🚨 Exciting News! 🚨 What happens when unconventional ideas drive to push boundaries? 🚀 Meet FerroTACs: a novel #PROTAC design using ferrocene as core unit to re-imagining linker design and fine-tune their phys-chem properties. Learn more about our work led by @alesalerno.bsky.social here: 🧪👇 1/5 - ThreadSky

alessiociulli.bsky.social • 90 days ago

🚨 Exciting News! 🚨

What happens when unconventional ideas drive to push boundaries? 🚀 Meet FerroTACs: a novel #PROTAC design using ferrocene as core unit to re-imagining linker design and fine-tune their phys-chem properties. Learn more about our work led by @alesalerno.bsky.social here: 🧪👇 1/5

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jsrosenblum.bsky.social•90 days ago

How many postdocs said No Way when you suggested they try this?
😅😁

alessiociulli.bsky.social•90 days ago

Loads! The idea first emerged ~7y ago at a group meeting, @andre-head.bsky.social recalls well. He was keen but had his hands full. 4 years later until anyone took the suggestion seriously (Claudia) she had many plates spinning too but @alesalerno.bsky.social had just joined and really run with it!

jsrosenblum.bsky.social•90 days ago

♥️😅

chemepi.bsky.social•90 days ago

Really cool, congrats!

alessiociulli.bsky.social•90 days ago

Cool to learn you like it! 👍

alessiociulli.bsky.social•90 days ago

We integrated in the linker ferrocene—an organometallic structure with freely rotating cyclopentadienyl rings around a sandwiched iron metal ion. This unique “molecular hinge” introduces dynamic flexibility and chameleonicity to PROTACs. ⚙️✨ 2/5

alessiociulli.bsky.social•90 days ago

Compared to benchmark PROTACs from 3 different classes, not just BETs (!) but also VHL and CRBN degraders, FerroTACs achieved:
✅Intramolecular interactions that foster a folded state in non-polar environments
✅Robust target degradation
✅Improved cell permeability
✅Reduced efflux liabilities
3/5

alessiociulli.bsky.social•90 days ago

Our findings, supported by NMR conformational analyses, reveal ferrocene’s ability to act as a versatile and effective dynamic linker in PROTACs. This opens up new avenues for designing next-gen chemical tools and starting points for therapeutics with optimised molecular dynamics. 🌟 4/5

alessiociulli.bsky.social•90 days ago

Last Christmas, Claudia and Alessandra gave us DCC PROTACs https://doi.org/10.26434/chemrxiv-2023-tz70z .. This year, to keep us in the theme, they together with Lianne are giving us something special.. 🎶 Big kudos to them all and great job @alesalerno.bsky.social for championing this. Let us know your thoughts! 5/5

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