David E. Heppner

Congrats to Abdul!

RSC Medicinal Chemistry promotional graphic for the Kinases themed collection.

📢We are delighted to share our latest themed collection on Kinases, guest edited by Hayley Binch, @heppnerd.bsky.social, Meizhong Jin and Philip Jones!

Explore the articles that make up this fantastic collection, here👇
pubs.rsc.org/en/journals/...

#chemsky 🧪

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SBGrid's eLife paper received a citation in August from @heppnerd.bsky.social from @sunyofficial.bsky.social at Buffalo in Journal of Medicinal Chemistry: Profiling and Optimizing Targeted Covalent Inhibitors through EGFR-Guided Studies.

Read more here: buff.ly/VwDYVh2

#SBGrid #ScienceMatters

Profiling and Optimizing Targeted Covalent Inhibitors through EGFR-Guided Studies Targeted covalent inhibitors (TCIs) are actively pursued in drug discovery due to their prolonged target engagement and clinical efficacy. Although kinetic parameters provide a path to their optimizat...

New paper out today in J. Med. Chem. pubs.acs.org/doi/10.1021/...

Honestly, this is the content we all need right now.

Thanks for your highlight, Erik!

Enhancing Selectivity and Potency of SNAr Covalent Inhibitors of NADPH Oxidase Enzymes Dysregulated reactive oxygen species (ROS) are implicated in various diseases, positioning NADPH oxidase enzymes (NOXs) as attractive therapeutic targets. However, progress in tool compound discovery ...

Sharing our most recent research published in #JMedChem @acsmedi.bsky.social @pubs.acs.org pubs.acs.org/doi/10.1021/...

An honor to be included in this class of impressive investigators!

a young man is smiling and talking about bingo . ALT: a young man is smiling and talking about bingo .

RIP Val Kilmer who gave us Chris Knight and the classic (we can drop “cult”, right?) “Real Genius”. A timeless treasure that hits home again and again.

Clearly something NY should strongly consider!

Drug Discovery and Development Faces an Ominous Future from NIH Indirect Costs Rate Cuts

Drug Discovery and Development Faces an Ominous Future from NIH Indirect Costs Rate Cuts
pubs.acs.org/doi/10.1021/...

Drug Discovery and Development Faces an Ominous Future from NIH Indirect Costs Rate Cuts

Drug Discovery and Development Faces an Ominous Future from NIH Indirect Costs Rate Cuts pubs.acs.org/doi/10.1021/...

Ascertaining a Structural Basis in Drug Discovery and Development OR SEARCH CITATIONS

New editorial in #JMedChem on “Ascertaining a Structural Basis in Drug Discovery and Development.” @pubs.acs.org @acsmedi.bsky.social

pubs.acs.org/doi/10.1021/...

Deep Cuts to Medical Research Funds Could Hobble University Budgets Grants from the National Institutes of Health come with additional money for overhead. Proposed funding cuts would leave colleges with large budget gaps.

NEW: The N.I.H. will cut about $4 Billion from federal research grants that support cancer, virus and heart disease research.

#Project2025 called for the cuts to end subsidies to "leftist" university agendas.

www.nytimes.com/2025/02/07/u...

NIH cuts billions of dollars in biomedical funding, effective immediately The move halts a large slice of money for most universities and research institutions virtually overnight, imperiling vital research in everything from cancer to heart disease.

NIH has cut billions of dollars in biomedical funding, effective immediately
The move halts a large slice of money for most universities and research institutions virtually overnight, imperiling vital research in everything from cancer to heart disease.

www.washingtonpost.com/health/2025/...

NIH cuts billions of dollars in biomedical funding, effective immediately The move halts a large slice of money for most universities and research institutions virtually overnight, imperiling vital research in everything from cancer to heart disease.

Another assault on US competitiveness at a time when biomedicine is roaring with innovation, an own-goal in a high-stakes international tournament. Of course the real losers are American people needing medicines and cures.

www.washingtonpost.com/health/2025/...

You finally get to one that I would truly resonate with…

Protein Data Bank (PDB) Deposition Service struggling today.

What a great way to round out a year! Thanks to Gunda Georg for hosting and the many members of the medicinal chemistry department, @umnchemistry.bsky.social, and others for the great meetings and opportunity to share our story.

Hi Bluesky 👋 We're looking forward to sharing our departmental news on this new platform. Please spread the word that we've joined!

We’re excited to announce that the ACS Division of Medicinal Chemistry is now on Bluesky! 🦋🔵

Follow us for updates on awards & fellowships, meetings, webinars, editorials, and all things MEDI. Stay connected with the latest news from the Division! 📣

Tilting the Scales toward EGFR Mutant Selectivity: Expanding the Scope of Bivalent “Type V” Kinase Inhibitors Binding multiple sites within proteins with bivalent compounds is a strategy for developing uniquely active agents. A new class of dual-site inhibitors has emerged targeting the epidermal growth factor receptor (EGFR) anchored to both the orthosteric (ATP) and allosteric sites. Despite proof-of-concept successes, enabling selectivity against oncogenic activating mutations has not been achieved and classifying these inhibitors among kinase inhibitors remains underexplored. This study investigates the structure–activity relationships, binding modes, and biological activity of ATP-allosteric bivalent inhibitors (AABIs). We find that AABIs selectively inhibit drug-resistant EGFR mutants (L858R/T790M and L858R/T790M/C797S) by anchoring a methyl isoindolinone moiety along the αC-helix channel of the allosteric site. In contrast, related Type I1/2 inhibitors target wild-type EGFR but are less effective against resistant mutants. This shift in selectivity demonstrates that mutant-selective AABIs classify as “Type V” bivalent inhibitors.

Our most recent work discovering bivalent Type V kinase inhibitors in collaboration with Stefan Laufer Eberhard Karls Universität Tübingen published in J. Med. Chem.
pubs.acs.org/doi/full/10....

Many thanks, Prof. Lacy!

The one time I really want to try streak seeding the cat has not left one of her typically reliable whiskers.

The Hallmarks of Precancer Summary:. Research on precancers, as defined as at-risk tissues and early lesions, is of high significance given the effectiveness of early intervention. We discuss the need for risk stratification to...

Earlier this year, we published an article in Cancer Discovery discussing six hallmarks of precancer and highlighting the need for a multi-omics approach to research in this area. aacrjournals.org/cancerdiscov...

Would love to connect with others working in this area!

Oh, my! I was operating under the assumption that I hadn’t put myself out there strong enough! Thanks.

Welcome to Bluesky! I created a starter pack for medicinal chemistry. Please comment/share and let me know if you wish to be added to the starter pack.

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Would appreciate being added!

📯📯 Chemical Biology starter pack 📯📯
140 PIs & groups posting primary research in chemical biology.

Please reskeet (?) & reply to this post if you want to be added!
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Mind adding my account? Thanks!