WIZ that leads to induction of fetal hemoglobin https://www.sciencedirect.com/science/article/abs/pii/S0006497123735398
Targeted Degradation of the Wiz Transcription Factor for Gamma Globin De-Repression

Sickle cell disease (SCD) is a life-threatening genetic condition arising from a point mutation in the β-globin gene that causes hemoglobin polymeriza…

Stephan HackerSep 12, 2024
Interesting talk by Samantha Bevill at #TPDWebinar. She talked about her research into developing tumor-specific PROTACs on the example of engaging the E3 ubiquitin ligase MDM2 to specifically degrade proteins in MDM2-amplified cancer cells. https://www.cell.com/cell-genomics/fulltext/S2666-979X(23)00089-7
Stephan HackerSep 12, 2024
The Dana Farber Targeted Protein Degradation #TPDWebinar is off to a great start with an insightful talk by Eric Fischer. He talked about his group's work on the functional targets of thalidomide and how to identify new (covalent) molecular glues. https://www.nature.com/articles/s41589-024-01668-4
Template-assisted covalent modification underlies activity of covalent molecular glues - Nature Chemical Biology

Characterization of DCAF16-based BRD4 molecular glue degraders revealed a trans-labeling mechanism termed ‘template-assisted covalent modification’, which opens a new path for proximity-driven pharmacology.

Nature
Radek NowakNov 17, 2022
Join us tomorrow for Mikko Taipale #TPDwebinar 12:00 noon EST. Register to join via zoom at https://www.danafarbertargetedproteindegradation.org/
Upcoming Speakers | Targeted Protein Degradation Webinar Series

Targeted Protein Deg